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When IDH1 undergoes mutation, it catalyzes the conversion of \u03b1\u2010KG into the oncogenic metabolite 2\u2010hydroxyglutarate (2\u2010HG). Subsequently, 2\u2010HG competitively suppresses a range of \u03b1\u2010KG\u2010dependent dioxygenase activities, ultimately leading to hypermethylation of DNA or histones, which in turn causes the occurrence of various malignant tumors, including acute myeloid leukemia (AML), glioma, and chondrosarcoma. Currently, the FDA has granted approval for the use of the small molecule inhibitor Ivosidenib (AG\u2010120) in the treatment of IDH1\u2010mutated AML and cholangiocarcinoma. Although AG\u2010120 has benefited patients clinically, drug resistance has gradually emerged and has become a major problem in the treatment of mutant IDH1 (mIDH1) diseases. In this review, we highlighted the function of IDH1 mutations in cancer treatment and described detailed resistance mechanisms in terms of IDH1\u2010specific mutation sites. Representative mIDH1 inhibitors and their binding modes were also discussed. 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