Drug intelligence / Profile preview

cyclophosphamide + epirubicin + fluorouracil + methotrexate + paclitaxel

Development stage
Preclinical
Lead developer
Takeda
Modality
Classical Binding Small Molecules → Small Molecules
Administration
Intravenous, Oral
01

Overview

This is a multi-agent chemotherapy combination consisting of five cytotoxic drugs: cyclophosphamide, epirubicin, fluorouracil, methotrexate, and paclitaxel. Each component has a distinct mechanism of action targeting rapidly dividing cancer cells: - Cyclophosphamide is an alkylating agent that crosslinks DNA strands, inhibiting DNA replication and leading to cell death. - Epirubicin is an anthracycline antibiotic that intercalates into DNA and inhibits topoisomerase II, preventing DNA repair and synthesis. - Fluorouracil (5-FU) is an antimetabolite that inhibits thymidylate synthase, disrupting DNA synthesis. - Methotrexate is also an antimetabolite; it inhibits dihydrofolate reductase (DHFR), blocking folic acid metabolism required for nucleotide synthesis. - Paclitaxel stabilizes microtubules and prevents their depolymerization during cell division. This combination would be expected to have broad-spectrum anti-tumor activity due to the complementary mechanisms of its components. While combinations such as CMF (cyclophosphamide, methotrexate, fluorouracil), CEF/ECF (cyclophosphamide/epirubicin/fluorouracil), or regimens including paclitaxel are established in breast cancer therapy[1][2][8], there are no standard regimens or clinical trial data supporting the use of all five agents together in a single protocol. The regimen would likely be highly myelosuppressive with significant toxicity risk.

02

Targets

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

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