DANOPREVIR (ITMN-191) …..a peptidomimetic inhibitor of the NS3/4A protease of hepatitis C virus (HCV)

New Drug Approvals

Danoprevir (ITMN-191) Chemical Structure

Danoprevir

Danoprevir(ITMN-191) is a peptidomimetic inhibitor of the NS3/4A protease of hepatitis C virus (HCV) with IC50 of 0.2-3.5 nM, inhibition effect for HCV genotypes 1A/1B/4/5/6 is ~10-fold higher than 2B/3A. Phase 2.

Array BioPharma (Originator)

RG7227
ITMN-191
RO5190591

2H-Isoindole-2-carboxylic acid, 4-fluoro-1,3-dihydro-, (2R,6S,12Z,13aS,14aR,16aS)-
14a-[[(cyclopropylsulfonyl)amino]carbonyl]-6-[[(1,1-dimethylethoxy)carbonyl]amino]-
1,2,3,5,6,7,8,9,10,11,13a,14,14a,15,16,16a-hexadecahydro-5,16-
dioxocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecin-2-yl ester

2. (2R,6S,12Z,13aS,14aR,16aS)-14a-[(cyclopropylsulfonyl)carbamoyl]-6-{[(1,1-
dimethylethoxy)carbonyl]amino}-5,16-dioxo-
1,2,3,5,6,7,8,9,10,11,13a,14,14a,15,16,16a-hexadecahydrocyclopropa[e]pyrrolo[1,2-
a][1,4]diazacyclopentadecin-2-yl 4-fluoro-1,3-dihydro-2H-isoindole-2-carboxylate
Treatment of hepatitis C

MOLECULAR FORMULA C35H46FN5O9S

MOLECULAR WEIGHT 731.8

MANUFACTURER Genentech

CODE DESIGNATION R05190591

CAS REGISTRY NUMBER 850876-88-9, 916881-67-9

Danoprevir(ITMN-191) is a peptidomimetic

ITMN-191 (R-7227), a macrocyclic protease inhibitor, is in phase II clinical evaluation for the treatment of chronic hepatitis C virus (HCV) infection as monotherapy and in combination with Pegasys(R) (pegylated interferon alpha-2a) and Copegus(R) (ribavirin). The product candidate is also being evaluated in combination with R-7128 in treatment-naive patients infected with HCV genotype 1.

Danoprevir (ITMN-191; RG-7227), under development by InterMune Inc and Roche Holding AG, is a promising, potent NS3/4A protease inhibitor for…

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About luciavazine

PHARMA PROFESSIONAL, ITALY
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