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
Danuglipron (PF‐06882961) is an oral small-molecule GLP-1 receptor agonist.
Source for this finding
“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
What the research looks like
Most published findings come from studies in people.
- 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
On Day 57, danuglipron significantly reduced fasting plasma glucose vs placebo, up to −40.87 mg/dl (90% CI −53.77 to −27.98).
Source for this finding
“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 mellitusOn Day 56, danuglipron significantly reduced mean daily glucose vs placebo, up to −67.89 mg/dl (90% CI −88.98 to −46.79).
Source for this finding
“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 mellitusIn meta-analysis, danuglipron lowered HbA1c (MD: -0.90; 95% CI: -1.06, -0.74).
Source for this finding
“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.In CHO cells, CHEMBL4518483 activated cynomolgus monkey GLP-1R (cAMP accumulation) with EC50 = 4.4 nM.
Source for this finding
“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 CHEMBL4518483The primary endpoint was change in weight from baseline to end of treatment.
Source for this finding
“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.
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.
Source for this finding
“Standard result: EC50 > 20000.0 nM”
ChEMBL activities for CHEMBL4518483CHEMBL4518483 bound to FAP-tagged human GLP-1R in a CHO-cell radioligand binding assay with Ki = 80.0 nM (displacing [3H]PF-06883365).
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.
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.
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
- 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.
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
- 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.
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
- 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).
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
- 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.
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
- 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.
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
- 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.
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
- 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.
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
- supports · Source-backed record
“Molecular formula: C31H30FN5O4”
DANUGLIPRON · Molecular properties
Identity
Danuglipron is an oral, non-peptide GLP-1 receptor agonist.
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
- 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).
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
- 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.
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
- 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.
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
- 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.
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
- 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.
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
- 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.
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
- 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.
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
- supports · Source-backed record
“Molecular weight: 555.61”
DANUGLIPRON · Molecular properties
Identity
Danuglipron is an oral small-molecule GLP-1 receptor agonist.
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
- 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.
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
- 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.
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
- supports · Source-backed record
“Molecule type: Small molecule”
DANUGLIPRON · Molecule identity
Identity
Danuglipron (PF-06882961) is an oral small-molecule GLP-1 receptor agonist.
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
- 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.
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
- 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.
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
- 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.
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
- 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.
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
- 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.
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
- 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
- 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.
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
- 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.
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
- 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).
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
- 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).
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
- 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.
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
- 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).
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
- 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.
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
- 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.
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
- 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.
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
- 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.
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
- 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.
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
- 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).
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
- 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).
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
- 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).
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
- 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.
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
- 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.
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
- 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.
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
- 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%).
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
- 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).
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
- 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).
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
- supports · Source-backed record
“Standard result: EC50 = 1.1 nM”
ChEMBL activities for CHEMBL4518483 · Activity 24929055
- 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).
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
- 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).
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
- 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.
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
- 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).
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
- 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).
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
- 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.
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
- 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).
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
- 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)
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.
- DANUGLIPRON
ChEMBL ID: CHEMBL4518483
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.
- "Next-in-class" GLP-1R Danuglipron- and Lotiglipron-like Agonists: A Patent Review (2020-2024).
Pfizer's danuglipron and lotiglipron, presented in 2018-2019, were "first-in-class" drug candidates, becoming prototypes for "next-in-class" drug development.
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.
- DANUGLIPRON
Preferred name: DANUGLIPRON
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.
- danuglipron
Type: Synthetic organic
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.
- Childhood obesity and cardiac risk in youth: Emerging challenges toward 2050.
Emerging therapies including cagrilintide plus semaglutide, oral agents such as orforglipron and danuglipron, and the triagonist retatrutide
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.
- DANUGLIPRON
Danuglipron; Pf-06882961; PF-06882961
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.
- "Next-in-class" GLP-1R Danuglipron- and Lotiglipron-like Agonists: A Patent Review (2020-2024).
Patents containing danuglipron- and lotiglipron-like agonists from January 2021 to July 2024 were browsed in databases, such as Espacenet and Google Patents, using specified keywords.
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
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.
- ChEMBL activities for CHEMBL4518483
Standard result: F = 5.0 %
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 %
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
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.
- ChEMBL activities for CHEMBL4518483
Standard result: Cmax = 253.78 nM
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
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.
- ChEMBL activities for CHEMBL4518483
Standard result: T1/2 = 3.61 hr
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.
- ChEMBL activities for CHEMBL4518483
Standard result: F = 11.0 %
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
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.
- ChEMBL activities for CHEMBL4518483
Standard result: Tmax = 0.5 hr
- ChEMBL activities for CHEMBL4518483
Assay: Tmax in Wistar Han rat at 5 mg/kg, po measured upto 24 hrs by LC-MS/MS analysis Assay format: organism-based format Standard result: Tmax = 0.5 hr
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.
- ChEMBL activities for CHEMBL4518483
Assay: Oral bioavailability in ICR mouse at 5 mg/kg by LC-MS/MS analysis Assay format: organism-based format Standard result: F = 54.17 %
- ChEMBL activities for CHEMBL4518483
Standard result: F = 54.17 %
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.
- ChEMBL activities for CHEMBL4518483 ↗
chembl-activities · published August 26, 2026 · retrieved August 26, 2026
- DANUGLIPRON ↗
chembl-molecule · published August 26, 2026 · retrieved August 26, 2026
- 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
- 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
- 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
- IUPHAR ligand commentary ↗
iuphar-comments · published August 26, 2026 · retrieved August 26, 2026
- danuglipron ↗
iuphar-ligand · published August 26, 2026 · retrieved August 26, 2026
- 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
- 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
- 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
- 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
- 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
- "Next-in-class" GLP-1R Danuglipron- and Lotiglipron-like Agonists: A Patent Review (2020-2024). ↗
pubmed · published August 26, 2025 · retrieved September 9, 2026
- Novel GLP-1-based Medications for Type 2 Diabetes and Obesity. ↗
pubmed · published March 11, 2026 · retrieved August 25, 2026
- 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
- 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
- Childhood obesity and cardiac risk in youth: Emerging challenges toward 2050. ↗
pubmed · published June 1, 2026 · retrieved August 26, 2026
- 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
- Comparative Positioning of Orforglipron Among Selected GLP-1 Receptor Agonist Benchmarks: A Narrative Review. ↗
pubmed · published June 1, 2026 · retrieved August 26, 2026
- 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
- 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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