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telaprevir + darunavir + ritonavir + fosamprenavir (Tibotec)
- Development stage
- Unknown
- Lead developer
- Johnson & Johnson
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
This entry refers to a combination of four antiviral drugs—telaprevir, darunavir, ritonavir, and fosamprenavir—that was investigated in a Phase I clinical trial (NCT00775125) to evaluate pharmacokinetic (PK) interactions. Telaprevir is a small molecule inhibitor of the Hepatitis C virus (HCV) NS3/4A serine protease. Darunavir and fosamprenavir are HIV-1 protease inhibitors, while ritonavir is used as a pharmacokinetic enhancer (booster) due to its potent inhibition of the CYP3A4 enzyme. The study, sponsored by Tibotec (a subsidiary of Johnson & Johnson), aimed to determine the safety and PK profiles when telaprevir was co-administered with ritonavir-boosted darunavir or fosamprenavir in healthy subjects. This research was critical for managing HIV/HCV co-infected patients, as all four drugs are metabolized by the cytochrome P450 system, leading to significant drug-drug interactions that can reduce the efficacy of both the HCV and HIV treatment regimens.
- Brand names
- IncivekIncivoPrezistaNorvirLexivaTelzir
- Other names
- telaprevir; darunavir; ritonavir; fosamprenavir
02
Targets
NS3/4A (Hepatitis C virus nonstructural protein 3/4A serine protease)CYP3A4 (Cytochrome P450 3A4)PR (Progesterone receptor)
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