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oral GLP-1 small molecule

Danuglipron

Published evidence · coverage incomplete

Anatomy in the research

Explore the structures studied.

These are anatomical mentions in cited research—not established treatment targets or proof of benefit in people.

Kidney · 5 cited passage(s)

Population: healthy participants with normal renal function and participants with t2d across normal, mild, moderate, or severe renal impairment (n = 39)

This Phase 1, open‐label study evaluated the effect of renal impairment on the pharmacokinetics, safety, and tolerability of danuglipron (20 mg)

Applies only to the source-defined population, formulation, dose, and assessment period.

Evidence relationship: supports

Read finding and source →

Population: participants with t2d with mild, moderate, or severe renal impairment (vs t2d with normal renal function)

In participants with T2D, renal impairment had no clinically meaningful effect on the pharmacokinetic, safety, and tolerability profiles of danuglipron

Applies only to the source-defined population, formulation, dose, and assessment period.

Evidence relationship: supports

Read finding and source →

Population: healthy participants with normal renal function and participants with t2d and normal renal function

Danuglipron pharmacokinetics were similar between healthy participants and participants with T2D and normal renal function.

Applies only to the source-defined population, formulation, dose, and assessment period.

Evidence relationship: supports

Read finding and source →

Population: participants stratified by renal function (healthy normal renal function; t2d with normal, mild, moderate, or severe renal impairment)

Log‐linear regression analyses and analyses of variance showed no evidence of a clinically significant effect of reduced renal function on danuglipron pharmacokinetics.

Applies only to the source-defined population, formulation, dose, and assessment period.

Evidence relationship: supports

Read finding and source →

Population: all renal function groups in the study

Renal clearance of unchanged danuglipron was minimal (<1% across all renal function groups).

Applies only to the source-defined population, formulation, dose, and assessment period.

Evidence relationship: supports

Read finding and source →

At a glance

What is it—and why does it matter?

Danuglipron (PF-06882961) is a non-peptide, orally active small-molecule agonist of the human (and monkey) GLP-1 receptor (GLP-1R). Danuglipron is an oral small-molecule drug that activates the GLP-1 receptor. The primary endpoint was change in weight from baseline to end of treatment.

Sources for this introduction: [1] [2] [3]

This published profile is a reference in progress. Findings retain their source context; missing topics are marked below.

Simple guide

Danuglipron, in plain English

The main points from the published research. Each one links to the source it comes from.

What it is

What the research looks like

Most published findings come from studies in people.

Who or what was studied, across 52 findings:
  • 40 People 77%
  • 3 Animals or lab 6%
  • 9 Other or unclear 17%

Counts show where findings come from, not how strong they are. Animal and lab findings are counted together because study types have not been labelled for this profile yet.

What studies in people found

What animal and lab studies suggest

Not proven in people. Results in animals or cells often do not hold up in humans.

  • CHEMBL4518483 had EC50 > 20000.0 nM at mouse GLP-1 receptors in CHO cells.

    Animal or lab studyStudied in: mouse (glp-1r expressed in cho cells)
    Source for this finding
    “Standard result: EC50 > 20000.0 nM”
    ChEMBL activities for CHEMBL4518483
  • CHEMBL4518483 bound to FAP-tagged human GLP-1R in a CHO-cell radioligand binding assay with Ki = 80.0 nM (displacing [3H]PF-06883365).

    Animal or lab study
    Source for this finding
    “Assay: Displacement of [3H]PF-06883365 from FAP-tagged human GLP-1R expressed in CHO cells assessed as inhibition constant by radioligand binding assay Assay format: cell-based format Standard result: Ki = 80.0 nM”
    ChEMBL activities for CHEMBL4518483

Safety

No safety findings are published in this profile yet. Missing safety data does not mean it is safe.

What we don't know

  • Not yet covered in this profile: administration, contraindications, interactions, regulatory status, safety.

A missing finding does not mean something is safe or effective.

Study types are labelled automatically and can be wrong; each finding links to its source.

This is general information, not medical advice.

See all 70 findings and sourcesEvery finding, grouped by topic, with its exact source passages

What is it?

A molecule, not a product name.

Identity

Danuglipron (PF‐06882961) is an oral small-molecule GLP-1 receptor agonist.

Human research · design must be checked

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Danuglipron (PF‐06882961) is an oral, small‐molecule glucagon‐like peptide‐1 receptor agonist”

    Effect of Renal Impairment on the Pharmacokinetics of a Single Oral Dose of Danuglipron in Participants With Type 2 Diabetes · Abstract

Identity

Danuglipron is a novel oral small-molecule GLP-1 receptor agonist.

Human research · design must be checked

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “This study assesses the efficacy and safety of the novel oral small molecule glucagon-like peptide-1 receptor agonists (GLP-1 RAs) danuglipron and orforglipron”

    The efficacy and safety of danuglipron and orforglipron in patients with type 2 diabetes and obesity: a systematic review and meta-analysis. · OBJECTIVE

Identity

Danuglipron is an orally active, small-molecule GLP-1 receptor agonist.

Molecular / pharmacology evidence

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “the emergence of orally active small-molecule GLP-1 receptor agonists like danuglipron”

    Novel GLP-1-based Medications for Type 2 Diabetes and Obesity. · Abstract

Identity

Danuglipron (PF-06882961) is an orally active, non-peptide small-molecule agonist of the GLP-1 receptor in humans (and monkeys).

Human research · design must be checked

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Danuglipron (PF-06882961) is a small molecule, non-peptide, orally active agonist of the human (and monkey) glucagon-like peptide-1 receptor (GLP-1R) [Reference 41855] [Reference 43828].”

    IUPHAR ligand commentary · General comments

Identity

Danuglipron (PF‐06882961) is an oral small-molecule GLP-1 receptor agonist.

Human research · design must be checked

1 cited source · 1 linked study ID

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “danuglipron (PF‐06882961), an oral small‐molecule glucagon‐like peptide‐1 (GLP‐1) receptor agonist”

    Efficacy and safety of danuglipron ( <scp>PF</scp> ‐06882961) in adults with obesity: A randomized, placebo‐controlled, dose‐ranging phase 2b study · Abstract

Identity

Danuglipron (PF-06882961) is a novel oral small-molecule GLP-1 receptor agonist.

Human research · design must be checked

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “This study investigated the safety, tolerability, pharmacokinetics and pharmacodynamics of danuglipron (PF-06882961), which is a novel, oral small-molecule glucagon-like peptide-1 receptor agonist, in Japanese participants with type 2 diabetes mellitus (T2DM).”

    A phase 1 study to evaluate the safety, tolerability, pharmacokinetics and pharmacodynamics of danuglipron (PF-06882961), an oral small-molecule glucagon-like peptide-1 receptor agonist, in Japanese adults with type 2 diabetes mellitus. · AIMS

Identity

Danuglipron is an oral small-molecule GLP-1 receptor agonist that resists enzymatic breakdown.

Human research · design must be checked

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Meanwhile, the emergence of orally active small-molecule GLP-1 receptor agonists like danuglipron and orforglipron, which are resistant to enzymatic degradation, marks a major advance in patient-friendly drug delivery.”

    Novel GLP-1-based Medications for Type 2 Diabetes and Obesity. · Abstract

Identity

Danuglipron’s molecular formula is C31H30FN5O4.

Molecular / pharmacology evidence

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Molecular formula: C31H30FN5O4”

    DANUGLIPRON · Molecular properties

Identity

Danuglipron is an oral, non-peptide GLP-1 receptor agonist.

Molecular / pharmacology evidence

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Recently, oral non-peptide GLP-1 receptor agonists like danuglipron and orforglipron, which are smaller and more stable, have been investigated.”

    Gastrointestinal side effects of the non-peptide GLP-1 receptor agonists: A systematic review and meta-analysis. · BACKGROUND

Identity

Danuglipron (PF-06882961) is a non-peptide, orally active small-molecule agonist of the human (and monkey) GLP-1 receptor (GLP-1R).

Human research · design must be checked

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Danuglipron (PF-06882961) is a small molecule, non-peptide, orally active agonist of the human (and monkey) glucagon-like peptide-1 receptor (GLP-1R) [Reference 41855] [Reference 43828].”

    IUPHAR ligand commentary · General comments

Identity

Danuglipron (PF‐06882961) is a novel oral small-molecule GLP-1 receptor agonist.

Human research · design must be checked

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “danuglipron (PF‐06882961), which is a novel, oral small‐molecule glucagon‐like peptide‐1 receptor agonist”

    A phase 1 study to evaluate the safety, tolerability, pharmacokinetics and pharmacodynamics of danuglipron ( <scp>PF</scp> ‐06882961), an oral small‐molecule glucagon‐like peptide‐1 receptor agonist, in Japanese adults with type 2 diabetes mellitus · Abstract

Identity

Danuglipron is an oral GLP-1 receptor agonist.

Human research · design must be checked

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Importantly, the model also recapitulated hepatotoxicity signals observed in recent clinical development, including for Bruton's tyrosine kinase inhibitors (tolebrutinib and evobrutinib), oral glucagon-like peptide-1 receptor agonists (danuglipron vs orforglipron), synergistic toxicity on azelaprag-tirzepatide coexposure and enhanced sensitivity to the IL-17A inhibitor LY3509754 on coculture with nonparenchymal liver cells.”

    Mechanistically resolved prediction of compound hepatotoxicity using primary human liver spheroids-Application to recent real-world cases. · Abstract

Identity

Danuglipron is also called PF-06882961.

Human research · design must be checked

1 cited source · 1 linked study ID

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “We developed danuglipron (PF-06882961), an oral small-molecule GLP-1R agonist”

    Danuglipron (PF-06882961) in type 2 diabetes: a randomized, placebo-controlled, multiple ascending-dose phase 1 trial. · Abstract

Identity

Danuglipron is an oral small-molecule GLP-1 receptor agonist.

Molecular / pharmacology evidence

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Seven additional comparator trials were selected through targeted citation verification because they represented clinically relevant benchmarks for oral semaglutide in type 2 diabetes and obesity, danuglipron as another oral small-molecule GLP-1 receptor agonist, and injectable semaglutide as a high-efficacy class comparator.”

    Comparative Positioning of Orforglipron Among Selected GLP-1 Receptor Agonist Benchmarks: A Narrative Review. · Abstract

Identity

Danuglipron is a novel oral small-molecule GLP-1 receptor agonist.

Human research · design must be checked

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “The present systematic review aimed to synthesize available data from recently published randomized trials (RCTs) investigating the efficacy and safety of the novel, orally administered, small-molecule glucagon-like peptide 1 receptor agonists (GLP-1RAs) orforglipron and danuglipron for the treatment of type 2 diabetes mellitus (T2DM), obesity or both.”

    Safety and efficacy of the new, oral, small-molecule, GLP-1 receptor agonists orforglipron and danuglipron for the treatment of type 2 diabetes and obesity: systematic review and meta-analysis of randomized controlled trials. · AIMS

Identity

Danuglipron’s molecular weight is 555.61.

Molecular / pharmacology evidence

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Molecular weight: 555.61”

    DANUGLIPRON · Molecular properties

Identity

Danuglipron is an oral small-molecule GLP-1 receptor agonist.

Human research · design must be checked

1 cited source · 1 linked study ID

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “To evaluate the tolerability, safety and pharmacodynamics of different dose-escalation schemes of the oral small-molecule glucagon-like peptide-1 receptor (GLP-1R) agonist danuglipron.”

    Tolerability, safety and pharmacodynamics of oral, small-molecule glucagon-like peptide-1 receptor agonist danuglipron for type 2 diabetes: A 12-week, randomized, placebo-controlled, Phase 2 study comparing different dose-escalation schemes. · AIM

Identity

Danuglipron is a small-molecule GLP-1 receptor agonist developed by Pfizer.

Molecular / pharmacology evidence

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “The small-molecule GLP-1R agonist danuglipron, developed by Pfizer, demonstrated strong GLP-1 agonistic properties, reductions in body weight and improved glycemic control.”

    Lead-guided prodrug development of small molecules as GLP-1R agonists. · Abstract

Identity

Danuglipron is a small molecule.

Molecular / pharmacology evidence

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Molecule type: Small molecule”

    DANUGLIPRON · Molecule identity

Identity

Danuglipron (PF-06882961) is an oral small-molecule GLP-1 receptor agonist.

Human research · design must be checked

1 cited source · 1 linked study ID

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “This randomized, double-blind, placebo-controlled Phase 2b study aimed to assess the efficacy, safety, and tolerability of danuglipron (PF-06882961), an oral small-molecule glucagon-like peptide-1 (GLP-1) receptor agonist, in adults with obesity.”

    Efficacy and safety of danuglipron (PF-06882961) in adults with obesity: A randomized, placebo-controlled, dose-ranging phase 2b study. · AIMS

How does it work?

Target, response, and disposition.

Mechanism

Danuglipron is an oral GLP-1 receptor agonist.

Human research · design must be checked

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “The oral GLP-1 RAs danuglipron and orforglipron”

    The efficacy and safety of danuglipron and orforglipron in patients with type 2 diabetes and obesity: a systematic review and meta-analysis. · CONCLUSION

Mechanism

CHEMBL4518483 activated cynomolgus monkey GLP-1 receptors in CHO cells with an EC50 of 4.4 nM.

Molecular / pharmacology evidence

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Standard result: EC50 = 4.4 nM”

    ChEMBL activities for CHEMBL4518483 · Activity 24929144

Mechanism

The review aims to summarize “next-in-class” GLP-1 receptor agonists and relate molecular structure to functional activity.

Human research · design must be checked

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “This review summarizes "next-in-class" GLP-1 receptor agonists developed, identifying different relationships between the molecular structure and functional activity of agonists.”

    "Next-in-class" GLP-1R Danuglipron- and Lotiglipron-like Agonists: A Patent Review (2020-2024). · OBJECTIVE

Mechanism

GLP-1 activates the GLP-1 receptor, which leads to glucose-dependent insulin release and reduced glucagon release.

Molecular / pharmacology evidence

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Glucagon-like peptide-1 (GLP-1) is an incretin hormone secreted by intestinal endocrine L cells that activates the GLP-1 receptor (GLP-1R), leading to glucose-dependent insulin secretion and suppression of glucagon release.”

    Novel Small Molecule GLP-1R Agonists Based on 1H-Benzo[d]imidazole-5-Carboxylic Acid Scaffold. · Abstract

Mechanism

CHEMBL4518483 activated human GLP-1 receptors in CHO-K1 cells with an EC50 of 1.1 nM.

Human research · design must be checked

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

2 cited passages across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Assay: Agonist activity at human GLP-1R expressed in CHO-K1 cells assessed as cAMP accumulation incubated for 30 mins in absence of BETP by plate reader method Assay format: cell-based format Standard result: EC50 = 1.1 nM”

    ChEMBL activities for CHEMBL4518483 · Activity 24929055

  2. supports · Source-backed record
    “Standard result: EC50 = 1.1 nM”

    ChEMBL activities for CHEMBL4518483 · Activity 24929055

Mechanism

CHEMBL4518483 triggered beta-arrestin 2 recruitment at human GLP-1R with an EC50 of 490.0 nM in a PathHunter assay.

Human research · design must be checked

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Standard result: EC50 = 490.0 nM”

    ChEMBL activities for CHEMBL4518483 · Activity 24929126

Mechanism

Danuglipron is an oral small-molecule drug that activates the GLP-1 receptor.

Human research · design must be checked

1 cited source · 1 linked study ID

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “We developed danuglipron (PF-06882961), an oral small-molecule GLP-1R agonist”

    Danuglipron (PF-06882961) in type 2 diabetes: a randomized, placebo-controlled, multiple ascending-dose phase 1 trial. · Abstract

Mechanism

CHEMBL4518483 bound to FAP-tagged human GLP-1R in a CHO-cell radioligand binding assay with Ki = 80.0 nM (displacing [3H]PF-06883365).

Animal / laboratory evidence

1 cited source · Study independence not established

Animal or laboratory findings do not establish benefit or safety in people.

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Assay: Displacement of [3H]PF-06883365 from FAP-tagged human GLP-1R expressed in CHO cells assessed as inhibition constant by radioligand binding assay Assay format: cell-based format Standard result: Ki = 80.0 nM”

    ChEMBL activities for CHEMBL4518483 · Activity 24929140

Pharmacokinetics

A Phase 1 open-label study tested how renal impairment affects danuglipron (20 mg) pharmacokinetics, safety, and tolerability in several renal-function groups (N = 39).

Human research · design must be checked

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “This Phase 1, open‐label study evaluated the effect of renal impairment on the pharmacokinetics, safety, and tolerability of danuglipron (20 mg)”

    Effect of Renal Impairment on the Pharmacokinetics of a Single Oral Dose of Danuglipron in Participants With Type 2 Diabetes · Abstract

Pharmacokinetics

In people with T2D, renal impairment did not have a clinically meaningful effect on danuglipron pharmacokinetics, safety, or tolerability.

Human research · design must be checked

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “In participants with T2D, renal impairment had no clinically meaningful effect on the pharmacokinetic, safety, and tolerability profiles of danuglipron”

    Effect of Renal Impairment on the Pharmacokinetics of a Single Oral Dose of Danuglipron in Participants With Type 2 Diabetes · Abstract

Pharmacokinetics

Danuglipron exposure increased dose-proportionally at steady state (Day 56).

Human research · design must be checked

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Dose‐proportional increases in danuglipron exposure parameters were observed at steady state (Day 56).”

    A phase 1 study to evaluate the safety, tolerability, pharmacokinetics and pharmacodynamics of danuglipron ( <scp>PF</scp> ‐06882961), an oral small‐molecule glucagon‐like peptide‐1 receptor agonist, in Japanese adults with type 2 diabetes mellitus · Abstract

Pharmacokinetics

Danuglipron pharmacokinetics were similar in healthy people and in people with T2D who had normal renal function.

Human research · design must be checked

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Danuglipron pharmacokinetics were similar between healthy participants and participants with T2D and normal renal function.”

    Effect of Renal Impairment on the Pharmacokinetics of a Single Oral Dose of Danuglipron in Participants With Type 2 Diabetes · Abstract

Pharmacokinetics

Reduced renal function did not show a clinically significant effect on danuglipron pharmacokinetics in the analyses.

Human research · design must be checked

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Log‐linear regression analyses and analyses of variance showed no evidence of a clinically significant effect of reduced renal function on danuglipron pharmacokinetics.”

    Effect of Renal Impairment on the Pharmacokinetics of a Single Oral Dose of Danuglipron in Participants With Type 2 Diabetes · Abstract

Pharmacokinetics

Less than 1% of unchanged danuglipron was cleared by the kidneys across all renal-function groups.

Human research · design must be checked

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Renal clearance of unchanged danuglipron was minimal (<1% across all renal function groups).”

    Effect of Renal Impairment on the Pharmacokinetics of a Single Oral Dose of Danuglipron in Participants With Type 2 Diabetes · Abstract

What has been studied?

What the evidence says.

Comparative evidence

CHEMBL4518483 had EC50 > 20000.0 nM at mouse GLP-1 receptors in CHO cells.

Animal / laboratory evidence

1 cited source · Study independence not established

Animal or laboratory findings do not establish benefit or safety in people.

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Standard result: EC50 > 20000.0 nM”

    ChEMBL activities for CHEMBL4518483 · Activity 24929147

Comparative evidence

CHEMBL4518483 had EC50 > 20000.0 nM at rat GLP-1 receptors in CHO cells.

Animal / laboratory evidence

1 cited source · Study independence not established

Animal or laboratory findings do not establish benefit or safety in people.

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Standard result: EC50 > 20000.0 nM”

    ChEMBL activities for CHEMBL4518483 · Activity 24929145

Study findings

On Day 57, danuglipron significantly reduced fasting plasma glucose vs placebo, up to −40.87 mg/dl (90% CI −53.77 to −27.98).

Human research · design must be checked

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “and on Day 57 for fasting plasma glucose [up to −40.87 (−53.77, −27.98) mg/dl]”

    A phase 1 study to evaluate the safety, tolerability, pharmacokinetics and pharmacodynamics of danuglipron ( <scp>PF</scp> ‐06882961), an oral small‐molecule glucagon‐like peptide‐1 receptor agonist, in Japanese adults with type 2 diabetes mellitus · Abstract

Study findings

On Day 56, danuglipron significantly reduced mean daily glucose vs placebo, up to −67.89 mg/dl (90% CI −88.98 to −46.79).

Human research · design must be checked

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Significant reductions from baseline were observed with danuglipron on Day 56 for mean daily glucose [least squares mean (90% confidence interval) placebo‐adjusted difference of up to −67.89 (−88.98, −46.79) mg/dl]”

    A phase 1 study to evaluate the safety, tolerability, pharmacokinetics and pharmacodynamics of danuglipron ( <scp>PF</scp> ‐06882961), an oral small‐molecule glucagon‐like peptide‐1 receptor agonist, in Japanese adults with type 2 diabetes mellitus · Abstract

Study findings

In meta-analysis, danuglipron lowered HbA1c (MD: -0.90; 95% CI: -1.06, -0.74).

Human research · design must be checked

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Meta-analysis results demonstrated that danuglipron significantly decreased HbA1c (mean difference [MD]: -0.90; 95% CI: -1.06, -0.74)”

    The efficacy and safety of danuglipron and orforglipron in patients with type 2 diabetes and obesity: a systematic review and meta-analysis. · RESULTS

Study findings

In CHO cells, CHEMBL4518483 activated cynomolgus monkey GLP-1R (cAMP accumulation) with EC50 = 4.4 nM.

Human research · design must be checked

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Assay: Activation of cynomolgus monkey GLP-1R expressed in CHO cells assessed as increase in cAMP accumulation Assay format: cell-based format Standard result: EC50 = 4.4 nM”

    ChEMBL activities for CHEMBL4518483 · Activity 24929144

Study findings

The primary endpoint was change in weight from baseline to end of treatment.

Human research · design must be checked

1 cited source · 1 linked study ID

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “The primary endpoint was the change in weight from baseline to the end of treatment;”

    Efficacy and safety of danuglipron (PF-06882961) in adults with obesity: A randomized, placebo-controlled, dose-ranging phase 2b study. · RESULTS

Study findings

In CHO-K1 cells with human GLP-1R, CHEMBL4518483 reached 79.0% maximal effect at 20 uM.

Human research · design must be checked

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Standard result: Emax = 79.0 %”

    ChEMBL activities for CHEMBL4518483 · Activity 24929083

Study findings

On Day 57, danuglipron significantly reduced glycated haemoglobin vs placebo, up to −1.41% (90% CI −2.01% to −0.82%).

Human research · design must be checked

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “glycated haemoglobin [up to −1.41% (−2.01%, −0.82%)]”

    A phase 1 study to evaluate the safety, tolerability, pharmacokinetics and pharmacodynamics of danuglipron ( <scp>PF</scp> ‐06882961), an oral small‐molecule glucagon‐like peptide‐1 receptor agonist, in Japanese adults with type 2 diabetes mellitus · Abstract

Study findings

In meta-analysis, danuglipron increased fasting plasma insulin (MD: 2.94; 95% CI: 1.50, 4.38).

Human research · design must be checked

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Meta-analysis results demonstrated that danuglipron significantly decreased HbA1c (mean difference [MD]: -0.90; 95% CI: -1.06, -0.74), FPG (MD: -24.66; 95% CI: -30.45, -18.86) and weight (MD: -2.17; 95% CI: -3.10, -1.23) and improved FPI (MD: 2.94; 95% CI: 1.50, 4.38).”

    The efficacy and safety of danuglipron and orforglipron in patients with type 2 diabetes and obesity: a systematic review and meta-analysis. · RESULTS

Study findings

In a cell assay, danuglipron activated the human GLP-1 receptor with an EC50 of 0.71 nM (with BETP).

Human research · design must be checked

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

2 cited passages across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Standard result: EC50 = 1.1 nM”

    ChEMBL activities for CHEMBL4518483 · Activity 24929055

  2. supports · Source-backed record
    “Standard result: EC50 = 0.71 nM”

    ChEMBL activities for CHEMBL4518483 · Activity 24929050

Study findings

Danuglipron bound to FAP-tagged human GLP-1 receptors in a CHO radioligand binding assay with Ki = 80.0 nM (displacing [3H]PF-06883365).

Human research · design must be checked

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Standard result: Ki = 80.0 nM”

    ChEMBL activities for CHEMBL4518483 · Activity 24929140

Study findings

At 20 uM (without BETP), danuglipron reached 79.0% Emax in a human GLP-1 receptor cAMP assay (relative to control).

Human research · design must be checked

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Standard result: Emax = 79.0 %”

    ChEMBL activities for CHEMBL4518483 · Activity 24929083

Study findings

In a receptor-internalization assay, danuglipron had an EC50 of 230.0 nM at FAP-tagged human GLP-1 receptors in HEK293 cells.

Human research · design must be checked

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Standard result: EC50 = 230.0 nM”

    ChEMBL activities for CHEMBL4518483 · Activity 24929064

Study findings

On Day 57, danuglipron significantly reduced body weight vs placebo, up to −1.87 kg (90% CI −3.58 to −0.17).

Human research · design must be checked

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “and body weight [up to −1.87 (−3.58, −0.17) kg]”

    A phase 1 study to evaluate the safety, tolerability, pharmacokinetics and pharmacodynamics of danuglipron ( <scp>PF</scp> ‐06882961), an oral small‐molecule glucagon‐like peptide‐1 receptor agonist, in Japanese adults with type 2 diabetes mellitus · Abstract

Study findings

In meta-analysis, danuglipron lowered fasting plasma glucose (MD: -24.66; 95% CI: -30.45, -18.86).

Human research · design must be checked

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Meta-analysis results demonstrated that danuglipron significantly decreased HbA1c (mean difference [MD]: -0.90; 95% CI: -1.06, -0.74), FPG (MD: -24.66; 95% CI: -30.45, -18.86)”

    The efficacy and safety of danuglipron and orforglipron in patients with type 2 diabetes and obesity: a systematic review and meta-analysis. · RESULTS

Study findings

CHEMBL4518483 reached 36.0% maximal beta-arrestin 2 recruitment in a human GLP-1R PathHunter assay.

Human research · design must be checked

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Standard result: Emax = 36.0 %”

    ChEMBL activities for CHEMBL4518483 · Activity 24929130

Study findings

In meta-analysis, danuglipron reduced weight (MD: -2.17; 95% CI: -3.10, -1.23).

Human research · design must be checked

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Meta-analysis results demonstrated that danuglipron significantly decreased HbA1c (mean difference [MD]: -0.90; 95% CI: -1.06, -0.74), FPG (MD: -24.66; 95% CI: -30.45, -18.86) and weight (MD: -2.17; 95% CI: -3.10, -1.23)”

    The efficacy and safety of danuglipron and orforglipron in patients with type 2 diabetes and obesity: a systematic review and meta-analysis. · RESULTS

Risks and interactions

Risks, organized for scanning.

This profile does not yet contain a published summary for this topic. This is a coverage gap, not evidence that no research exists.

Products and regulatory status

Same ingredient. Different records.

This profile does not yet contain a published summary for this topic. This is a coverage gap, not evidence that no research exists.

Administration context

The practical clinical context.

This profile does not yet contain a published summary for this topic. This is a coverage gap, not evidence that no research exists.

Additional research & classification gaps

18 archived statements are kept separate from drug-effect findings. Media studies, economic models, methods, and records with unresolved scope are not used as medical-effect evidence.

Inspect contextual research (18)
Research context · scope unclassified

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Danuglipron’s ChEMBL ID is CHEMBL4518483.

Research context only—not evidence of a treatment effect.

Research context · scope unclassified

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Pfizer presented danuglipron in 2018-2019 as a “first-in-class” drug candidate that became a prototype for “next-in-class” development.

Research context only—not evidence of a treatment effect.

Research context · scope unclassified

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

The preferred name is DANUGLIPRON.

Research context only—not evidence of a treatment effect.

Research context · scope unclassified

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Danuglipron is classified as synthetic organic.

Research context only—not evidence of a treatment effect.

Research context · scope unclassified

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Danuglipron is described as an oral agent among emerging obesity therapies.

Research context only—not evidence of a treatment effect.

Research context · scope unclassified

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Danuglipron is also called Pf-06882961.

Research context only—not evidence of a treatment effect.

Research context · scope unclassified

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

The authors browsed patents (January 2021 to July 2024) containing danuglipron- and lotiglipron-like agonists in databases like Espacenet and Google Patents.

Research context only—not evidence of a treatment effect.

Analytical / formulation research

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

2 cited passages across 1 source record. 1 publication group(s) lack a resolved study identity.

In Wistar Han rats, oral danuglipron 100 mg/kg reached a Cmax of 5075.5 nM (measured up to 24 hrs).

Research context only—not evidence of a treatment effect.

  • ChEMBL activities for CHEMBL4518483
    Assay: Cmax in Wistar Han rat at 100 mg/kg, po measured upto 24 hrs by LC-MS/MS analysis Assay format: organism-based format Standard result: Cmax = 5075.5 nM
  • ChEMBL activities for CHEMBL4518483
    Assay: Cmax in Wistar Han rat at 100 mg/kg, po measured upto 24 hrs by LC-MS/MS analysis Assay format: organism-based format Standard result: Cmax = 5075.5 nM
Analytical / formulation research

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

In cynomolgus monkeys, CHEMBL4518483 had 5.0% oral bioavailability at 5 mg/kg.

Research context only—not evidence of a treatment effect.

Analytical / formulation research

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

In cynomolgus monkeys given 5 mg/kg orally, CHEMBL4518483 had oral bioavailability F = 5.0% (measured up to 24 hrs).

Research context only—not evidence of a treatment effect.

  • ChEMBL activities for CHEMBL4518483
    Assay: Oral bioavailability in cynomologus monkey at 5 mg/kg measured upto 24 hrs by LC-MS/MS analysis Assay format: organism-based format Standard result: F = 5.0 %
Analytical / formulation research

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

In human Caco-2 cells at 10 uM, CHEMBL4518483 had apical-to-basolateral permeability of 3.93 10^-6 cm/s after 120 mins.

Research context only—not evidence of a treatment effect.

  • ChEMBL activities for CHEMBL4518483
    Assay: Permeability across apical to basolateral in human Caco-2 cells at 10 uM incubated for 120 mins by LC-MS/MS analysis Assay format: cell-based format Standard result: permeability = 3.93 10^-6 cm/s
Analytical / formulation research

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

In Wistar Han rats, CHEMBL4518483 reached a Cmax of 253.78 nM after 5 mg/kg taken orally.

Research context only—not evidence of a treatment effect.

Analytical / formulation research

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

In Sprague-Dawley rats, oral danuglipron 5 mg/kg had AUC(0 to infinity) of 654.59 ng.hr.mL-1 (measured up to 24 hrs).

Research context only—not evidence of a treatment effect.

  • ChEMBL activities for CHEMBL4518483
    Assay: AUC (0 to infinity) in Sprague-Dawley rat at 5 mg/kg, po measured up to 24 hrs by LC-MS/MS analysis Assay format: organism-based format Standard result: AUC = 654.59 ng.hr.mL-1
Analytical / formulation research

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

In Sprague-Dawley rats, CHEMBL4518483 had a half-life of 3.61 hr after 5 mg/kg orally.

Research context only—not evidence of a treatment effect.

Analytical / formulation research

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

In Wistar Han rats, CHEMBL4518483 had 11.0% oral bioavailability at 5 mg/kg.

Research context only—not evidence of a treatment effect.

Analytical / formulation research

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

In Sprague-Dawley rats given 5 mg/kg orally, CHEMBL4518483 had T1/2 = 3.61 hr (measured up to 24 hrs).

Research context only—not evidence of a treatment effect.

  • ChEMBL activities for CHEMBL4518483
    Assay: Half life in Sprague-Dawley rat at 5 mg/kg, po measured up to 24 hrs by LC-MS/MS analysis Assay format: organism-based format Standard result: T1/2 = 3.61 hr
Analytical / formulation research

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

2 cited passages across 1 source record. 1 publication group(s) lack a resolved study identity.

In Wistar Han rats, oral danuglipron 5 mg/kg had a Tmax of 0.5 hr (measured up to 24 hrs).

Research context only—not evidence of a treatment effect.

Analytical / formulation research

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

2 cited passages across 1 source record. 1 publication group(s) lack a resolved study identity.

In ICR mice, oral danuglipron 5 mg/kg had bioavailability of 54.17%.

Research context only—not evidence of a treatment effect.

Research status + gaps

What still needs better answers?

  • Not yet covered in this profile: administration, contraindications, interactions, regulatory status, safety.
  • Some extracted findings are not shown because they did not pass Peplexicon's automated evidence checks.

These are the limits of this profile, not an exhaustive list of scientific uncertainties.

References + discovery

Open the records yourself.

  1. ChEMBL activities for CHEMBL4518483 ↗

    chembl-activities · published August 26, 2026 · retrieved August 26, 2026

  2. DANUGLIPRON ↗

    chembl-molecule · published August 26, 2026 · retrieved August 26, 2026

  3. Effect of Renal Impairment on the Pharmacokinetics of a Single Oral Dose of Danuglipron in Participants With Type 2 Diabetes ↗

    doi · published November 2, 2023 · retrieved September 4, 2026

  4. A phase 1 study to evaluate the safety, tolerability, pharmacokinetics and pharmacodynamics of danuglipron ( <scp>PF</scp> ‐06882961), an oral small‐molecule glucagon‐like peptide‐1 receptor agonist, in Japanese adults with type 2 diabetes mellitus ↗

    doi · published December 19, 2022 · retrieved September 9, 2026

  5. Efficacy and safety of danuglipron ( <scp>PF</scp> ‐06882961) in adults with obesity: A randomized, placebo‐controlled, dose‐ranging phase 2b study ↗

    doi · published June 20, 2025 · retrieved September 8, 2026

  6. IUPHAR ligand commentary ↗

    iuphar-comments · published August 26, 2026 · retrieved August 26, 2026

  7. danuglipron ↗

    iuphar-ligand · published August 26, 2026 · retrieved August 26, 2026

  8. Danuglipron (PF-06882961) in type 2 diabetes: a randomized, placebo-controlled, multiple ascending-dose phase 1 trial. ↗

    pubmed · published June 1, 2021 · retrieved September 8, 2026

  9. A phase 1 study to evaluate the safety, tolerability, pharmacokinetics and pharmacodynamics of danuglipron (PF-06882961), an oral small-molecule glucagon-like peptide-1 receptor agonist, in Japanese adults with type 2 diabetes mellitus. ↗

    pubmed · published March 1, 2023 · retrieved September 4, 2026

  10. Tolerability, safety and pharmacodynamics of oral, small-molecule glucagon-like peptide-1 receptor agonist danuglipron for type 2 diabetes: A 12-week, randomized, placebo-controlled, Phase 2 study comparing different dose-escalation schemes. ↗

    pubmed · published October 1, 2023 · retrieved September 4, 2026

  11. Safety and efficacy of the new, oral, small-molecule, GLP-1 receptor agonists orforglipron and danuglipron for the treatment of type 2 diabetes and obesity: systematic review and meta-analysis of randomized controlled trials. ↗

    pubmed · published December 1, 2023 · retrieved September 9, 2026

  12. Efficacy and safety of danuglipron (PF-06882961) in adults with obesity: A randomized, placebo-controlled, dose-ranging phase 2b study. ↗

    pubmed · published September 1, 2025 · retrieved September 4, 2026

  13. "Next-in-class" GLP-1R Danuglipron- and Lotiglipron-like Agonists: A Patent Review (2020-2024). ↗

    pubmed · published August 26, 2025 · retrieved September 9, 2026

  14. Novel GLP-1-based Medications for Type 2 Diabetes and Obesity. ↗

    pubmed · published March 11, 2026 · retrieved August 25, 2026

  15. The efficacy and safety of danuglipron and orforglipron in patients with type 2 diabetes and obesity: a systematic review and meta-analysis. ↗

    pubmed · published January 1, 2025 · retrieved September 3, 2026

  16. Gastrointestinal side effects of the non-peptide GLP-1 receptor agonists: A systematic review and meta-analysis. ↗

    pubmed · published December 26, 2025 · retrieved September 3, 2026

  17. Childhood obesity and cardiac risk in youth: Emerging challenges toward 2050. ↗

    pubmed · published June 1, 2026 · retrieved August 26, 2026

  18. Novel Small Molecule GLP-1R Agonists Based on 1H-Benzo[d]imidazole-5-Carboxylic Acid Scaffold. ↗

    pubmed · published March 29, 2026 · retrieved August 26, 2026

  19. Comparative Positioning of Orforglipron Among Selected GLP-1 Receptor Agonist Benchmarks: A Narrative Review. ↗

    pubmed · published June 1, 2026 · retrieved August 26, 2026

  20. Mechanistically resolved prediction of compound hepatotoxicity using primary human liver spheroids-Application to recent real-world cases. ↗

    pubmed · published August 1, 2026 · retrieved August 27, 2026

  21. Lead-guided prodrug development of small molecules as GLP-1R agonists. ↗

    pubmed · published September 15, 2026 · retrieved August 17, 2026

Publication history and provenance

Version 14 · Automated assessment · September 9, 2026

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