Drug intelligence / Profile preview

cyclophosphamide + doxorubicin + epirubicin + fluorouracil + methotrexate

Development stage
Unknown
Lead developer
Pfizer
Modality
Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Intravenous (iv)
01

Overview

This is a combination chemotherapy regimen consisting of five cytotoxic agents: cyclophosphamide, doxorubicin, epirubicin, fluorouracil (5-FU), and methotrexate. Each drug has a distinct mechanism of action targeting rapidly dividing cancer cells: - Cyclophosphamide is an alkylating agent that cross-links DNA strands, inhibiting DNA replication and transcription. - Doxorubicin and epirubicin are anthracycline antibiotics that intercalate into DNA and inhibit topoisomerase II, leading to DNA breaks and apoptosis. - Fluorouracil is an antimetabolite that inhibits thymidylate synthase, disrupting DNA synthesis. - Methotrexate is a folic acid antagonist that inhibits dihydrofolate reductase, blocking the synthesis of nucleotides required for DNA replication. While combinations such as FAC (fluorouracil, doxorubicin, cyclophosphamide) or FEC (fluorouracil, epirubicin, cyclophosphamide) are established in breast cancer treatment[7], there is no widely recognized clinical regimen combining all five agents together. Each component targets different aspects of cell division or metabolism to maximize antitumor efficacy. This combination would be expected to have significant toxicity due to overlapping myelosuppression and other adverse effects.

02

Targets

TS (Thymidylate synthase)DHFR (Dihydrofolate reductase)TOP2A (DNA topoisomerase II)DNA

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