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fulzerasib + itraconazole
- Development stage
- Unknown
- Lead developer
- Innovent Biologics
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Fulzerasib (IBI351) is a potent, orally bioavailable, covalent small-molecule inhibitor of the KRAS G12C mutation, developed by Innovent Biologics in collaboration with GenFleet Therapeutics. It is designed to treat advanced solid tumors, particularly non-small cell lung cancer (NSCLC) and colorectal cancer, by locking the KRAS protein in its inactive GDP-bound state. The combination with itraconazole, a strong CYP3A4 inhibitor and triazole antifungal, is primarily utilized in clinical pharmacology studies to evaluate drug-drug interactions (DDI). Because fulzerasib is a substrate for the cytochrome P450 3A4 (CYP3A4) enzyme, co-administration with itraconazole is used to characterize the impact of metabolic inhibition on the drug's systemic exposure and pharmacokinetics, which is essential for establishing safe dosing guidelines in patients receiving concomitant medications.
- Brand names
- DufulinSporanox
- Other names
- fulzerasibitraconazole
02
Targets
CYP51A1 (Sterol 14α-demethylase)CYP3A4 (Cytochrome P450 3A4)ABCB1 (P-glycoprotein)ABCG2 (Breast cancer resistance protein)
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