molecules of the month


oral GLP-1-RA full agonist

obesity Ph. IIb, 2.5-120 mg QD, T2D Ph. II, 40-200 mg

from sensitized cell HTS of 2.8M cmpds + opt.

Press release, June 26, 2023

Pfizer, Cambridge, MA

danuglipron, GLP-1R, oral GLP-1-RA full agonist, obesity Ph. IIb, 2.5-120 mg QD, T2D, Ph. II, 40-200 mg, from sensitized cell HTS of 2.8M cmpds + opt., Press release, June 26, 2023, PFIZER, CAMBRIDGE, MA
13 mins read

An oral GLP-1R agonist competing with peptide injectables for diabetes and obesity. Peptidic GLP-1R agonists have received significant media coverage over the past year. Shortages of the semaglutide-based injectable diabetes medication Ozempic, which accounts for 40% of GLP-1R agonist US market share, have even emerged, driven by overwhelming demand for the weight loss formulation Wegovy, both for treatment of obesity and for short-term weight loss popularized by celebrities on social media. Though they have been challenging to discover, small molecule GLP-1R agonists like danuglipron and orforglipron could offer more convenient and lower-cost alternatives to peptides. Figure 1. GLP-1 agonists. The first small molecule GLP-1R agonist to generate Ph. II data, with impressive results  A phase II trial ofdanuglipron, Pfizer's first…

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