テラプレビル

Also known as VX-950, VX 950, (1S,3aR,6aS)-(2S)-2-cyclohexyl-N-(pyrazinylcarbonyl)glycyl-3-methyl-L-valyl-N-((1S)-1-((cyclopropylamino)oxoacetyl)butyl)octahydrocyclopenta(c)pyrrole-1-carboxamide, (1S,3AR,6as)-(2S)-2-cyclohexyl-N-(pyrazinylcarbonyl)glycyl-3-methyl-L-valyl-N-((1S)-1-((cyclopropylamino)oxoacetyl)butyl)octahydrocyclopenta(c)pyrrole-1-carboxamide, Telaprevir

Telaprevir (VX-950), was marketed under the brand names Incivek and Incivo, is a pharmaceutical drug for the treatment of hepatitis C co-developed by Vertex Pharmaceuticals and Johnson & Johnson. It is a member of a class of antiviral drugs known as protease inhibitors. Specifically, telaprevir inhibits the hepatitis C viral enzyme NS3/4A serine protease. Telaprevir is only indicated for use against hepatitis C genotype 1 viral infections and has not been proven to be safe or effective when used for other genotypes of the virus. The standard therapy of pegylated interferon and ribavirin is les

Key facts

Drug.Verifiedfields: changed
Drug.Watchedfields: changed
Drug.verifiedrevid: 458630745
Drug.IUPAC_name: (1S,3aR,6aS)-2-[(2S)-2-[[(2S)-2-Cyclohexyl-2-(pyrazine-2-carbonylamino)acetyl]amino]-3,3-dimethylbutanoyl]-N-[(3S)-1-(cyclopropylamino)-1,2-dioxohexan-3-yl]-3,3a,4,5,6,6a-hexahydro-1H-cyclopenta[c]pyrrole-1-carboxamide | image = Telaprevir structure.svg | image_class = skin-invert-image | width = 280 | tradename = Incivek, Incivo | Drugs.com = | MedlinePlus = a611038 | licence_US = Telaprevir | pregnancy_AU = | pregnancy_US = B | pregnancy_category = | legal_AU = | legal_CA = | legal_UK = | legal_US = Rx-only | legal_status = | routes_of_administration = Oral | bioavailability = | protein_bound = 59–76% | metabolism = extensive hepatic | elimination_half-life = 9–11 hours | excretion = 90% (bile), 9% (exhaled air), 1% (urine) | IUPHAR_ligand = 7871 | CAS_number_Ref = | CAS_number = 402957-28-2 | ATC_prefix = J05 | ATC_suffix = AP02 | ChEBI_Ref = | ChEBI = 68595 | ChEMBL_Ref = | ChEMBL = 231813 | PubChem = 3010818 | DrugBank_Ref = | DrugBank = DB05521 | ChemSpiderID_Ref = | ChemSpiderID = 2279948 | UNII_Ref = | UNII = 655M5O3W0U | KEGG_Ref = | KEGG = D09012 | NIAID_ChemDB = 213006 | C=36 | H=53 | N=7 | O=6 | StdInChI_Ref = | StdInChI = 1S/C36H53N7O6/c1-5-10-25(29(44)34(48)39-23-15-16-23)40-33(47)28-24-14-9-13-22(24)20-43(28)35(49)30(36(2,3)4)42-32(46)27(21-11-7-6-8-12-21)41-31(45)26-19-37-17-18-38-26/h17-19,21-25,27-28,30H,5-16,20H2,1-4H3,(H,39,48)(H,40,47)(H,41,45)(H,42,46)/t22-,24-,25-,27-,28-,30+/m0/s1 | StdInChIKey_Ref = | StdInChIKey = BBAWEDCPNXPBQM-GDEBMMAJSA-N | SMILES = CCC[C@@H](C(=O)C(=O)NC1CC1)NC(=O)[C@@H]2[C@H]3CCC[C@H]3CN2C(=O)[C@H](C(C)(C)C)NC(=O)[C@H](C4CCCCC4)NC(=O)c5cnccn5 | SMILES2 = C0CC0NC(=O)C(=O)[C@H](CCC)NC(=O)[C@@H]1[C@H]2CCC[C@H]2CN1C(=O)[C@H](C(C)(C)C)NC(=O)[C@H](C3CCCCC3)NC(=O)c4nccnc4

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Research

1,588 papers

Telaprevir.Drugs in R&D · 2010
Telaprevir user's guide.Clinics in liver disease · 2011
[Telaprevir resistance].Enfermedades infecciosas y microbiologia clinica · 2013
Telaprevir user's guide.Liver international : official journal of the International Association for the Study of the Liver · 2012
Telaprevir-related dermatitis.JAMA dermatology · 2013

via PubMed

Article · 日本語

テラプレビル（Telaprevir）は、セリンプロテアーゼ阻害作用を持つ抗ウイルス薬に分類される。テラプレビルはC型肝炎ウイルスのへの選択性が高い。遺伝子型1型（1a、1b）または2型（2a、2b）のウイルスに対してのみ有効性・安全性が確認されており、他のタイプのウイルスへの効果は明らかではない。C型肝炎の治療薬である。標準治療であるとリバビリンの併用療法は1型C型肝炎には効果が弱い。商品名テラビック。田辺三菱製薬が創薬した。開発コードMP-424、VX-950。日本ではC型肝炎ウイルスに対する最初の直接作用型抗ウイルス薬（Direct-Acting Antiviral: DAA）として2011年から2017年に使用された（現在販売終了）。

Abstract from DBpedia / Wikipedia · CC BY-SA

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