Mercaptopurine is an antineoplastic agent used to treat acute lymphocytic leukemia. An antimetabolite antineoplastic agent with immunosuppressant properties.
- Mechanism
- Curator reviewed
Mercaptopurine competes with hypoxanthine and guanine for the enzyme hypoxanthine-guanine phosphoribosyltransferase (HGPRTase) and is itself converted to thioinosinic acid (TIMP). TIMP inhibits several reactions that involve inosinic acid (IMP), such as the conversion of IMP to xanthylic acid (XMP) and the conversion of IMP to adenylic acid (AMP) via adenylosuccinate (SAMP). Upon methylation, TIMP forms 6-methylthioinosinate (MTIMP) which inhibits glutamine-5-phosphoribosylpyrophosphate amidotransferase in addition to TIMP. Glutamine-5-phosphoribosylpyrophosphate amidotransferase is the first enzyme unique to the de novo pathway for purine ribonucleotide synthesis. According to experimental findings using radiolabeled mercaptopurine, mercaptopurine may be recovered from the DNA in the form of deoxythioguanosine. In comparison, some mercaptopurine may be converted to nucleotide derivatives of 6-thioguanine (6-TG) via actions of inosinate (IMP) dehydrogenase and xanthylate (XMP) aminase that convert TIMP to thioguanylic acid (TGMP).
- Primary indication
- For remission induction and maintenance therapy of acute lymphatic leukemia.Curator reviewed · 6 structured indications
- Formula / weight
- C5H4N4S · 152.177 g/mol (avg)
- First approval
- Canada, 2013 · United States, 2004 · European Union, 2020
- Also known as
- 1,9-DIHYDRO-6H-PURINE-6-THIONE · 6 Thiohypoxanthine · 6MP · Mercapurin
- Code names
- Bw 57-323H · NCI-C04886 · U-4748 · WR-2785
- Brand names
Resolves to
GLVAUDGFNGKCSF-UHFFFAOYSA-NSMILESS=C1N=CNC2=C1NC=N2What you can answer from here — as of September 23, 2026
Which drugs share a target with Mercaptopurine, and which of those have an active Phase 3 trial?
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