Drug intelligence / Profile preview

fulzerasib + cetuximab beta + fluorouracil + leucovorin + irinotecan

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

Overview

This combination regimen consists of fulzerasib (a covalent KRAS G12C inhibitor), cetuximab beta (an anti-EGFR monoclonal antibody), and the FOLFIRI chemotherapy regimen (fluorouracil, leucovorin, and irinotecan). It is being evaluated in clinical trials, such as the Phase II CRUCIAL study, for the first-line treatment of patients with KRAS G12C-mutated metastatic colorectal cancer (mCRC). By combining a direct KRAS G12C inhibitor with an EGFR inhibitor and standard chemotherapy, the regimen aims to overcome EGFR-mediated feedback reactivation and adaptive resistance, which typically limit the efficacy of KRAS G12C inhibitor monotherapy in colorectal cancer.

Brand names
Dupert
Other names
CRUCIAL regimenfulzerasib + cetuximab beta + FOLFIRIfulzerasib + Enlituo + FOLFIRIfulzerasib + Enlituo + fluorouracil + leucovorin + irinotecanGFH925 + CMAB009 + FOLFIRIIBI351 + cetuximab beta + FOLFIRIIBI351 + Enlituo + FOLFIRI
02

Targets

DNATOP1 (DNA Topoisomerase I)EGFR (Epidermal growth factor receptor)KRASG12C (Kirsten rat sarcoma viral oncogene homolog G12C)TS (Thymidylate synthase)

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