Les antagonistes du récepteur CCR5 : une nouvelle classe d'antirétroviraux

A decade after identification of the chemokine receptor CCR5 as a coreceptor for human immunodeficiency virus (HIV), the first CCR5 antagonist has recently been approved by the European Medicines Evaluation Agency (EMEA) for treatment of HIV infected patients. Maraviroc (Celsentri®) is a small molecule that specifically inhibits CCR5 and thereby blocks HIV entry into its target cells. Viral tropism testing is mandatory before prescribing maraviroc, due to its unique mode of action limited to CCR5-tropic viruses. Maraviroc is administered orally, twice daily. Daily dose must be adapted in case of association with a cytochrome P450 inducer or inhibitor. Efficacy of maraviroc has been demonstrated in patients failing other antiretroviral classes. Its potential for first line or switch therapy has to be proven in future trials.