Drug intelligence / Profile preview

RAD001 + cisplatin + fluorouracil + leucovorin

Development stage
Unknown
Lead developer
Novartis
Modality
Small Molecules
Administration
Oral (for Everolimus), Intravenous (for Cisplatin, Fluorouracil, Leucovorin)
01

Overview

This is a **combination regimen** of four drugs: everolimus (RAD001), cisplatin, fluorouracil, and leucovorin. - **Everolimus (RAD001)** is an orally bioavailable inhibitor of mammalian target of rapamycin (mTOR), a key component of the PI3K/Akt pathway in human cancers. It forms a complex with FKBP12, binding to mTOR and inhibiting downstream effectors S6K1 and 4EBP1, thereby blocking cell cycle progression and protein synthesis in tumor cells. Everolimus is approved for several cancers and exhibits antineoplastic and immunosuppressive activity[1][2][3][5][9]. - **Cisplatin** is a platinum-based chemotherapy drug that forms DNA crosslinks and induces apoptosis in rapidly dividing tumor cells. - **Fluorouracil** (5-FU) is a pyrimidine analog that inhibits thymidylate synthase, disrupting DNA and RNA synthesis. - **Leucovorin** enhances the cytotoxicity of fluorouracil by stabilizing its binding to thymidylate synthase. This combination targets multiple pathways involved in cancer cell proliferation and survival, and it is typically investigated in clinical trials for advanced solid tumors, including gastrointestinal and biliary tract cancers, though the specific quadruple combination is experimental.

Brand names
Afinitor
Other names
everolimus + cisplatin + fluorouracil + leucovorin
02

Targets

DNATS (Thymidylate synthase)mTOR (Mammalian target of rapamycin kinase)

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