TPMT is best known for its role in the metabolism of the thiopurine drugs such as azathioprine, 6-mercaptopurine and 6-thioguanine. TPMT catalyzes the S-methylation of thiopurine drugs.

2012年9月20日 · Individuals with thiopurine S-methyl transferase (TPMT) or nucleotide diphosphatase (NUDT15) deficiency may be at an increased risk of severe and life-threatening myelotoxicity if receiving conventional doses of azathioprine. Death associated with pancytopenia has been reported in individuals with absent TPMT activity receiving azathioprine.

2021年11月9日 · Thiopurine methyltransferase (TPMT) is an enzyme that breaks down a class of drugs called thiopurines. TPMT tests are used to identify people at risk of developing severe side effects from thiopurine treatment.

Thiopurine S-methyltransferase (TPMT) deficiency is a condition characterized by significantly reduced activity of an enzyme that helps the body process drugs called thiopurines. These drugs, which include 6-thioguanine, 6-mercaptopurine, and azathioprine, inhibit (suppress) the body's immune system.

The inactivation of thiopurine drugs is catalyzed in part by thiopurine methyltransferase (TPMT) and nudix hydrolase 15 (NUDT15). This test fact sheet focuses on enzyme activity phenotype testing for TPMT, which can be measured directly prior to drug administration.

2023年6月15日 · The most commonly used thiopurine drug is called azathioprine. Approximately 0.3% of the population lack thiopurine s-methyltransferase (TPMT), an enzyme which helps remove thiopurine drugs such as azathioprine from the body.

The recommendation for a TPMT intermediate metabolizer/NUDT15 intermediate metabolizer has been updated for all thiopurines to recommend a starting dose at 20%-50% of normal dosages, depending on the starting dose. See here for updated recommendation tables (azathioprine, mercaptopurine, thioguanine).

These drugs, which include 6-thioguanine, 6-mercaptopurine, and azathioprine, inhibit (suppress) the body's immune system. They are used to treat several forms of cancer and other disorders involving immune system malfunction, such as Crohn's disease and rheumatoid arthritis .

2025年3月1日 · This comprehensive review explores the role of TPMT in drug-drug interactions by investigating its interactions with co-factors, substrates, and inhibitors. We focus on the principal interactions of TPMT with clinically relevant inhibitors, and add to this information with molecular docking analyses for the substrate and co-factor binding sites ...

Thiopurine methyltransferase (TPMT) catalyzes the S-methylation of thiopurine drugs such as 6-mercaptopurine (6-MP), thioguanine and azathioprine (AZA). These drugs are used to treat conditions such as acute lymphoblastic leukemia, inflammatory bowel disease, rheumatoid arthritis, and organ transpla …