Drug intelligence / Profile preview

cyclophosphamide + doxorubicin + fluorouracil + leucovorin + methotrexate + vincristine

Development stage
Unknown
Lead developer
Takeda
Modality
Small Molecules
Administration
Intravenous
01

Overview

This is a multi-agent chemotherapy regimen composed of six drugs: cyclophosphamide, doxorubicin, fluorouracil, leucovorin, methotrexate, and vincristine. Each component has a distinct mechanism of action targeting rapidly dividing cancer cells: - Cyclophosphamide is an alkylating agent that cross-links DNA strands to prevent cell division. - Doxorubicin (also known as Adriamycin) is an anthracycline antibiotic that intercalates into DNA and inhibits topoisomerase II, leading to DNA damage. - Fluorouracil (5-FU) is a pyrimidine analog that inhibits thymidylate synthase and disrupts RNA synthesis. - Leucovorin enhances the binding of 5-FU to thymidylate synthase and also serves as a "rescue" agent for normal cells during high-dose methotrexate therapy. - Methotrexate is an antimetabolite that inhibits dihydrofolate reductase, blocking folic acid metabolism required for DNA synthesis. - Vincristine (Oncovin) binds tubulin and prevents microtubule formation during mitosis. This combination targets multiple pathways in cancer cell proliferation. Such regimens are primarily used in the treatment of advanced or metastatic breast cancer[1][3]. The inclusion of all six agents in one protocol represents an aggressive approach designed to maximize cytotoxic effects by attacking tumor cells at different points in the cell cycle.

02

Targets

TS (Thymidylate synthase)DHFR (Dihydrofolate reductase)TOP2A (DNA topoisomerase II)DNATUBB (Tubulin (alpha and beta subunits))

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