fulzerasib + dextromethorphan

IBI351 + dextromethorphan is a drug combination primarily utilized in clinical pharmacology to evaluate the drug-drug interaction (DDI) profile of fulzerasib (IBI351). Fulzerasib is a potent, orally bioavailable, covalent small molecule inhibitor that specifically targets the KRAS G12C mutation. It works by locking the KRAS protein in its inactive GDP-bound state, thereby inhibiting downstream oncogenic signaling pathways such as MAPK/ERK, which are critical for the proliferation of KRAS G12C-mutant solid tumors like non-small cell lung cancer (NSCLC) and colorectal cancer. Dextromethorphan, a common antitussive, serves as a sensitive probe substrate for the Cytochrome P450 2D6 (CYP2D6) enzyme. In clinical trials, this combination is administered to assess whether fulzerasib acts as an inhibitor or inducer of CYP2D6, providing essential safety data for patients who may require concomitant medications metabolized by this pathway.

Other names

IBI351 + dextromethorphanfulzerasib + dextromethorphan hydrobromide