Drug intelligence / Profile preview

simeprevir + peginterferon alfa-2b + ribavirin

Development stage
Unknown
Lead developer
Janssen Pharmaceutical
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Recombinant Proteins and Enzymes, DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules
Administration
Oral (simeprevir, Ribavirin), Subcutaneous (peginterferon Alfa-2b)
01

Overview

This combination drug regimen consists of three agents used together for the treatment of chronic hepatitis C virus (HCV) infection, specifically genotype 1 and sometimes genotype 4, in adults with compensated liver disease (including cirrhosis). The regimen includes: - **Simeprevir (formerly TMC435, brand name Olysio)**, an oral, once-daily, second-generation HCV NS3/4A serine protease inhibitor. Simeprevir blocks viral replication by inhibiting the protease that processes viral polyprotein precursors, thus preventing the formation of mature viral proteins and suppressing virus production[1][2][3][7][8]. - **Peginterferon alfa-2b**, a pegylated interferon, is an immunomodulatory and antiviral cytokine that activates intracellular signaling cascades, leading to an antiviral state and enhanced immune clearance of HCV-infected cells. - **Ribavirin**, a nucleoside analog, enhances the antiviral activity of interferons and direct-acting antivirals through multiple mechanisms, including inhibition of viral RNA synthesis and modulation of immune responses. The triple regimen has been shown in Phase 2/3 clinical trials to result in higher sustained virological response (SVR) rates in both treatment-naïve and treatment-experienced chronically infected HCV adult patients, including subpopulations with advanced liver disease. Simeprevir is generally well tolerated, but resistance can occur, particularly in patients with certain HCV polymorphisms (such as Q80K in genotype 1a)[1][2][3][8].

Brand names
Olysio
Other names
simeprevir + peginterferon alfa-2b + ribavirin
02

Targets

OATP1B1 (Organic anion transporting polypeptide 1B1)MRP2 (Canalicular multispecific organic anion transporter 1)ABCB1 (P-glycoprotein)NS5B (Hepatitis C virus non-structural protein 5B (NS5B) RNA-dependent RNA polymerase)SLCO1B3 (Organic anion transporting polypeptide 1B3)IFNAR (Immune system modulation via type I interferon receptor)NS3/4A (Hepatitis C virus nonstructural protein 3/4A serine protease)

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