Ciluprevir
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Routes of administration | By mouth |
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Pharmacokinetic data | |
Protein binding | >99.1%[1] |
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Ciluprevir was a drug used experimentally in the treatment of
4A protease inhibitor to enter clinical development and tested in human.[2] Ciluprevir is a potent competitive reversible inhibitor of NS3/4A protease from HCV genotype 1a (Ki = 0.3 nM) and 1b (Ki = 0.66 nM). It shows good selectivity for NS3 protease against representative serine and cysteine proteases, human leukocyte elastase and cathepsin B (IC50 > 30 μM).[1]
Its development was halted in phase Ib clinical trials because of toxicity in animals. However, ciluprevir scaffold was exploited to design new macrocyclic inhibitors such as simeprevir (TMC-435) and danoprevir.[3]
References
- ^ ISBN 978-1-904455-78-3.
- PMID 21250377.
- PMID 21994705.