Pyrrolidine, also known as tetrahydropyrrole, is a saturated five-membered heterocyclic ring, which is miscible with water. Pyrrolidine exists in many alkaloids and drug molecules, such as kappa opioids, antagonists of dopamine D4 receptors, and HIV reverse transcriptase inhibitors.
Jan. 10, 2024, EC approves KRAZATI (adagrasib) as a targeted treatment option for patients with advanced non-small cell lung cancer (NSCLC) with a KRAS G12C mutation.
Adagrasib is an orally available, potent, irreversible, small molecule inhibitor of KRAS G12C mutant isoform for the treatment of solid tumours harbouring KRAS G12C oncogenic driver mutation. Adagrasib covalently binds to the mutant cysteine in KRAS G12C and locks the mutant KRAS protein in its inactive state, thereby preventing downstream signalling without affecting wild-type KRAS protein.