What inactivates 6-mercaptopurine?

[Perrywalton]

6-Mercaptopurine (6-MP) is a medication used to treat certain types of cancer and autoimmune diseases. Once inside the body, it needs to be activated to work effectively. However, it can also be inactivated through different pathways, which means it stops working. One major way 6-MP is inactivated is by an enzyme called thiopurine methyltransferase (TPMT). This enzyme adds a methyl group to 6-MP, turning it into an inactive form called 6-methylmercaptopurine (6-MMP), which can cause liver toxicity if it builds up too much147. Another pathway involves an enzyme called xanthine oxidase (XO), which converts 6-MP into 6-thiouric acid, another inactive form that doesn't contribute to the drug's therapeutic effects61719. Some people have genetic variations that affect how well these enzymes work, which can influence how much of the medicine gets inactivated. For example, people with low TPMT activity may have higher levels of active 6-MP, leading to more side effects. Understanding these inactivation pathways helps doctors adjust doses to make the treatment safer and more effective for each patient.

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