Les nouvelles molécules anti-VIH : la place du raltégravir

Principles: Integrase is an essential HIV-1-specific enzyme that is an active target for antiretroviral drug development. Integrase has at least two functions: firstly, it catalyses the 3′ processing at both ends of the retrotranscribed DNA, stabilizing the protein and allowing it to transpose to the nucleus and, secondly, it inhibits strand transfer integration into the human DNA. Without integration, there can be no viral replication in the host cell. Studies: Recently, a new class of drugs that specifically inhibits strand transfer has been developed. Two of these drugs are in late stage development: raltegravir, which has just been approved for use in treatment-experienced patients, and elvitegravir, currently in phase III trials. Raltegravir is dosed twice daily and has few drug-drug interactions since it is a drug metabolized through the UGTA1 pathway and not through the cytochrome P450 complex. Clinical studies: In both treatment-naive and experienced patients, trials have demonstrated raltegravir to be highly effective. One of the very specific features of its activity is a rapid antiviral efficacy within few weeks compared to standard therapies. Conclusion: Raltegravir has an excellent tolerability and can be combined easily to other new drugs.