Enasidenib
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| Trade names | Idhifa |
| Other names | AG-221 |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a617040 |
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| Routes of administration | By mouth |
| Drug class | IDH2 inhibitor |
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| Chemical and physical data | |
| Formula | C19H17F6N7O |
| Molar mass | 473.383 g·mol−1 |
| 3D model (JSmol) | |
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Enasidenib, sold under the brand name Idhifa, is an anti-cancer medication used to treat relapsed or refractory acute myeloid leukemia.[2][3] It is an inhibitor of isocitrate dehydrogenase 2 (IDH2).[2]
Common side effects of enasidenib include nausea, vomiting, diarrhea, increased levels of bilirubin (substance found in bile), and decreased appetite.[4] Women who are pregnant or breastfeeding should not take enasidenib because it may cause harm to a developing fetus or a newborn baby.[4]
Enasidenib was approved for medical use in the United States in August 2017.[2][4] The US Food and Drug Administration (FDA) considers it to be a first-in-class medication.[5]
Medical use
Enasidenib is indicated for the treatment of relapsed or refractory acute myeloid leukemia in adults with specific mutations of the IDH2 gene, determined by an FDA-approved IDH2 companion diagnostic test.[2][3]
Adverse effects
Common side effects of enasidenib include nausea, vomiting, diarrhea, increased levels of bilirubin (substance found in bile) and decreased appetite.[4] Women who are pregnant or breastfeeding should not take enasidenib because it may cause harm to a developing fetus or a newborn baby.[4] The prescribing information for enasidenib includes a boxed warning that an adverse reaction known as differentiation syndrome can occur and can be fatal if not treated.[4][6]
History
The efficacy of enasidenib was studied in a single-arm trial of 199 participants with relapsed or refractory acute myeloid leukemia who had isocitrate dehydrogenase-2 mutations as detected by the RealTime IDH2 Assay.[4] The trial measured the percentage of participants with no evidence of disease and full recovery of blood counts after treatment (complete remission), as well as participants with no evidence of disease and partial recovery of blood counts after treatment (complete remission with partial hematologic recovery).[4] With a minimum of six months of treatment, 19 percent of participants experienced complete remission for a median 8.2 months, and 4 percent of participants experienced complete remission with partial hematologic recovery for a median 9.6 months.[4] Of the 157 participants who required transfusions of blood or platelets due to acute myeloid leukemia at the start of the study, 34 percent no longer required transfusions after treatment with enasidenib.[4]
The US Food and Drug Administration (FDA) granted the application for enasidenib priority review and orphan drug designations.[4]
Society and culture
Legal status
Enasidenib was approved by the FDA in August 2017, for relapsed or refractory acute myeloid leukemia (AML) in people with specific mutations of the IDH2 gene, determined by an FDA-approved IDH2 companion diagnostic test.[2][3][4]
References
- ^ "Summary Basis of Decision (SBD) for Idhifa". Health Canada. 23 October 2014. Archived from the original on 8 August 2024. Retrieved 29 May 2022.
- ^ a b c d e f "Idhifa- enasidenib mesylate tablet, film coated". DailyMed. 21 December 2023. Archived from the original on 23 March 2021. Retrieved 8 August 2024.
- ^ a b c Kim ES (October 2017). "Enasidenib: First Global Approval". Drugs. 77 (15): 1705–1711. doi:10.1007/s40265-017-0813-2. PMID 28879540. S2CID 7685848.
- ^ a b c d e f g h i j k l "FDA approves new targeted treatment for relapsed or refractory acute myeloid leukemia". U.S. Food and Drug Administration (Press release). 1 August 2017. Archived from the original on 2 August 2024. Retrieved 8 August 2024.
This article incorporates text from this source, which is in the public domain.
- ^ New Drug Therapy Approvals 2017 (PDF). U.S. Food and Drug Administration (FDA) (Report). January 2018. Archived from the original on 23 October 2020. Retrieved 16 September 2020.
- ^ Brunton LL, Hilal-Dandan R, Knollmann BC (5 December 2017). Goodman & Gilman's the pharmacological basis of therapeutics (13th ed.). New York: McGraw Hill Education. ISBN 9781259584732. OCLC 993810322.
External links
- "Enasidenib mesylate". NCI Dictionary of Cancer Terms. National Cancer Institute.
- "Enasidenib mesylate". National Cancer Institute. 8 August 2017.
