ciluprevir
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. 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). — Wikipedia
Clinical trial activity
3 trials · 1 clinical orgs · 0 marketing orgs
Earliest trial started Jun 1, 2001 (NCT02268760)
Timeline
Indications
Mechanism of action
- Hepatitis C virusINHIBITOR
Hepatitis C virus inhibitor
Hepatitis C virus serine protease, NS3/NS4A inhibitor
Chemistry & pharmacology
SMILES
COc1ccc2c(O[C@@H]3C[C@H]4C(=O)N[C@]5(C(=O)O)C[C@H]5/C=C\CCCCC[C@H](NC(=O)OC5CCCC5)C(=O)N4C3)cc(-c3csc(NC(C)C)n3)nc2c1- Mol. weight
- 774.94 g/mol
- Lipinski Ro5
- 3 violation(s)
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- WikipediaCiluprevir ↗
- ChEMBLCHEMBL297884 ↗
Also known as
- biln2061
- biln 2061
- biln 2061
- biln 2061
- biln-2061
- biln-2061
- biln-2061
- biln-2061-zw
- biln-2061-zw
- ciluprevir
- ciluprevir
- ciluprevir
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT02226939 | Phase 2 | Sep 1, 2002 | Boehringer Ingelheim |
| NCT02226952 | Phase 1/Phase 2 (Phase 2) | Nov 1, 2001 | Boehringer Ingelheim |
| NCT02268760 | Phase 1 | Jun 1, 2001 | Boehringer Ingelheim |
Organizations
Research & Development (1)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Boehringer Ingelheim | For profit | 3 | 3 | 2 | 2001 |