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Samatasvir

Samatasvir (IDX-719) is an experimental drug for the treatment of hepatitis C. It was originally developed by Idenix, and development has been continued by Merck & Co. following their acquisition of Idenix. Samatasvir has shown good results in Phase II trials.[1]

Samatasvir
Clinical data
Routes of
administration
Oral
Legal status
Legal status
  • Investigational
Identifiers
  • N-((1R)-2-((2S)-2-(5-(4-(6-(2-((2S)-1-((2S)-2-((methoxycarbonyl)amino)-3-methylbutanoyl)pyrrolidin-2-yl)-3H-benzimidazol-5-yl)thieno(3,2-b)thiophen-3-yl)phenyl)-1H-imidazol-2-yl)pyrrolidin-1-yl)-2-oxo-1-phenylethyl)carbamate
CAS Number
  • 1312547-19-5
PubChem CID
  • 53302707
ChemSpider
  • 30843806
UNII
  • 21P699C5FC
KEGG
  • D10665 Y
CompTox Dashboard (EPA)
  • DTXSID70156982
Chemical and physical data
FormulaC47H48N8O6S2
Molar mass885.07 g·mol−1
3D model (JSmol)
  • Interactive image
  • CC(C)[C@@H](C(=O)N1CCC[C@H]1c2[nH]c3ccc(cc3n2)c4csc5c4scc5c6ccc(cc6)c7c[nH]c(n7)[C@@H]8CCCN8C(=O)[C@@H](c9ccccc9)NC(=O)OC)NC(=O)OC
  • InChI=1S/C47H48N8O6S2/c1-26(2)38(52-46(58)60-3)44(56)55-21-9-13-37(55)43-49-33-19-18-30(22-34(33)50-43)32-25-63-40-31(24-62-41(32)40)27-14-16-28(17-15-27)35-23-48-42(51-35)36-12-8-20-54(36)45(57)39(53-47(59)61-4)29-10-6-5-7-11-29/h5-7,10-11,14-19,22-26,36-39H,8-9,12-13,20-21H2,1-4H3,(H,48,51)(H,49,50)(H,52,58)(H,53,59)/t36-,37-,38-,39+/m0/s1
  • Key:ATOLIHZIXHZSBA-BTSKBWHGSA-N

Samatasvir is a highly potent and selective inhibitor of the hepatitis C virus NS5A replication complex.[2] While it showed promising results when administered as monotherapy, it is probable that samatasvir would be marketed as a combination product with other anti-hepatitis drugs to increase efficacy and reduce the chance of resistance developing, as with most other novel treatments for hepatitis C currently under development. Trials of samatasvir in combination with other antiviral drugs such as simeprevir are also underway.[3]

See also edit

References edit

  1. ^ Vince B, Hill JM, Lawitz EJ, O'Riordan W, Webster LR, Gruener DM, et al. (May 2014). "A randomized, double-blind, multiple-dose study of the pan-genotypic NS5A inhibitor samatasvir in patients infected with hepatitis C virus genotype 1, 2, 3 or 4". Journal of Hepatology. 60 (5): 920–7. doi:10.1016/j.jhep.2014.01.003. PMID 24434503.
  2. ^ Bilello JP, Lallos LB, McCarville JF, La Colla M, Serra I, Chapron C, et al. (August 2014). "In vitro activity and resistance profile of samatasvir, a novel NS5A replication inhibitor of hepatitis C virus". Antimicrobial Agents and Chemotherapy. 58 (8): 4431–42. doi:10.1128/AAC.02777-13. PMC 4136001. PMID 24867983.
  3. ^ Clinical trial number NCT01852604 for "Samatasvir (IDX719) in Combinations With Simeprevir and/or TMC647055/Ritonavir With or Without Ribavirin for 12 Weeks in Participants With Chronic Hepatitis C Infection (MK-1894-005)" at ClinicalTrials.gov

samatasvir, experimental, drug, treatment, hepatitis, originally, developed, idenix, development, been, continued, merck, following, their, acquisition, idenix, shown, good, results, phase, trials, clinical, dataroutes, ofadministrationorallegal, statuslegal, . Samatasvir IDX 719 is an experimental drug for the treatment of hepatitis C It was originally developed by Idenix and development has been continued by Merck amp Co following their acquisition of Idenix Samatasvir has shown good results in Phase II trials 1 SamatasvirClinical dataRoutes ofadministrationOralLegal statusLegal statusInvestigationalIdentifiersIUPAC name N 1R 2 2S 2 5 4 6 2 2S 1 2S 2 methoxycarbonyl amino 3 methylbutanoyl pyrrolidin 2 yl 3H benzimidazol 5 yl thieno 3 2 b thiophen 3 yl phenyl 1H imidazol 2 yl pyrrolidin 1 yl 2 oxo 1 phenylethyl carbamateCAS Number1312547 19 5PubChem CID53302707ChemSpider30843806UNII21P699C5FCKEGGD10665 YCompTox Dashboard EPA DTXSID70156982Chemical and physical dataFormulaC 47H 48N 8O 6S 2Molar mass885 07 g mol 13D model JSmol Interactive imageSMILES CC C C H C O N1CCC C H 1c2 nH c3ccc cc3n2 c4csc5c4scc5c6ccc cc6 c7c nH c n7 C H 8CCCN8C O C H c9ccccc9 NC O OC NC O OCInChI InChI 1S C47H48N8O6S2 c1 26 2 38 52 46 58 60 3 44 56 55 21 9 13 37 55 43 49 33 19 18 30 22 34 33 50 43 32 25 63 40 31 24 62 41 32 40 27 14 16 28 17 15 27 35 23 48 42 51 35 36 12 8 20 54 36 45 57 39 53 47 59 61 4 29 10 6 5 7 11 29 h5 7 10 11 14 19 22 26 36 39H 8 9 12 13 20 21H2 1 4H3 H 48 51 H 49 50 H 52 58 H 53 59 t36 37 38 39 m0 s1Key ATOLIHZIXHZSBA BTSKBWHGSA N Samatasvir is a highly potent and selective inhibitor of the hepatitis C virus NS5A replication complex 2 While it showed promising results when administered as monotherapy it is probable that samatasvir would be marketed as a combination product with other anti hepatitis drugs to increase efficacy and reduce the chance of resistance developing as with most other novel treatments for hepatitis C currently under development Trials of samatasvir in combination with other antiviral drugs such as simeprevir are also underway 3 See also editDiscovery and development of NS5A inhibitorsReferences edit Vince B Hill JM Lawitz EJ O Riordan W Webster LR Gruener DM et al May 2014 A randomized double blind multiple dose study of the pan genotypic NS5A inhibitor samatasvir in patients infected with hepatitis C virus genotype 1 2 3 or 4 Journal of Hepatology 60 5 920 7 doi 10 1016 j jhep 2014 01 003 PMID 24434503 Bilello JP Lallos LB McCarville JF La Colla M Serra I Chapron C et al August 2014 In vitro activity and resistance profile of samatasvir a novel NS5A replication inhibitor of hepatitis C virus Antimicrobial Agents and Chemotherapy 58 8 4431 42 doi 10 1128 AAC 02777 13 PMC 4136001 PMID 24867983 Clinical trial number NCT01852604 for Samatasvir IDX719 in Combinations With Simeprevir and or TMC647055 Ritonavir With or Without Ribavirin for 12 Weeks in Participants With Chronic Hepatitis C Infection MK 1894 005 at ClinicalTrials gov nbsp This antiinfective drug article is a stub You can help Wikipedia by expanding it vte Retrieved from https en wikipedia org w index php title Samatasvir amp oldid 1187851700, wikipedia, wiki, book, books, library,

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