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Ivosidenib

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ivosidenib

 (I-voh-SIH-deh-nib)A drug used to treat acute myeloid leukemia (AML) that has relapsed (come back) or has not gotten better after treatment with other anticancer therapy. It is used in patients whose cancer has a mutated (changed) form of a gene called isocitrate dehydrogenase-1 (IDH1). It is also being studied in the treatment of other types of cancer. Ivosidenib blocks the protein made by the mutated IDH1 gene. Blocking this protein may help keep cancer cells from growing. Ivosidenib is a type of enzyme inhibitor and a type of targeted therapy. Also called Tibsovo.

Clinical use of Ivosidenib

Ivosidenib is an orally available small molecule inhibitor of isocitrate dehydrogenase 2 which is used as an antineoplastic agent in the treatment of selected cases of acute myeloid leukemia (AML).     

Ivosidenib
Ivosidenib

Liver safety of Ivosidenib

Ivosidenib is associated with a moderate rate of serum aminotransferase elevations during therapy and is suspected to be the cause of rare instances of clinically apparent acute liver injury.

Mechanism of action of Ivosidenib

Ivosidenib (eye" voe sid' i nib) is a small molecule inhibitor of isocitrate dehydrogenase-1 (IDH1), an enzyme rearranged and mutated in some forms of leukemia and lymphoma.  The mutated IDH promotes unregulated cell growth and proliferation and is overexpressed in some leukemias.  Ivosidenib has been found to inhibit mutated IDH1 and in several clinical trials was found to induce objective responses in a proportion of patients with refractory AML with detectable IDH1 mutations. 

FDA approval information for Ivosidenib

Ivosidenib received accelerated approval for use refractory or relapsed AML with mutated IDH1 in the United States in 2018. A specific small molecule inhibitor of IDH2, enasidenib, was approved as therapy of AML with mutations in IDH2 in 2017.  These two IDH inhibitors appear to have similar efficacy against their respective mutated enzyme as well as similar adverse effects. 

Dosage and administration for Ivosidenib

Ivosidenib is available in tablets of 250 mg under the brand name Tibsovo.  The dose is 500 mg once daily, continued until progressive disease or intolerable toxicity occurs. 

Side effects of Ivosidenib

Side effects are common and can include fatigue, arthralgia, fever, diarrhea, nausea, abdominal pain, dyspnea, cough, peripheral edema, mucositis and rash.  Uncommon, but potentially severe side effects include differentiation syndrome, QTc prolongation, Guillian Barre’ syndrome, and embryo-fetal toxicity.

Alphabetic list of antineoplastic agents - 0-9 - A1 - A2 - A3 - A4 - A5 -A6 - B - C - D - E - F - G - H - I - JK - L - M - NO - PQ - R - S - T - UVW - XYZ

 

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