PNB-028

PNB-028 is an investigational small molecule drug developed by PNB Vesper Life Sciences that acts as a selective and irreversible antagonist of the cholecystokinin A (CCK-A) receptor, also known as the CCK1 receptor. Chemically, it is a fluorinated 5-arylated 5-hydroxypyrrolone derivative. PNB-028 is primarily being developed for the treatment of colon cancer and pancreatic cancer. It exhibits high potency with a binding affinity of 12 nM and demonstrates 60-fold selectivity for CCK-A over the CCK-B receptor. Preclinical studies have shown that the compound can completely inhibit tumor growth in chemo-resistant MAC16 colon cancer and MIAPACA pancreatic cancer xenograft models. The drug possesses favorable pharmacokinetic properties, including nearly 100% oral bioavailability, and has progressed to Phase 1/2 clinical trials in India following approval by the DCGI in 2019.

Other names

N-isobutyl-5-hydroxy-5-aryl-pyrrol-2-oneN-isobutyl5-hydroxy-5-aryl-pyrrol-2-oneN-isobutyl 5-hydroxy-5-aryl-pyrrol-2-one