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Methylthioinosine is a nucleoside that serves as a key metabolite in the intracellular processing of thiopurine drugs like mercaptopurine, which are used in the treatment of acute lymphoblastic leukemia and inflammatory bowel disease. Its phosphorylated forms, such as methylthioinosine monophosphate (meTIMP), are potent inhibitors of de novo purine synthesis, contributing to the cytotoxic effects of thiopurines. Additionally, 5'-methylthioinosine (MTI) is a Plasmodium-specific intermediate in the purine salvage pathway and functions as a pathogen-derived agonist of Toll-like receptor 8 (TLR8), suggesting a role in innate immune sensing of *Plasmodium falciparum*. It has also been investigated for potential activity against SARS-CoV-2 and has been isolated from natural sources.
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