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

Aditi R. Saxena
Pfizer Inc.
January 1, 2021
Nat Med
https://pubmed.ncbi.nlm.nih.gov/34127852

This article is currently being updated. View its version on PubMed.

https://pubmed.ncbi.nlm.nih.gov/34127852

Research summary

This phase 1 clinical trial evaluated danuglipron, a small-molecule oral GLP-1 receptor agonist, for safety, pharmacokinetics, and preliminary efficacy in adults with type 2 diabetes. Danuglipron produced dose-dependent improvements in fasting plasma glucose, postprandial glucose, and body weight. Preclinical validation was supported by studies using a humanized GLP1R mouse model developed by genOway.

Key outcome of the study

Danuglipron demonstrated promising glycemic control and weight reduction effects, validating the approach of targeting human GLP-1R with an oral small-molecule agonist.

Mouse model

Humanized GLP1R Knockin mouse model developed by genOway, with the human GLP1R extracellular domain replacing the mouse counterpart for preclinical drug evaluation.

TARGET:
GLP1R
Glucagon-like peptide-1 receptor

Keywords

Type 2 diabetes, Oral GLP-1 therapy, Small-molecule GLP-1R agonist, Glycemic control

Technical specifications

Humanized Knockin model, GLP1R extracellular domain replacement, Preclinical pharmacology

Related products

Catalogue product

genO-hGLP‑1R

Preclinical genO‑hGLP-1R model for assessment of agents targeting human GLP-1R

Customized product

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