| 词条 | Ciluprevir |
| 释义 |
| IUPAC_name = (2R,6S,12Z,13aS,14aR,16aS)-6-[(Cyclopentyloxycarbonyl)amino]-2-({7-methoxy-2-[(propan-2-ylamino)-1,3-thiazol-4-yl]quinolin- 4-yl}oxy)-5,16-dioxo-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid | image = Ciluprevir.svg | width = 285 | alt = | caption = | tradename = | pregnancy_AU = | pregnancy_US = | pregnancy_category = | legal_AU = | legal_CA = | legal_UK = | legal_US = | legal_status = Development terminated | routes_of_administration = By mouth | bioavailability = | protein_bound = >99.1%[1] | metabolism = | elimination_half-life = | excretion = | CAS_number = 300832-84-2 | ATCvet = | ATC_prefix = None | ATC_suffix = | DrugBank = | UNII_Ref = {{fdacite|correct|FDA}} | UNII = 75C8DU40T0 | ChEMBL = 297884 | PubChem = 9853710 | ChemSpiderID = 8029420 | C=40 | H=50 | N=6 | O=8 | S=1 | molecular_weight = 774.93 g/mol | smiles = O=C2N[C@]7(C(=O)O)C[C@H]7/C=C\\CCCCC[C@H](NC(=O)OC1CCCC1)C(=O)N6[C@H]2C[C@@H](Oc3cc(nc4c3ccc(OC)c4)c5nc(sc5)NC(C)C)C6 | StdInChI = 1S/C40H50N6O8S/c1-23(2)41-38-43-32(22-55-38)31-19-34(28-16-15-26(52-3)17-30(28)42-31)53-27-18-33-35(47)45-40(37(49)50)20-24(40)11-7-5-4-6-8-14-29(36(48)46(33)21-27)44-39(51)54-25-12-9-10-13-25/h7,11,15-17,19,22-25,27,29,33H,4-6,8-10,12-14,18,20-21H2,1-3H3,(H,41,43)(H,44,51)(H,45,47)(H,49,50)/b11-7-/t24-,27-,29+,33+,40-/m1/s1 | StdInChIKey = PJZPDFUUXKKDNB-KNINVFKUSA-N }}Ciluprevir was a drug used experimentally in the treatment of hepatitis C. It is manufactured by Boehringer Ingelheim and developed under the research code of BILN 2061. It was the first-in-class NS3/4A protease inhibitor to enter clinical development and tested in human.[2] Ciluprevir is a potent competitive reversible inhibitor of NS3/4A protease from HCV genotype 1a (Ki = 0.3 nM) and 1b (Ki = 0.66 nM). It shows good selectivity for NS3 protease against representative serine and cysteine proteases, human leukocyte elastase and cathepsin B (IC50 > 30 μM).[1] Its development was halted in phase Ib clinical trials because of toxicity in animals. However, ciluprevir scaffold was exploited to design new macrocyclic inhibitors such as simeprevir (TMC-435) and danoprevir.[3] References1. ^1 {{cite book|editor1-last=Tan|editor1-first=Seng-Lai|editor2-last=He|editor2-first=Yupeng|title=Hepatitis C: Antiviral Drug Discovery and Development|date=2011|publisher=Caister Academic Press|location=Norfolk, UK|isbn=978-1-904455-78-3|page=199}} {{RNA antivirals}}{{antiinfective-drug-stub}}2. ^{{cite book | editor1-last = Tan | editor1-first = Seng-Lai | title = Hepatitis C Viruses: Genomes and Molecular Biology | date = 2006 | publisher = Horizon Bioscience | location = Norfolk (UK) | isbn = 978-1-904933-20-5 | url = https://www.ncbi.nlm.nih.gov/books/NBK1613/ | chapter = 6. HCV NS3-4A Serine Protease}} 3. ^{{cite journal | last1 = Chatel-Chaix | first1 = L | last2 = Baril | first2 = M | last3 = Lamarre | first3 = D | title = Hepatitis C Virus NS3/4A Protease Inhibitors: A Light at the End of the Tunnel | journal = Viruses | date = August 2010 | volume = 2 | issue = 8 | pages = 1752–65 | doi = 10.3390/v2081752 | pmid = 21994705 | pmc = 3185733}} 2 : Abandoned drugs|NS3/4A protease inhibitors |
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