Drug intelligence / Profile preview

GLP1R0017

Development stage
Unknown
Lead developer
AstraZeneca
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics
01

Overview

GLP1R0017 (also referred to as Glp1R0017) is a monoclonal antagonistic antibody targeting the glucagon-like peptide-1 receptor (GLP1R). Developed through a collaboration between the University of Cambridge, MedImmune, and AstraZeneca, the antibody was isolated from a naïve phage display library as a single-chain variable fragment (ScFv) and subsequently converted into a human IgG1 framework. GLP1R0017 exhibits highly specific, competitive antagonism against human, mouse, rat, dog, and cynomolgus monkey GLP1R, with no cross-reactivity toward other class B GPCRs such as GIPR, GLP-2R, or the glucagon receptor. In vitro, it blocks GLP-1-stimulated cAMP signaling and insulin secretion in pancreatic beta cells. In vivo, GLP1R0017 effectively reverses the glucose-lowering effects of GLP-1 mimetics like liraglutide, making it a valuable research tool for investigating the physiological roles of GLP1R signaling in extrapancreatic tissues.

02

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