This was a loaded month for pioneering drug discovery programs! Among the highlights are a reversible-covalent inhibitor from Novartis, the hotly followed SHP2 inhibitor from Novartis, several innovative compounds from Pfizer including an oral GLP-1R agonist with a cryo-EM structure, a liver-targeted ACC inhibitor, and an oral KHK inhibitor. Remarkably, half of the molecules are negatively charged or pro-drugs of anions, and several have oral bioavailability beyond what a chemist 20 years ago would have thought probable. Most of these don’t look like they would be low-clearance, high bioavailability drugs, but they are! Detailed comments and links below.
September 2020
- FGF401 (roblitinib)
- TNO155
- BMS-986143
- AZD9833
- AL-611
- PF-06882961
- PF-05221304
- PF-06835919
- "compound 9"
- GLPG1205
- OP-5244
- SCO-267
- "compound 23"
- TAS-120 (futibatinib)