filibuvir
Filibuvir was a non-nucleoside orally available NS5B inhibitor developed by Pfizer for the treatment of hepatitis C. It binds to the non-catalytic Thumb II allosteric pocket of NS5B viral polymerase and causes a decrease in viral RNA synthesis. It is a potent and selective inhibitor, with a mean IC50 of 0.019 μM against genotype 1 polymerases. Several filibuvir-resistant mutations have been identified, M423 being the most common that occurred after filibuvir monotherapy. It was intended to be taken twice-daily. — Wikipedia
Clinical trial activity
9 trials · 1 clinical orgs · 0 marketing orgs
Earliest trial started Jan 1, 2007 (NCT00445315)
Timeline
Indications
Mechanism of action
- NS5B proteinINHIBITOR
NS5B inhibitor
- RNA-directed RNA polymeraseINHIBITOR
RNA-directed RNA polymerase inhibitor
Hepatitis C virus NS5B RNA-dependent RNA polymerase inhibitor
Chemistry & pharmacology
SMILES
CCc1cc(CC[C@]2(C3CCCC3)CC(O)=C(Cc3nc4nc(C)cc(C)n4n3)C(=O)O2)cc(CC)n1- Mol. weight
- 503.65 g/mol
- Lipinski Ro5
- 2 violation(s)
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- WikipediaFilibuvir ↗
- ChEMBLCHEMBL490672 ↗
Also known as
- 6-cyclopentyl-6-(2-(2,6-diethylpyridin-4-yl)ethyl)-3-((5,7-dimethyl-(1,2,4)triazolo(1,5-a)pyrimidin-2-yl)methyl)-4-hydroxy-5,6-dihydropyran-2-one
- filibuvir
- filibuvir
- filibuvir
- filibuvir
- filibuvir
- pf00868554
- pf 00868554
- pf-00868554
- pf-00868554
- pf-00868554
- pf-00868554
- pf868554
- pf 868554
- pf-868554
- pf-868554
- pf-868554
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT01210404 | Phase 1 | Feb 1, 2011 | Pfizer |
| NCT00918476 | Phase 1 | Jun 1, 2010 | Pfizer |
| NCT00987337 | Phase 2 | Nov 1, 2009 | Pfizer |
| NCT00875628 | Phase 1 | Apr 1, 2009 | Pfizer |
| NCT00823745 | Phase 1 | Jan 1, 2009 | Pfizer |
| NCT00720434 | Phase 2 | Aug 1, 2008 | Pfizer |
| NCT00671671 | Phase 1 | Apr 1, 2008 | Pfizer |
| NCT00651027 | Phase 1 | Feb 1, 2008 | Pfizer |
| NCT00445315 | Phase 1 | Jan 1, 2007 | Pfizer |
Organizations
Research & Development (1)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Pfizer | For profit | 9 | 9 | 2 | 2007 |