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6-mercaptopurine

Thiopurine drug

Thiopurine drugATC null
CDSCO approved
EXCRETION
not curated
INTERACTIONS
1 major
SEVERE in our sources
PREGNANCY
X
FDA category + note
Top interactions
  • AllopurinolSevereTextbookKDT 7e · p217

Mechanism

6-mercaptopurine (6-MP) serves as a prodrug metabolized by hypoxanthine guanine phosphoribosyl transferase (HGPRT) to 6-thioguanine nucleotides (6-TGNs), which are incorporated into DNA and RNA, resulting in arrest of DNA replication and cytotoxicity. TPMT is responsible for the detoxification of 6-MP.

Indications

Inflammatory bowel diseaseAutoimmune disorders (e.g., systemic lupus erythematosus, rheumatoid arthritis)Childhood acute lymphoblastic leukemiaCrohn’s diseasecancer

Pharmacokinetics

Metabolism
Undergoes S-methylation catalyzed by thiopurine methyltransferase (TPMT) for detoxification.

Contraindications

  • Genetic deficiency in thiopurine methyltransferase (TPMT) (risk of severe toxicities)

Side effects

Serious
  • severe bone marrow toxicity (with thiopurine methyl transferase (TPMT) deficiency)

Pregnancy & lactation

Pregnancy

X

Drug interactions

Allopurinol
Severe
Textbook

Increased 6-mercaptopurine levels and toxicity.

The dose of 6-mercaptopurine should be reduced to 1/3rd.

Source: KDT 7e · p217

Related guidelines

Other Unclassified drugs

Ask House about 6-mercaptopurine

Continue into a citation-backed clinical answer with the drug context already attached.

Sources: KD Tripathi 7e, Goodman & Gilman 14e·Verified: 2026-05-10 · House clinical team