Drug intelligence / Profile preview

methotrexate + 6-mercaptopurine

Development stage
Unknown
Modality
Small Molecules
Administration
Oral
01

Overview

Methotrexate + 6-mercaptopurine is a combination of two antimetabolite chemotherapeutic agents commonly used in the maintenance therapy of acute lymphoblastic leukemia (ALL), particularly in pediatric patients. Methotrexate inhibits dihydrofolate reductase, leading to impaired DNA synthesis and cell replication. 6-Mercaptopurine is a purine analog that interferes with nucleotide synthesis and metabolism, further inhibiting DNA and RNA production. The combination acts synergistically by targeting different steps in the purine biosynthesis pathway, resulting in enhanced cytotoxicity against malignant lymphoblasts[1][2][4]. This regimen has been shown to improve remission rates compared to monotherapy but may increase the risk of certain toxicities or secondary malignancies depending on dose intensity and patient-specific factors such as thiopurine methyltransferase activity[2]. The drugs are typically administered orally during maintenance phases following induction chemotherapy for ALL.

Other names
MTX + 6-MPmethotrexate and 6-mercaptopurine
02

Targets

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

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