Drug intelligence / Profile preview

methotrexate + cyclophosphamide + vincristine + doxorubicin + bleomycin

Development stage
Unknown
Lead developer
Pfizer
Modality
Small Molecules
Administration
Intravenous, Oral
01

Overview

This is an unbranded multi-agent chemotherapy regimen combining methotrexate, cyclophosphamide, vincristine, doxorubicin and bleomycin, all of which are classic cytotoxic agents used in oncology. Methotrexate is an antifolate antimetabolite that inhibits dihydrofolate reductase and thymidylate synthesis, blocking DNA synthesis in rapidly dividing cells. Cyclophosphamide is an alkylating prodrug that forms DNA crosslinks after hepatic activation, leading to apoptosis. Vincristine is a vinca alkaloid that binds tubulin and inhibits microtubule polymerization, arresting cells in metaphase. Doxorubicin is an anthracycline that intercalates into DNA, inhibits topoisomerase II and generates free radicals, causing DNA strand breaks. Bleomycin is a glycopeptide antibiotic that chelates metal ions and induces DNA strand breaks through free radical formation, with particular toxicity for lung and skin. Together, these agents provide broad cell-cycle–nonspecific and cell-cycle–specific antineoplastic activity and would be expected to be used in investigational or institution-specific protocols rather than as a standard named regimen.

02

Targets

TOP2A (DNA topoisomerase II)TUBB (Tubulin (alpha and beta subunits))DHFR (Dihydrofolate reductase)DNA

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