Ivosidenib (trade name Tibsovo) is a potent inhibitor of isocitrate dehydrogenase 1 (IDH1). It is an orally administered small molecule drug that is used for the treatment of acute myeloid leukemia (AML) in patients with IDH1 mutations. Ivosidenib was approved by the FDA in July 2018.
Chemical name: (S)-2-(4-((2-(1H-tetrazol-5-yl)thiazol-4-yl)amino)phenyl)-3-(4-(2-(1-methylpyridin-4-yl)pyrimidin-4-yl)phenyl)acrylonitrile
Molecular formula: C27H20N8S
Formula weight: 500.56 g/mol
CAS No: 3448347-49-6
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Health benefits of this product: Ivosidenib is primarily used for the treatment of AML in patients with IDH1 mutations. AML is a type of cancer that affects the blood and bone marrow. The IDH1 gene mutation is found in approximately 6-10% of AML patients. Ivosidenib works by blocking the activity of the mutated IDH1 protein, which inhibits cancer cell growth and promotes apoptosis (programmed cell death) in cancer cells.
Potential effects: Ivosidenib has been shown to produce positive therapeutic effects on AML patients with IDH1 mutations. In a phase 1 trial, 73% of patients achieved a complete remission or complete remission with incomplete hematologic recovery (CR/CRh) after receiving ivosidenib therapy. In a phase 3 study (AGILE), the median overall survival in patients treated with ivosidenib was 8.4 months, compared to 4.1 months for those who received placebo. Ivosidenib has also been shown to have a manageable safety profile.
Product mechanism: Ivosidenib is an isocitrate dehydrogenase 1 (IDH1) inhibitor. The IDH1 enzyme normally converts isocitrate to alpha-ketoglutarate in the Krebs cycle. This is an important step in producing energy in cells. However, in some cancer cells, the IDH1 gene is mutated, leading to the production of an abnormal form of the IDH1 enzyme. This abnormal enzyme produces 2-hydroxyglutarate (2-HG), which promotes cancer cell growth and inhibits apoptosis. Ivosidenib blocks the activity of the mutated IDH1 enzyme, which reduces the level of 2-HG and promotes apoptosis in cancer cells.
Safety: Ivosidenib has a manageable safety profile. The most common side effects observed in clinical trials were fatigue, nausea, vomiting, diarrhea, decreased appetite, and leukocytosis (an increase in white blood cells). More serious side effects, such as differentiation syndrome and QT prolongation, have also been observed in some patients. Patients receiving ivosidenib should be closely monitored for these and other potential side effects.
Side effects: The most common side effects of ivosidenib include fatigue, nausea, vomiting, diarrhea, decreased appetite, and leukocytosis
