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Clinical data | |
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Routes of administration | By mouth |
ATC code |
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Legal status | |
Legal status |
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Pharmacokinetic data | |
Protein binding | >99.1% [1] |
Identifiers | |
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CAS Number | |
PubChem CID | |
ChemSpider | |
UNII | |
ChEMBL | |
CompTox Dashboard ( EPA) | |
Chemical and physical data | |
Formula | C40H50N6O8S |
Molar mass | 774.93 g·mol−1 |
3D model ( JSmol) | |
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Ciluprevir was a drug used experimentally in the treatment of hepatitis C. It is manufactured by Boehringer Ingelheim and developed under the research code of BILN 2061. It was the first-in-class NS3/ 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]
![]() | |
Clinical data | |
---|---|
Routes of administration | By mouth |
ATC code |
|
Legal status | |
Legal status |
|
Pharmacokinetic data | |
Protein binding | >99.1% [1] |
Identifiers | |
| |
CAS Number | |
PubChem CID | |
ChemSpider | |
UNII | |
ChEMBL | |
CompTox Dashboard ( EPA) | |
Chemical and physical data | |
Formula | C40H50N6O8S |
Molar mass | 774.93 g·mol−1 |
3D model ( JSmol) | |
| |
|
Ciluprevir was a drug used experimentally in the treatment of hepatitis C. It is manufactured by Boehringer Ingelheim and developed under the research code of BILN 2061. It was the first-in-class NS3/ 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]