Drug intelligence / Profile preview

leucovorin + fluorouracil + irinotecan + vemurafenib + cetuximab

Development stage
Preclinical
Lead developer
Pfizer
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Intravenous, Oral
01

Overview

This is a combination chemotherapy regimen consisting of leucovorin, fluorouracil, irinotecan, vemurafenib, and cetuximab. The combination targets multiple pathways in cancer cells: - Leucovorin enhances the cytotoxic effects of fluorouracil by stabilizing the binding of fluorouracil metabolite (FdUMP) to thymidylate synthase - Fluorouracil is an antimetabolite that disrupts DNA synthesis - Irinotecan is a topoisomerase I inhibitor that prevents DNA unwinding and replication - Vemurafenib is a BRAF inhibitor targeting the BRAF V600E mutation - Cetuximab is a monoclonal antibody that targets the epidermal growth factor receptor (EGFR) This combination is likely used for metastatic colorectal cancer with BRAF V600E mutations, combining traditional chemotherapy with targeted therapy approaches.

02

Targets

TOP1 (DNA Topoisomerase I)BRAF V600ETS (Thymidylate synthase)EGFR (Epidermal growth factor receptor)

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