Drug intelligence / Profile preview

tretinoin + 6-mercaptopurine + methotrexate

Development stage
Phase 3
Modality
Small Molecules
Administration
Oral, Intramuscular (for Methotrexate), Subcutaneous (for Methotrexate)
01

Overview

**tretinoin + 6-mercaptopurine + methotrexate** is a combination chemotherapy regimen primarily used as maintenance or induction therapy in acute promyelocytic leukemia (APL), especially in pediatric and adult populations. Tretinoin (all-trans retinoic acid, ATRA) induces cytodifferentiation of leukemic promyelocytes via agonism of retinoic acid receptor alpha (RARα), promoting blast maturation. 6-Mercaptopurine and methotrexate are antimetabolite chemotherapeutics: 6-mercaptopurine inhibits de novo purine synthesis by incorporation into nucleic acids, while methotrexate inhibits dihydrofolate reductase, impairing nucleotide synthesis and cell proliferation. This regimen is typically used after consolidation therapy in APL, sometimes for relapsed cases, to reduce residual disease and maintain remission[1][4][9]. Development and usage have been described in pediatric oncology and adult hematology[4][9].

Other names
tretinoin + 6-MP + methotrexatetretinoin + mercaptopurine + methotrexate
02

Targets

DHFR (Dihydrofolate reductase)PPAT (Amidophosphoribosyltransferase)HPRT1 (Hypoxanthine-guanine phosphoribosyltransferase)RARA (Retinoic acid receptor alpha)XO (Xanthine Oxidoreductase)IMPDH (Inosine-5'-monophosphate dehydrogenase 1)

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