RUZASVIR

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C49H55FN10O7S
Molecular Weight	947.087
Optical Activity	UNSPECIFIED
Defined Stereocenters	5 / 5
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

COC(=O)N[C@@H](C(C)C)C(=O)N1CCC[C@H]1C2=NC=C(N2)C3=CC4=C(C=C3)N5[C@@H](OC6=C(C5=C4)C(F)=CC(=C6)C7=CN=C(N7)[C@@H]8CCCN8C(=O)[C@@H](NC(=O)OC)C(C)C)C9=CN=C(S9)C%10CC%10

InChI

InChIKey=AXWDHVUJXNOWCC-RAEGKSCOSA-N

InChI=1S/C49H55FN10O7S/c1-24(2)40(56-48(63)65-5)45(61)58-15-7-9-34(58)42-51-21-31(54-42)27-13-14-33-29(17-27)19-36-39-30(50)18-28(20-37(39)67-47(60(33)36)38-23-53-44(68-38)26-11-12-26)32-22-52-43(55-32)35-10-8-16-59(35)46(62)41(25(3)4)57-49(64)66-6/h13-14,17-26,34-35,40-41,47H,7-12,15-16H2,1-6H3,(H,51,54)(H,52,55)(H,56,63)(H,57,64)/t34-,35-,40-,41-,47-/m0/s1

HIDE SMILES / InChI

Molecular Formula	C49H55FN10O7S
Molecular Weight	947.087
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	5 / 5
E/Z Centers	0
Optical Activity	UNSPECIFIED

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/31108015 | https://www.ncbi.nlm.nih.gov/pubmed/27808515

Ruzasvir (previously known as MK-8408) was developed as a nonstructural protein 5A (NS5A) inhibitor for the treatment of hepatitis C and hepatitis C infection. Ruzasvir successfully completed phase II clinical trial for combination therapy. The obtained results have shown that ruzasvir in combination with uprifosbuvir was highly effective and well-tolerated in participants infected with hepatitis C virus genotypes GT1, GT2, GT4, GT5, and GT6, with a lower efficacy in GT3-infected persons.

Originator

Approval Year

PubMed

Title	Date	PubMed
Grazoprevir, ruzasvir, and uprifosbuvir for hepatitis C virus after NS5A treatment failure.	2017 Dec	28688129
Safety and efficacy of an 8-week regimen of grazoprevir plus ruzasvir plus uprifosbuvir compared with grazoprevir plus elbasvir plus uprifosbuvir in participants without cirrhosis infected with hepatitis C virus genotypes 1, 2, or 3 (C-CREST-1 and C-CREST-2, part A): two randomised, phase 2, open-label trials.	2017 Nov	28802816
Efficacy and safety of ruzasvir 60 mg and uprifosbuvir 450 mg for 12 weeks in adults with chronic hepatitis C virus genotype 1, 2, 3, 4 or 6 infection.	2019 Jun	30739366
Efficacy and safety of a two-drug direct-acting antiviral agent regimen ruzasvir 180 mg and uprifosbuvir 450 mg for 12 weeks in adults with chronic hepatitis C virus genotype 1, 2, 3, 4, 5 or 6.	2019 Sep	31108015

Sample Use Guides

In Vivo Use Guide

All participants received ruzasvir 180 mg plus uprifosbuvir 450 mg once daily for 12 weeks

Route of Administration: Oral

Substance Class	Chemical Created by `admin` on `Sat Dec 16 09:51:31 UTC 2023` Edited by `admin` on `Sat Dec 16 09:51:31 UTC 2023`
Record UNII	LX752BD95Y
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

RUZASVIR

Official Name

English

ruzasvir [INN]

Common Name

English

CARBAMIC ACID, N,N'-(((6S)-6-(2-CYCLOPROPYL-5-THIAZOLYL)-1-FLUORO-6H-INDOLO(1,2-C)(1,3)BENZOXAZINE-3,10-DIYL)BIS(1H-IMIDAZOLE-5,2-DIYL-(2S)-2,1-PYRROLIDINEDIYL((1S)-1-(1-METHYLETHYL)-2-OXO-2,1-ETHANEDIYL)))BIS-, C,C'-DIMETHYL ESTER

Systematic Name

English

MK-8408

Code

English

Ruzasvir [WHO-DD]

Common Name

English

RUZASVIR [USAN]

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C281