Drug intelligence / Profile preview

5-fluorouracil + cyclophosphamide + cytosine arabinoside + doxorubicin + methotrexate + vincristine

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

Overview

This is a combination chemotherapy regimen consisting of six cytotoxic agents: 5-fluorouracil, cyclophosphamide, cytosine arabinoside (also known as cytarabine), doxorubicin, methotrexate, and vincristine. Each drug has a distinct mechanism of action targeting different phases or processes in the cell cycle to maximize antitumor activity and minimize resistance. This intensive multi-agent protocol is designed to expose rapidly proliferating tumor cells to synergistic effects throughout the cell cycle. The regimen has been used primarily for advanced stages of diffuse high-grade non-Hodgkin's lymphoma and has also been studied in metastatic breast cancer settings[2][1][3]. - 5-fluorouracil inhibits thymidylate synthase, disrupting DNA synthesis. - Cyclophosphamide is an alkylating agent that crosslinks DNA. - Cytosine arabinoside (cytarabine) inhibits DNA polymerase. - Doxorubicin intercalates into DNA and inhibits topoisomerase II. - Methotrexate inhibits dihydrofolate reductase, blocking folate metabolism required for nucleotide synthesis. - Vincristine binds tubulin and disrupts microtubule formation during mitosis.

Other names
F-MACHOP
02

Targets

TS (Thymidylate synthase)DNATUBB (Tubulin (alpha and beta subunits))DNA polymerase familyTOP2A (DNA topoisomerase II)DHFR (Dihydrofolate reductase)

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