Preliminary clinical success of Pfizer's oral GLP-1 agonist

On September 21, 2022, Pfizer presented the latest clinical data on oral GLP-1 agonists at the EASD2022 meeting.The development barrier of GLP-1R small molecule agonists is high. Pfizer has established a high-sensitivity detection method and screened 2.8 million compounds, and finally obtained two PCCs, Danuglipron and PF-07081532.

Pfizer announced the Phase II clinical data of Danuglipron and the Phase 1b clinical data of PF-07081532.

Danuglipron treatment for 16 weeks significantly reduced basal blood glucose HbA1c, postprandial blood glucose FPG, and body weight.

Another Phase 2a clinical study of Danuglipron, using a 200mg BID dose, reduced HbA1c by 1.57% at 12 weeks, compared with a 1.25% reduction in the placebo group, and reduced body weight by 5.4 kg and 5.0 kg compared with the placebo group.

The Phase 1b clinical trial of PF-07081532 has designed 6 dose groups, with a half-life of more than 20 hours, which can be taken orally once a day.

GLP-1 is the most important progress in the field of hypoglycemic drugs in recent years. Eli Lilly's GLP-1R/GIPR dual-target agonist has been approved for marketing, and Novo Nordisk has developed an oral version of semaglutide. Today, Pfizer's small-molecule GLP-1R agonists also show strong therapeutic potential. Although the peptide can be developed as an oral version, its bioavailability is too low and the cost is much higher than the injection version. If the small molecule oral GLP-1R is successful, it will have broad market prospects.