Thiopurine-based therapeutic drugs may accumulate to toxic levels in patients carrying genetic variants of the drug-metabolizing enzyme TPMT. The PGX-TPMT StripAssay® identifies the most frequent TPMT variants of therapeutic relevance.
Thiopurines are widely used in the treatment of leukemias and autoimmune disorders, and as immunosuppressants after organ transplantation.
Thiopurine compounds are converted to therapeutically inactive metabolites by thiopurine S-methyltransferase (TPMT). Certain TPMT isoforms have substantially reduced activity leading to elevated thiopurine blood levels at standard dosage. Subsequent toxic myelosuppression may occur and may lead to life-threatening conditions.
Assessment of the patient’s TPMT isoform is a prerequisite for avoiding toxic effects of thiopurine treatment.