II. Indications
- Acute Myelogenous Leukemia (AML)
- Acute Lymphoblastic Leukemia (ALL, off-label use)
III. Mechanism
- Synthetic guanosine analog antimetabolite
- Thioguanine is phosphorylated by HGPRT (hypoxanthine-guanine phosphoribosyltransferase)
- Incorporated into DNA and RNA in place of guanosine
- Inhibits DNA and RNA synthesis
- Inhibits GPAT (Glutamine-5-phosphoribosylpyrophosphate amidotransferase)
- Inhibits Purine synthesis
IV. Medications
- Thioguanine 40 mg scored tablets
V. Dosing
- See other references for disease specific dosing protocols
VI. Adverse Effects
- Alopecia
- Hepatotoxicity
- Hyperuricemia
- Myelosuppression
- Thioprine-Related Toxicity (Severe)
- Associated with NUDT15 Gene Anomaly (Nudix Hydrolase 15 deficiency)
VII. Safety
- Avoid in Pregnancy (any trimester)
- Use reliable Contraception
- Avoid in Lactation
- Monitoring