| 词条 | Enasidenib |
| 释义 |
| drug_name = | INN = | type = | image = Enasidenib.svg | caption = | pronounce = | tradename = Idhifa | pregnancy_AU = | pregnancy_US = | pregnancy_category= | routes_of_administration = | legal_US = Rx-only | legal_status = | bioavailability = | protein_bound = | metabolism = | excretion = | CAS_number = 1446502-11-9 | class = | ATCvet = | ATC_prefix = L01 | ATC_suffix = XX59 | PubChem = 89683805 | DrugBank = | ChemSpiderID = 38772329 | UNII = | KEGG = D10901 | ChEBI = | ChEMBL = | StdInChI = 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) | StdInChIKey = DYLUUSLLRIQKOE-UHFFFAOYSA-N | C=19 | H=17 | F=6 | N=7 | O=1 | SMILES = CC(C)(CNC1=NC(=NC(=N1)NC2=CC(=NC=C2)C(F)(F)F)C3=NC(=CC=C3)C(F)(F)F)O }} Enasidenib (INN; trade name Idhifa) is a drug 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.[1] It is an inhibitor of IDH2. It was developed by Agios Pharmaceuticals and is licensed to Celgene for further development. Medical useEnasidenib 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.[1] Adverse effects{{expand section|date=November 2017}}The US Food and Drug Administration (FDA) says the life-threatening side effect known as differentiation syndrome is not being recognized by clinicians in patients receiving the acute myeloid leukemia (AML) drug enasidenib (Idhifa, Celgene).Early recognition and aggressive management of differentiation syndrome are needed to lessen the likelihood of serious illness and death, according to the FDA. The syndrome has occurred as early as 10 days and up to 5 months after starting the medicine. PharmacologyIsocitrate 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,[1] in those affected with AML. Enasidenib disrupts this cycle by decreasing total (R)-2-HG levels in the mitochondria.{{mcn|date=November 2017}} HistoryAgios Pharmaceuticals was founded in Cambridge, Massachusetts in 2008.[1] The drug was discovered in 2009 by scientists at Agoios and the development names for the drug was AG-221 and CC-90007.{{cn|date=November 2017}} Agios Pharmaceuticals and Celgene entered into a partnership in 2010,[1][2] which was revised in 2016.[3][4] The first Phase I studies of enasidenib were conducted in 2013.[5] The FDA granted fast track designation and orphan drug status for acute myeloid leukemia in 2014.[6] The fast track designation allows this drug to be developed in what in markedly less than the average 14 years it takes for a drug to be developed and approved.[7] 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.[4][13][8] The trade name under which it was approved was Idhifa.[9] References1. ^{{cite news|last1=Carroll|first1=John|title=Agios Pharmaceuticals - 2009 Fierce 15|url=http://www.fiercebiotech.com/special-report/agios-pharmaceuticals-2009-fierce-15|work=FierceBiotech|date=2009|language=en}} 2. ^{{cite news|last1=Carroll|first1=John|title=Agios scores $130M upfront from ambitious Celgene pact|url=http://www.fiercebiotech.com/biotech/agios-scores-130m-upfront-from-ambitious-celgene-pact|work=FierceBiotech|date=April 15, 2010|language=en}} 3. ^{{cite news|last1=Carroll|first1=John|title=Celgene pays $200M to start ambitious Agios immuno-oncology pact|url=http://www.fiercebiotech.com/celgene-pays-200m-to-kick-off-ambitious-immuno-oncology-pact-agios|work=FierceBiotech|date=May 17, 2016|language=en}} 4. ^1 2 3 4 5 {{cite journal|last1=Kim|first1=ES|title=Enasidenib: First Global Approval|journal=Drugs|volume=77|issue=15|pages=1705|date=6 September 2017|doi=10.1007/s40265-017-0813-2|pmid=28879540}} 5. ^{{cite web|title=Agios Form 10-Q For the quarterly period ended September 30, 2016|url=https://www.sec.gov/Archives/edgar/data/1439222/000119312516758835/d172494d10q.htm|publisher=SEC Edgar|accessdate=2 November 2017}} 6. ^{{cite web|title=Enasidenib|url=http://adisinsight.springer.com/drugs/800038591|website=AdisInsight|accessdate=31 January 2017}} 7. ^{{cite news|last1=Fidler|first1=Ben|title=Celgene Plots Speedy FDA Filing for Agios Blood Cancer Drug|url=http://www.xconomy.com/boston/2016/09/07/celgene-plots-speedy-fda-filing-for-agios-blood-cancer-drug/|work=Xconomy|date=7 September 2016}} 8. ^{{cite news|title=Press release: FDA granted regular approval to enasidenib for the treatment of relapsed or refractory AML|url=https://www.fda.gov/drugs/informationondrugs/approveddrugs/ucm569482.htm|work=FDA|date=August 1, 2017|language=en}} 9. ^1 {{cite news|title=FDA Approves New Treatment for Leukemia|url=https://www.genengnews.com/gen-news-highlights/fda-approves-new-treatment-for-leukemia/81254750|work=GEN|date=August 2, 2017}} External links
4 : Antineoplastic drugs|Pyridines|Triazines|Trifluoromethyl compounds |
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