Pfizer's PF-06882961 (Danuglipron) Granted IND Approval in China for Type 2 Diabetes Treatment

On March 17, the CDE website showed that Pfizer’s PF-06882961 tablets (danuglipron) had received default approval for clinical trial application, with plans to conduct clinical studies for the treatment of type 2 diabetes.

Danuglipron (code name: PF-06882961 tablets) is an oral small-molecule GLP-1 receptor agonist developed by Pfizer. Distinct from injectable and oral peptide-based GLP-1 RAs, this small-molecule drug offers a differentiated innovative therapy for patients with diabetes and obesity.

The potential advantages of danuglipron include: ① effective control of blood glucose and body weight; ② tolerability and safety profiles similar to those of peptide-based GLP-1 receptor agonists (GLP-1 RAs), with the added convenience of an oral formulation; ③ favorable bioavailability; ④ unlike oral macromolecular GLP-1 RAs, it is not subject to food or dose restrictions; and ⑤ suitability for development as monotherapy or in combination therapy.

Pfizer announced at its virtual Investor Day event held in August 2020

Phase I Clinical Study Data of Danuglipron. Patients with type 2 diabetes were randomly assigned to receive placebo or danuglipron at doses of 15 mg, 70 mg, or 120 mg twice daily. After 28 days of treatment, patients exhibited significant reductions in fasting blood glucose levels, glycated hemoglobin (HbA1c) levels, and body weight. Notably, in the danuglipron 120 mg dose group, fasting blood glucose decreased by up to 90 mg/dL, HbA1c decreased by 1.2%, and body weight was reduced by 8 kg.

Pfizer has already initiated Phase II clinical trials to evaluate the efficacy of danuglipron in treating patients with diabetes, with proof-of-concept results expected in the third quarter. The company will also launch a Phase IIb clinical trial to assess the efficacy of this oral small-molecule GLP-1 receptor agonist in treating patients with non-alcoholic steatohepatitis (NASH).

Previously, Novo Nordisk’s Rybelsus (oral semaglutide, once daily) has been approved by the FDA for marketing and is currently the only marketed oral formulation of a GLP-1 receptor agonist.