Drug intelligence / Profile preview

5-fluorouracil + leucovorin + cetuximab + vemurafenib

Development stage
Unknown
Lead developer
Roche
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Intravenous (5-fluorouracil, Leucovorin, Cetuximab), Oral (vemurafenib)
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Overview

This is a **combination therapy** consisting of four drugs: - **5-fluorouracil**: an antimetabolite chemotherapeutic agent that interferes with RNA synthesis and, to a lesser degree, DNA synthesis, resulting in cytotoxicity and cell death, especially effective in gastrointestinal cancers[1][7]. - **Leucovorin (folinic acid)**: a vitamin supplement used to increase the efficacy of 5-fluorouracil by stabilizing its binding to thymidylate synthase, enhancing cytotoxicity and modulating folate metabolism (mechanistic inference based on clinical usage). - **Cetuximab**: a chimeric monoclonal antibody against epidermal growth factor receptor (EGFR), inhibiting downstream signaling pathways critical for cancer cell survival and proliferation (mechanistic inference based on established usage). - **Vemurafenib**: a small molecule BRAF kinase inhibitor that selectively inhibits the activity of mutated BRAF V600E, blocking MAPK/ERK pathway signaling and suppressing cancer cell growth[2][4][6]. This specific combination is designed primarily for colorectal cancers with BRAF V600E mutation and EGFR expression, aiming for multi-pathway targeting—antimetabolic, signal transduction, and receptor inhibition.

02

Targets

BRAF V600ETS (Thymidylate synthase)EGFR (Epidermal growth factor receptor)

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