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6-mercaptopurine + methotrexate + vincristine + dexamethasone
- Development stage
- Unknown
- Lead developer
- Pfizer
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
- Administration
- Oral, Intravenous, Intrathecal
01
Overview
This is a multi-agent chemotherapy regimen composed of four drugs—6-mercaptopurine, methotrexate, vincristine, and dexamethasone—commonly used in the treatment of acute lymphoblastic leukemia (ALL), particularly in pediatric and adolescent patients. Each component has a distinct mechanism of action: - 6-mercaptopurine is an antimetabolite that inhibits purine synthesis, interfering with DNA and RNA production. - Methotrexate is an antimetabolite that inhibits dihydrofolate reductase, blocking folic acid metabolism required for DNA synthesis. - Vincristine is a vinca alkaloid that disrupts microtubule formation during cell division. - Dexamethasone is a synthetic glucocorticoid corticosteroid with anti-inflammatory and cytotoxic effects on lymphoid cells. This combination targets leukemic cells at multiple points in their growth cycle to maximize cytotoxicity and reduce the risk of resistance. It forms part of various phases (induction, consolidation/maintenance) in ALL protocols[2][5][9].
- Other names
- VCR + 6-MP + MTX + DEXVincristine, Mercaptopurine, Methotrexate, and Dexamethasone combination6-MP/MTX with vincristine and dexamethasone therapy
02
Targets
GR (Glucocorticoid receptor)HPRT1 (Hypoxanthine-guanine phosphoribosyltransferase)TUBB (Tubulin (alpha and beta subunits))DHFR (Dihydrofolate reductase)
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