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proteasome inhibitor peptide

Carfilzomib

Published evidence · coverage incomplete
Anatomical contextAnatomy connections are not mapped yet.

No body region is highlighted until this profile has a supported anatomical connection. This does not mean the peptide has no biological effects.

Read published mechanism findings ↓

At a glance

What is it—and why does it matter?

Carfilzomib is categorized here as a proteasome inhibitor (PI), i.e., a drug class targeting the proteasome within the ubiquitin–proteasome system. Carfilzomib inhibits the proteasome’s β-5 subunit chymotrypsin-like activity. A fold-change (FC) > 100.0 indicates strong preference for inhibiting chymotrypsin-like activity compared with caspase-like activity in the human 20S proteasome. Microsomal extraction ratio (ERH) is a metabolic stability-related parameter; CHEMBL451887 showed ERH = 0.93 in human liver microsomes at 1 uM.

Sources for this introduction: [1] [2] [3] [4]

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

What is it?

A molecule, not a product name.

Identity

Carfilzomib is characterized here as a second-generation inhibitor of the proteasome, used to study proteasome blockade in cPAC cell lines.

Sources[3]pubmedProteasome Inhibitor-Induced Cytotoxic Mechanisms in Canine Pulmonary Adenocarcinoma Cell Lines.Guided by this result, we focused subsequent investigations on proteasome blockade and evaluated the antitumor activity and mechanisms of bortezomib together with a second-generation proteasome inhibitor, carfilzomib-alone and in combination with standard cytotoxics-in three cPAC cell lines (CLAC, HDC, and LuBi).
Source records
1
Independent studies
1

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

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Guided by this result, we focused subsequent investigations on proteasome blockade and evaluated the antitumor activity and mechanisms of bortezomib together with a second-generation proteasome inhibitor, carfilzomib-alone and in combination with standard cytotoxics-in three cPAC cell lines (CLAC, HDC, and LuBi).”

    Proteasome Inhibitor-Induced Cytotoxic Mechanisms in Canine Pulmonary Adenocarcinoma Cell Lines. · Abstract

    pubmed:41943258:8736e4619a50:8736e4619a50

Identity

Carfilzomib is categorized here as a proteasome inhibitor (PI), i.e., a drug class targeting the proteasome within the ubiquitin–proteasome system.

Sources[4]pubmedNanoparticle-Based delivery of proteasome inhibitors for glioblastoma Therapy: Strategies to overcome Blood-Brain barrier and therapeutic resistance.Thus, proteasome inhibitors (PIs) such bortezomib (BTZ), carfilzomib, ixazomib, and marizomib are promising treatments.
Source records
1
Independent studies
1

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

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Thus, proteasome inhibitors (PIs) such bortezomib (BTZ), carfilzomib, ixazomib, and marizomib are promising treatments.”

    Nanoparticle-Based delivery of proteasome inhibitors for glioblastoma Therapy: Strategies to overcome Blood-Brain barrier and therapeutic resistance. · Abstract

    pubmed:42142763:4eeed0acbf8b:4eeed0acbf8b

How does it work?

Target, response, and disposition.

Mechanism

Carfilzomib inhibits the proteasome’s β-5 subunit chymotrypsin-like activity.

Sources[2]iuphar-commentsIUPHAR ligand commentaryThis drug is a proteasome inhibitor, inhibiting the chymotrypsin-like activity of the β-5 subunit of the 20S proteasome
Source records
1
Independent studies
1

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 drug is a proteasome inhibitor, inhibiting the chymotrypsin-like activity of the β-5 subunit of the 20S proteasome”

    IUPHAR ligand commentary · Mechanism of action

    iuphar-comments:7420:f14e8f67e643:f14e8f67e643

Mechanism

In cell-line drug-interaction testing, carfilzomib combined with carboplatin produced synergistic interactions that were reproducible in HDC and LuBi lines.

Sources[3]pubmedProteasome Inhibitor-Induced Cytotoxic Mechanisms in Canine Pulmonary Adenocarcinoma Cell Lines.Drug-interaction analysis showed reproducible synergy between carfilzomib and carboplatin in HDC and LuBi, whereas combinations with vinorelbine were mainly additive or antagonistic effects.
Source records
1
Independent studies
1

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

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Drug-interaction analysis showed reproducible synergy between carfilzomib and carboplatin in HDC and LuBi, whereas combinations with vinorelbine were mainly additive or antagonistic effects.”

    Proteasome Inhibitor-Induced Cytotoxic Mechanisms in Canine Pulmonary Adenocarcinoma Cell Lines. · Abstract

    pubmed:41943258:8736e4619a50:8736e4619a50

Pharmacokinetics

Chemical stability in simulated intestinal fluid can indicate susceptibility to degradation; CHEMBL451887 showed < 5.0 % remaining after 15 mins at 4 uM.

Sources[1]chembl-activitiesChEMBL activities for CHEMBL451887Standard result: Stability < 5.0 %
Reported result
Stability < 5.0 %
Source records
1
Independent studies
1

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: Stability < 5.0 %”

    ChEMBL activities for CHEMBL451887 · Activity 2529307

    chembl-activities:chembl451887:b6f7430cd047:b6f7430cd047

Pharmacokinetics

Chemical stability testing in simulated gastric fluid assesses degradation under gastric-like conditions; CHEMBL451887 had 15.0 % remaining after 15 mins at 4 uM.

Sources[1]chembl-activitiesChEMBL activities for CHEMBL451887Standard result: Stability = 15.0 %
Reported result
Stability = 15.0 %
Source records
1
Independent studies
1

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: Stability = 15.0 %”

    ChEMBL activities for CHEMBL451887 · Activity 2529308

    chembl-activities:chembl451887:b6f7430cd047:b6f7430cd047

Pharmacokinetics

In vitro mouse liver microsome extraction ratio (ERH) reflects metabolic stability; CHEMBL451887 showed ERH = 0.98 at 1 uM.

Sources[1]chembl-activitiesChEMBL activities for CHEMBL451887Standard result: ERH = 0.98
Reported result
ERH = 0.98
Source records
1
Independent studies
1

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: ERH = 0.98”

    ChEMBL activities for CHEMBL451887 · Activity 2529306

    chembl-activities:chembl451887:b6f7430cd047:b6f7430cd047

Pharmacokinetics

Microsomal extraction ratio (ERH) is a metabolic stability-related parameter; CHEMBL451887 showed ERH = 0.93 in human liver microsomes at 1 uM.

Sources[1]chembl-activitiesChEMBL activities for CHEMBL451887Standard result: ERH = 0.93
Reported result
ERH = 0.93
Source records
1
Independent studies
1

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: ERH = 0.93”

    ChEMBL activities for CHEMBL451887 · Activity 2529305

    chembl-activities:chembl451887:b6f7430cd047:b6f7430cd047

What has been studied?

What the evidence says.

Comparative evidence

A fold-change (FC) > 100.0 indicates strong preference for inhibiting chymotrypsin-like activity compared with tyrosine-like activity in the human 20S proteasome.

Sources[1]chembl-activitiesChEMBL activities for CHEMBL451887Standard result: FC > 100.0
Reported result
FC > 100.0
Source records
1
Independent studies
1

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: FC > 100.0”

    ChEMBL activities for CHEMBL451887 · Activity 2529603

    chembl-activities:chembl451887:b6f7430cd047:b6f7430cd047

Comparative evidence

A fold-change (FC) > 100.0 indicates strong preference for inhibiting chymotrypsin-like activity compared with caspase-like activity in the human 20S proteasome.

Sources[1]chembl-activitiesChEMBL activities for CHEMBL451887Standard result: FC > 100.0
Reported result
FC > 100.0
Source records
1
Independent studies
1

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: FC > 100.0”

    ChEMBL activities for CHEMBL451887 · Activity 2529604

    chembl-activities:chembl451887:b6f7430cd047:b6f7430cd047

Study findings

An IC50 in the single-digit nM range indicates high potency; CHEMBL451887 showed IC50 = 5.7 nM against human 20S proteasome chymotrypsin-like activity by spectrofluorimetry.

Sources[1]chembl-activitiesChEMBL activities for CHEMBL451887Standard result: IC50 = 5.7 nM
Reported result
IC50 = 5.7 nM
Source records
1
Independent studies
1

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: IC50 = 5.7 nM”

    ChEMBL activities for CHEMBL451887 · Activity 2529315

    chembl-activities:chembl451887:b6f7430cd047:b6f7430cd047

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.

Research status + gaps

What still needs better answers?

  • No publishable claim yet for: administration, contraindication, interaction, regulatory, safety
  • 92 compiled claim(s) withheld by automated assurance: assurance_score_below_0.58 (57), assurance_score_below_0.72 (29), current_regulatory_source_required (15), extraction_ambiguity (62), extraction_confidence_not_high (4), high_risk_requires_regulatory_or_two_independent_sources (32), no_direct_support (82), proposal_not_staged (3)

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

References + discovery

Open the records yourself.

  1. ChEMBL activities for CHEMBL451887 ↗

    chembl-activities · published 2026-08-26 · retrieved 2026-08-26T20:21:51Z

  2. IUPHAR ligand commentary ↗

    iuphar-comments · published 2026-08-26 · retrieved 2026-08-26T08:42:26Z

  3. Proteasome Inhibitor-Induced Cytotoxic Mechanisms in Canine Pulmonary Adenocarcinoma Cell Lines. ↗

    pubmed · published 2026-09-01 · retrieved 2026-08-26T08:42:26Z

  4. Nanoparticle-Based delivery of proteasome inhibitors for glioblastoma Therapy: Strategies to overcome Blood-Brain barrier and therapeutic resistance. ↗

    pubmed · published 2026-09-01 · retrieved 2026-08-26T08:42:26Z

Publication history and provenance

Version 6 · Automated assessment · 2026-08-26T20:21:51Z

aa89d47bcd78d28b569a071b68d3d1cd3f632cc4999cf5f2df75d0c2365faa61