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Oral Small Molecule GLP-1R agonist obtained clinical trial approval

------ powerful glucose-lowering and weight loss in the phase I trial

Oral Small Molecule GLP-1R Agonist
Global pharmaceutical companies sales in 2020 shows that the clinical benefits of GLP-1 drugs in the treatment of type 2 diabetes led to rapid increase of sales volume. The expansion of new indications for other metabolic diseases will open a broader market space for GLP-1 drugs.

First of all, GLP-1 drugs have remarkable effects in a variety of metabolic diseases and can gain comprehensive clinical benefits as “Drugs for effective treatment of metabolism”. Besides dominating the field of hypoglycemic drugs, it is also actively exploring the territory of obesity and NASH (nonalcoholic steatohepatitis), and the potential of Magical Medicine" is fully realized.

Secondly, replacing macromolecules with small molecules is a topic never out of date in the pharmaceutical field. One obvious advantage of small molecule agonists is oral administration, which increase patient compliance. In addition, small molecule drugs are more economical than protein drugs.

Therefore, GLP-1 + small molecule agonists are more successful than many polypeptide GLP-1 analogues, for it’s better safety, effective, and economy.

Pfizer Oral Small Molecule GLP-1R Agonist
At the annual meeting of the American Diabetes Association in June, 2020, Pfizer released Phase 1 clinical study data about oral small molecule Glucagon like peptide 1 receptor (GLP-1R) agonist PF-06882961 taken by patients with T2DM (type 2 diabetes mellitus). The result showed that FPG, MDG and body weight of T2DM adults patients decreased significantly on Day 28. The state of all the patients took GLP-1 agonists were improved. Those who took the 120mg dose achieved the highest improvement results: the average weight loss was about 18 pounds, the FPG and MDG reduction was 89.7mg and 105.9mg separately.

In March 2021, the official website of CDE showed that Pfizer's oral clinical application of small molecule GLP-1 agonist PF-06882961 (Danuglipron) received acquiescence, and developing clinical research on type 2 diabetes mellitus was in plan. The small molecule drug is different from the GLP-1RA for injection and oral use. It can provide a differentiated innovative therapy for diabetics and obesity patients.

The potential advantages of oral GLP-1 small molecule agonist Danuglipron include:
① effective control of blood glucose and body weight;
② The tolerance & safety are similar to peptide GLP-1RA, and the oral dosage form is convenient;
③ Good bioavailability;
④ Different from oral macromolecule GLP-1RA, it is not limited by food or dose;
⑤ It can be developed for single drug or combined drug use.

Drug name: Danuglipron
Developer: Pfizer
CAS : 2230198-02-2
Indications: glucose-lowering, weight loss
Key intermediates and building blocks of Danuglipron.


↑Accela is capable to produce KG to hundreds KGS of the key intermediate.
↓Accela can also provide other more building blocks.


Reference:医药魔方/Study: Pfizer's Experimental Diabetes Drug Robustly Reduces Weight and Glucose/Frost & Sullivan/点石资本