Pfizer's Class 1 New Drug PF-07934040 Granted Clinical Trial Approval in China for KRAS-Mutated Advanced Solid Tumors

Intelligent Finance APP learned on February 17 that the official website of the Center for Drug Evaluation (CDE) under the China National Medical Products Administration announced that Pfizer's (PFE.US) new Class 1 drug, PF-07934040 tablets, had received implied permission for clinical trials. This drug is intended to be developed for treating advanced solid tumors carrying KRAS mutations. According to publicly available information from Pfizer, this is an investigational pan-KRAS inhibitor currently undergoing Phase 1 clinical trials internationally. Based on publicly available information, this is the first time the product has received IND approval in China. The approval of PF-07934040 for clinical trials in China means that the product is about to commence clinical research in China.

Source of Screenshot: CDE Official Website

According to the introduction on Pfizer's official website, PF-07934040 is a pan-KRAS "ON/OFF" inhibitor with activity against wild-type (wt) KRAS and major mutant subtypes, but no activity against NRAS or HRAS. PF-07934040 shows binding to both the OFF (GDP-bound) and ON (GTP-loaded) states of KRAS wt, with very low binding affinity to mutants, and its selectivity for KRAS is 5000 times higher than that for HRAS/NRAS.

Studies show that PF-07934040 blocks the binding of RAF-RBD to GTPgS-loaded KRAS mutants, suggesting its mechanism of action may include binding to the KRAS on-state and inhibiting RAF binding, modulating downstream signaling.

Schematic Diagram of PF-07934040 Mechanism of Action (Screenshot Source: Pfizer Official Website)