| 词条 | Glecaprevir |
| 释义 |
| IUPAC_name = (3aR,7S,10S,12R,21E,24aR)-7-tert-Butyl-N(1R,2R)-2-(difluoromethyl)-1-[(1-methylcyclopropane-1-sulfonyl)carbamoyl]cyclopropyl20,20-difluoro-5,8-dioxo-2,3,3a,5,6,7,8,11,12,20,23,24a-dodecahydro-1H,10H-9,12-methanocyclopenta[18,19][1,10,17,3,6]trioxadiazacyclonon adecino[11,12-b]quinoxaline-10-carboxamide | image = Glecaprevir.svg | width = | tradename = Mavyret (combination with pibrentasvir) | Drugs.com = | licence_US = | pregnancy_AU = | pregnancy_US = | pregnancy_category = | legal_AU = | legal_CA = | legal_UK = | legal_US = | legal_status = | routes_of_administration = By mouth | bioavailability = | protein_bound = 97.5% | metabolism = CYP3A | elimination_half-life = 6 hours | excretion = Faeces (92.1%), urine (0.7%) | CAS_number = 1365970-03-1 | ATC_prefix = None | ATC_suffix = | PubChem = 66828839 | ChemSpiderID = 35013015 | UNII = K6BUU8J72P | KEGG = D10814 | ChEMBL = | NIAID_ChemDB = | PDB_ligand = | synonyms = ABT-493 | chemical_formula = | C = 38 | H = 46 | F = 4 | N=6 | O=9 | S=1 | molecular_weight = | smiles = CC1(CC1)S(=O)(=O)NC(=O)[C@]2(C[C@H]2C(F)F)NC(=O)[C@@H]3C[C@@H]4CN3C(=O)[C@@H](NC(=O)O[C@@H]5CCC[C@H]5OC/C=C/C(C6=NC7=CC=CC=C7N=C6O4)(F)F)C(C)(C)C | StdInChI = 1S/C38H46F4N6O9S/c1-35(2,3)28-32(50)48-19-20(17-24(48)30(49)46-37(18-21(37)29(39)40)33(51)47-58(53,54)36(4)14-15-36)56-31-27(43-22-9-5-6-10-23(22)44-31)38(41,42)13-8-16-55-25-11-7-12-26(25)57-34(52)45-28/h5-6,8-10,13,20-21,24-26,28-29H,7,11-12,14-19H2,1-4H3,(H,45,52)(H,46,49)(H,47,51)/b13-8+/t20-,21+,24+,25-,26-,28-,37-/m1/s1 | StdInChIKey = MLSQGNCUYAMAHD-ITNVBOSISA-N }}Glecaprevir (INN,[1]) is a hepatitis C virus (HCV) nonstructural (NS) protein 3/4A protease inhibitor that was identified jointly by AbbVie and Enanta Pharmaceuticals. It is being developed as a treatment of chronic hepatitis C infection in co-formulation with an HCV NS5A inhibitor pibrentasvir. Together they demonstrated potent antiviral activity against major HCV genotypes and high barriers to resistance in vitro.[2] On 19 December 2016, AbbVie submitted a new drug application to the U.S. Food and Drug Administration for the glecaprevir/pibrentasvir (trade name Mavyret) regimen for the treatment of all major genotypes (1–6) of chronic hepatitis C. On 3 August 2017 the FDA approved the combination for hepatitis C treatment.[3] In Europe, it was approved on 17 August 2017 for the same indication, under the trade name Maviret.[4] References1. ^{{cite web | title = International Nonproprietary Names for Pharmaceutical Substances (INN). Recommended International Nonproprietary Names: List 76 | url = http://www.who.int/medicines/publications/druginformation/innlists/RL76.pdf | publisher = World Health Organization | accessdate = 25 February 2017 | page = 503}} {{RNA antivirals}}{{antiinfective-drug-stub}}2. ^{{cite journal | last1 = Lawitz | first1 = EJ | last2 = O'Riordan | first2 = WD | last3 = Asatryan | first3 = A | last4 = Freilich | first4 = BL | last5 = Box | first5 = TD | last6 = Overcash | first6 = JS | last7 = Lovell | first7 = S | last8 = Ng | first8 = TI | last9 = Liu | first9 = W | last10 = Campbell | first10 = A | last11 = Lin | first11 = CW | last12 = Yao | first12 = B | last13 = Kort | first13 = J | title = Potent Antiviral Activities of the Direct-Acting Antivirals ABT-493 and ABT-530 with Three-Day Monotherapy for Hepatitis C Virus Genotype 1 Infection | journal = Antimicrobial Agents and Chemotherapy | date = 28 December 2015 | volume = 60 | issue = 3 | pages = 1546–55 | doi = 10.1128/AAC.02264-15 | pmid = 26711747 | pmc = 4775945}} 3. ^{{cite news | title = AbbVie Submits New Drug Application to U.S. FDA for its Investigational Regimen of Glecaprevir/Pibrentasvir (G/P) for the Treatment of All Major Genotypes of Chronic Hepatitis C. | url = https://news.abbvie.com/news/abbvie-submits-new-drug-application-to-us-fda-for-its-investigational-regimen-glecaprevirpibrentasvir-gp-for-treatment-all-major-genotypes-chronic-hepatitis-c.htm | accessdate = 25 February 2017 | publisher = AbbVie Inc. North Chicago, Illinois, U.S.A. | date = December 19, 2016 | language = en}} 4. ^{{cite web|url=http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Summary_for_the_public/human/004430/WC500233680.pdf|title=Maviret: EPAR – Summary for the public|publisher=European Medicines Agency|date=2017-08-17}} 11 : Carboxamides|Carbamates|Cyclopropanes|Ethers|NS3/4A protease inhibitors|Organofluorides|Pyrrolidines|Quinoxalines|Sulfonamides|Tert-butyl compounds|Cyclopentanes |
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