Thiopurine is an analogue of apurine wherein a C=O/C-OH group has been replaced by a C=S/C-SH group. Theseorganosulfur compounds are bioactive in beneficial and complicating manner. They interfere with purine biosynthesis. Thiopurine drugsantimetabolites widely used in the treatment ofacute lymphoblastic leukemia,autoimmune disorders (e.g.,Crohn's disease,rheumatoid arthritis), andorgan transplant recipients.Azathioprine is aprodrug. 6-Mercaptopurine is substrate for three enzyme]]s:thiopurine methyltransferase (to give 6-methylmercaptopurine),xanthine oxidase (to give6-thiouric acid], andhypoxanthine phosphoribosyltransferase (to give 6-thioisonine 5'-monphosphate).[1] They are also substrates fornudix hydrolase 15 (NUDT15).[2]
Litigation over patents covering diagnostic kits to monitor the dosing of these drugs led to a US Supreme Court case,Mayo Collaborative Services v. Prometheus Laboratories, Inc. that dramatically changed the nature of patent law in the United States.[3][4]
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