Samatasvir

Samatasvir
Systematic (IUPAC) 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)carbamate
Clinical data
Legal status	Investigational
Routes of administration	Oral
Identifiers
CAS Number	1312547-19-5
PubChem	CID 53302707
Chemical data
Formula	C₄₇H₄₈N₈O₆S₂
Molar mass	885.062 g/mol
SMILES c9ccccc9C(NC(=O)OC)C(=O)N3CCCC3c8[nH]cc(n8)-c7ccc(cc7)-c6csc1c(csc16)-c(ccc4n5)cc4[nH]c5C2CCCN2C(=O)C(C(C)C)NC(=O)OC

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 is a highly potent and selective inhibitor of the hepatitis C virus NS5a replication complex.^[2] While it showed promising results when administered as a monotherapy, it is most likely that samatasvir would be marketed as a combination product with other anti-hepatitis drugs to increase efficacy, as with most other novel treatments for Hepatitis C currently under development. Trials of samatasvir in combination with other antiviral drugs such as simeprevir and ritonavir are also underway.^[3]

References

↑ Vince B, Hill JM, Lawitz EJ, O'Riordan W, Webster LR, Gruener DM, Mofsen RS, Murillo A, Donovan E, Chen J, McCarville JF, Sullivan-Bólyai JZ, Mayers D, Zhou XJ. 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. 2014 May;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, Gillum JM, Pierra C, Standring DN, Seifer M. In vitro activity and resistance profile of samatasvir, a novel NS5A replication inhibitor of hepatitis C virus. Antimicrobobial Agents and Chemotherapy. 2014 Aug;58(8):4431-42. doi: 10.1128/AAC.02777-13. PMID 24867983
↑ 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)

RNA virus antivirals (primarily J05, also S01AD and D06BB)

Hepatitis C

NS3/4A protease inhibitors (–previr)	Asunaprevir Boceprevir Faldaprevir^‡ Grazoprevir Paritaprevir Simeprevir Telaprevir

NS5A inhibitors (–asvir)	Daclatasvir Elbasvir Ledipasvir MK-3682 MK-8408 Odalasvir^† Ombitasvir Ravidasvir^† Samatasvir^†

NS5B RNA polymerase inhibitors (–buvir)	Beclabuvir^† Dasabuvir Deleobuvir^§ Filibuvir^§ Setrobuvir^§ Sofosbuvir Radalbuvir^†

Combination drugs	Elbasvir/grazoprevir Ledipasvir/sofosbuvir Ombitasvir/paritaprevir/ritonavir

Picornavirus

viral entry: Pleconaril^†

Anti-influenza agents

Umifenovir

neuraminidase inhibitors/release phase (Oseltamivir
Zanamivir
Peramivir, Laninamivir^†)

Multiple/general

Interferon	Interferon alfa 2b Peginterferon alfa-2a^#

Multiple/unknown	BCX4430 Favipiravir Moroxydine Ribavirin^#/Taribavirin^† Triazavirin

^#WHO-EM
^‡Withdrawn from market
Clinical trials:
- ^†Phase III
- ^§Never to phase III

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