Drug intelligence / Profile preview

fluorouracil + lenalidomide + leucovorin + oxaliplatin

Development stage
Unknown
Lead developer
Roche
Modality
Small Molecules
Administration
Intravenous, Oral
01

Overview

This is a combination regimen consisting of four drugs: - **Fluorouracil (5-FU):** An antimetabolite chemotherapy that inhibits thymidylate synthase, disrupting DNA synthesis and leading to cell death. - **Lenalidomide:** An immunomodulatory agent with antiangiogenic and direct antineoplastic effects. It modulates the immune system, inhibits cytokine release, and has antiproliferative activity. - **Leucovorin (Folinic acid):** A reduced form of folic acid used to enhance the efficacy of fluorouracil by stabilizing its binding to thymidylate synthase. - **Oxaliplatin:** A platinum-based chemotherapeutic that forms DNA crosslinks, inhibiting DNA replication and transcription. This specific four-drug combination is not a standard named regimen but has been studied in early-phase clinical trials for advanced cancers, particularly colorectal cancer. The rationale is based on the established FOLFOX backbone (fluorouracil + leucovorin + oxaliplatin) with the addition of lenalidomide for potential synergistic anticancer effects[1]. The mechanism involves both direct cytotoxicity against tumor cells and modulation of the tumor microenvironment via immunomodulation.

02

Targets

CRBN (Cereblon)DNATS (Thymidylate synthase)

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