Drug intelligence / Profile preview

fulzerasib + cetuximab beta

Development stage
Unknown
Lead developer
Innovent Biologics
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Intravenous, Oral
01

Overview

fulzerasib + Enlituo is a combination therapy consisting of fulzerasib (Dupert), an orally active, selective, covalent, and irreversible small-molecule inhibitor of the KRAS G12C mutant protein, and Enlituo (cetuximab beta), a recombinant epidermal growth factor receptor (EGFR) monoclonal antibody. Developed through a collaboration involving GenFleet Therapeutics, Mabpharm, Innovent Biologics, and Simcere Zaiming, this combination is designed to overcome resistance to KRAS G12C inhibition. KRAS inhibition often triggers feedback reactivation of the EGFR pathway, and combining it with an anti-EGFR antibody like cetuximab beta synergistically blocks downstream MAPK signaling, enhancing antitumor efficacy. The combination is currently being evaluated in Phase II clinical trials for the treatment of KRAS G12C-mutated metastatic colorectal cancer (mCRC) and untreated advanced non-small cell lung cancer (NSCLC).

Brand names
Dupert
Other names
cetuximab beta + fulzerasibCMAB009 + GFH925CMAB009 + IBI351fulzerasib + cetuximab betafulzerasib + EnlituoGFH925 + cetuximab betaGFH925 + EnlituoIBI351 + cetuximab betaIBI351 + CMAB009IBI351 + Enlituo
02

Targets

EGFR (Epidermal growth factor receptor)FcγR (Low affinity immunoglobulin gamma Fc region receptor II-c)KRASG12C (Kirsten rat sarcoma viral oncogene homolog G12C)

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