Information about Enasidenib
Enasidenib is an orally available small molecule inhibitor of isocitrate dehydrogenase and antineoplastic agent that is used in the therapy of selected cases of acute myeloid leukemia (AML).
Liver safety of Enasidenib
Enasidenib is associated with a moderate rate of serum aminotransferase elevations during therapy and rare instances of clinically apparent acute liver injury.
Mechanism of action of Enasidenib
Enasidenib (en" a sid' e nib) is a small molecule inhibitor of isocitrate dehydrogenase-2 (IDH2), an enzyme rearranged and mutated in some forms of leukemia and lymphoma. The mutated IDH2 causes epigenetic alterations that result in a block in myeloid cell differentiation. Enasidenib has been found to inhibit mutated IDH2 and in several clinical trials was found to induce objective responses in a high proportion of patients with refractory AML who harbored mutant IDH2.
FDA approval information for Enasidenib
Enasidenib received accelerated approval for use in refractory or relapsed AML with IDH2 mutations in 2017. Enasidenib is available in tablets of 50 and 100 mg under the brand name IDHIFA.
Dosage and administration for Enasidenib
The recommended initial dose is 100 mg once daily, continued until progressive disease or intolerable toxicity occurs. side effects are common and frequently severe (77%), leading to dose interruptions (43%) or discontinuations (17%).
Side effects of Enasidenib
Common adverse events include diarrhea, nausea and vomiting, abdominal pain, fatigue and anorexia. Less common but potentially severe side effects include differentiation syndrome, tumor lysis syndrome and embryo-fetal toxicity.