NS3/4A Protease Inhibitors

Inhibitors of the NS3/4A serine protease of Hepatitis C Virus (HCV).
DrugDrug NameDrug Indication
DB05521TelaprevirTelaprevir, when used in combination with [DB00811], [DB00008], and [DB00022] is indicated for use in the treatment of chronic HCV genotype 1 infection in adults [FDA Label].
DB08873BoceprevirBoceprevir, when used in combination with [DB00811], [DB00008], and [DB00022] is indicated for use in the treatment of chronic HCV genotype 1 infection in adults [FDA Label].
DB11575GrazoprevirGrazoprevir is indicated in combination with [DB11574] (as the fixed dose combination product Zepatier) with or without [DB00811] for treatment of chronic HCV genotypes 1a, 1b, or 4 infection in adults.
DB06290SimeprevirIndicated for the treatment of adults with chronic hepatitis C virus (HCV) infection: typically in combination with sofosbuvir in patients with HCV genotype 1 without cirrhosis or with compensated cirrhosis and in combination with peginterferon alfa (Peg-IFN-alfa) and ribavirin (RBV) in patients with HCV genotype 1 or 4 without cirrhosis or with compensated cirrhosis. Resistance: Reduced susceptibility to simeprevir was most commonly associated with the viral NS3 Q80K polymorphism. Amino acid substitutions at NS3 positions S122, R155 and/or D168 are also shown to reduce susceptibility to simeprevir in genotype 1a/b patients.
DB09297ParitaprevirWhen used within the fixed-dose combination product with [DB09296], [DB09183], and [DB00503] as the FDA-approved product Viekira Pak, paritaprevir is indicated for the treatment of HCV genotype 1b without cirrhosis or with compensated cirrhosis, and when combined with [DB00811] for the treatment of HCV genotype 1a without cirrhosis or with compensated cirrhosis. When used within the fixed-dose combination product with [DB09296] and [DB00503] as the FDA- and Health Canada-approved product Technivie, paritaprevir is indicated in combination with [DB00811] for the treatment of patients with genotype 4 chronic hepatitis C virus (HCV) infection without cirrhosis or with compensated cirrhosis. When used within the fixed-dose combination product with [DB09296], [DB09183], and [DB00503] as the Health Canada-approved, commercially available product Holkira Pak, paritaprevir is indicated for the treatment of HCV genotype 1b with or without cirrhosis, and when combined with [DB00811] for the treatment of HCV genotype 1a with or without cirrhosis.
DB12026VoxilaprevirVosevi (Voxilaprevir/[DB08934]/[DB11613]) is approved for use in patients with genotypes 1-6 who have been previously treated with an NS5A inhibitor, or patients with genotypes 1a or 3 infection who have previously been treated with an HCV regimen containing [DB08934] without an NS5A inhibitor [L935].
DB13879GlecaprevirIndicated for the treatment of adult patients with chronic hepatitis C virus (HCV) genotype 1, 2, 3, 4, 5 or 6 infection without cirrhosis or with compensated cirrhosis (Child-Pugh A). MAVYRET is also indicated for the treatment of adult patients with HCV genotype 1 infection, who previously have been treated with a regimen containing an HCV NS5A inhibitor or an NS3/4A protease inhibitor (PI), but not both [FDA Label].
DrugDrug NameTargetType
DB05521TelaprevirSerum albumincarrier
DB05521TelaprevirAlpha-1-acid glycoprotein 1carrier
DB05521TelaprevirCytochrome P450 3A4enzyme
DB05521TelaprevirCytochrome P450 3A5enzyme
DB05521TelaprevirNS3/4A proteintarget
DB05521TelaprevirSolute carrier organic anion transporter family member 1B1target
DB05521TelaprevirSolute carrier organic anion transporter family member 2B1target
DB05521TelaprevirMultidrug resistance protein 1transporter
DB08873BoceprevirCytochrome P450 3A4enzyme
DB08873BoceprevirCytochrome P450 3A5enzyme
DB08873BoceprevirNS3/4A proteintarget
DB08873BoceprevirMultidrug resistance protein 1transporter
DB11575GrazoprevirSerum albumincarrier
DB11575GrazoprevirAlpha-1-acid glycoprotein 1carrier
DB11575GrazoprevirCytochrome P450 3A4enzyme
DB11575GrazoprevirNS3/4A proteintarget
DB11575GrazoprevirMultidrug resistance protein 1transporter
DB11575GrazoprevirSolute carrier organic anion transporter family member 1B1transporter
DB11575GrazoprevirSolute carrier organic anion transporter family member 1B3transporter
DB06290SimeprevirSerum albumincarrier
DB06290SimeprevirCytochrome P450 1A2enzyme
DB06290SimeprevirCytochrome P450 3A4enzyme
DB06290SimeprevirNS3 proteasetarget
DB06290SimeprevirMultidrug resistance protein 1transporter
DB06290SimeprevirSolute carrier organic anion transporter family member 1B1transporter
DB06290SimeprevirSolute carrier organic anion transporter family member 1B3transporter
DB06290SimeprevirCanalicular multispecific organic anion transporter 1transporter
DB06290SimeprevirATP-binding cassette sub-family G member 2transporter
DB06290SimeprevirSolute carrier organic anion transporter family member 2B1transporter
DB06290SimeprevirSodium/bile acid cotransportertransporter
DB06290SimeprevirBile salt export pumptransporter
DB09297ParitaprevirCytochrome P450 3A4enzyme
DB09297ParitaprevirCytochrome P450 3A5enzyme
DB09297ParitaprevirNS3/4A proteintarget
DB09297ParitaprevirATP-binding cassette sub-family G member 2transporter
DB09297ParitaprevirMultidrug resistance protein 1transporter
DB09297ParitaprevirSolute carrier organic anion transporter family member 1B1transporter
DB09297ParitaprevirSolute carrier organic anion transporter family member 1B3transporter
DB12026VoxilaprevirCytochrome P450 3A4enzyme
DB12026VoxilaprevirCytochrome P450 1A2enzyme
DB12026VoxilaprevirCytochrome P450 2C8enzyme
DB12026VoxilaprevirNS3/4A proteintarget
DB12026VoxilaprevirMultidrug resistance protein 1transporter
DB12026VoxilaprevirATP-binding cassette sub-family G member 2transporter
DB12026VoxilaprevirSolute carrier organic anion transporter family member 1B1transporter
DB12026VoxilaprevirSolute carrier organic anion transporter family member 1B3transporter
DB13879GlecaprevirCYP3Aenzyme
DB13879GlecaprevirUDP-glucuronosyltransferase 1-1enzyme
DB13879GlecaprevirNS3 proteasetarget
DB13879GlecaprevirMultidrug resistance protein 1transporter
DB13879GlecaprevirATP-binding cassette sub-family G member 2transporter
DB13879GlecaprevirSolute carrier organic anion transporter family member 1B1transporter
DB13879GlecaprevirSolute carrier organic anion transporter family member 1B3transporter