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Tibsovo: Mechanism of Action
The enzyme activity of the mutant isocitrate dehydrogenase 1 (IDH1) is inhibited by a small medication known as ivosidenib. R132H and R132C mutations are the most prevalent in AML patients.
Compared to wild-type IDH1, ivosidenib significantly decreased the quantity required to inhibit a variety of IDH1 R132 mutants in vitro. Ivosidenib decreased 2HG levels and increased myeloid growth both in vitro and in vivo in mice xenograft models of AML with an IDH1 mutation by inhibiting the mutant IDH1 enzyme. Blood samples from people with AML and mutant IDH1 showed a reduction in ex-vivo 2-HG levels, blast counts, and the fraction of mature myeloid cells after treatment with ivosidenib.
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