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Ciluprevir (BILN 2061) is a small molecule, macrocyclic peptidomimetic inhibitor of the Hepatitis C Virus (HCV) NS3/4A serine protease. Developed by Boehringer Ingelheim, it was the first protease inhibitor to demonstrate potent antiviral activity in humans, showing a rapid and significant reduction in HCV RNA levels in patients with genotype 1 infection. Despite its initial promise as a first-in-class therapy, clinical development was terminated during Phase 2 trials after preclinical studies revealed evidence of myocardial toxicity in animal models, specifically dogs. It served as a critical proof-of-concept for the development of subsequent successful protease inhibitors like telaprevir and boceprevir.
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