Drug intelligence / Profile preview

ITMN-8187

Development stage
Discontinued
Lead developer
InterMune
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

ITMN-8187 is a research-stage, nonmacrocyclic small molecule inhibitor of the hepatitis C virus (HCV) NS3/4A protease, originally developed by InterMune. It was designed for the treatment of chronic hepatitis C infection by blocking the viral protease essential for polyprotein processing and viral replication. Preclinical studies demonstrated low nanomolar potency against NS3/4A protease derived from multiple HCV genotypes, including 1, 2b, 4, 5, and 6. Structurally, ITMN-8187 is distinct from macrocyclic inhibitors like simeprevir but exhibits a highly similar binding mode and resistance profile. The compound was evaluated in a Phase 1 microdosing crossover study in healthy adult volunteers to assess its pharmacokinetics after intravenous and oral administration, with results supporting a potential once-daily oral dosing schedule. However, the drug did not advance to late-stage clinical trials or regulatory approval.

02

Targets

NS3/4A (Hepatitis C virus nonstructural protein 3/4A serine protease)

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