Darunavir/cobicistat for the treatment of HIV-1: a new era for compact drugs with high genetic barrier to resistance

Abstract

Introduction: Cobicistat-boosted darunavir is a boosted protease inhibitor in a fixed-dose combination to be approved for the treatment of human immunodeficiency virus type1 infection. It contains darunavir, a well-known protease inhibitor with a good efficacy and safety profile, and the new pharmacokinetic enhancer cobicistat. The convenience of this combination in a single pill makes this compound easier to take, thus improving adherence.

Areas covered: PubMed and www.clinicaltrials.gov were searched with the term "darunavir/cobicistat" for all clinical trials conducted up to date, as well as for those ongoing and to be opened in the near future as well as for pharmacology data. A review of abstracts from major infectious diseases (particularly those dedicated to human immunodeficiency disease) and pharmacology conferences from 2010 to 2015 was also conducted.

Expert opinion: improving adherence, particularly by minimizing pill burden with convenient formulations (i.e., fixed-dose combination), is one of the major objectives of modern antiretroviral treatment of patients with human immunodeficiency virus disease. Cobicistat is an alternative agent to ritonavir for boosting plasma drug levels for several antiretrovirals. Darunavir co-administered with low-dose ritonavir, in combination with other antiretrovirals, is recommended in several guidelines for treatment of patients with human immunodeficiency disease. Darunavir/cobicistat fixed-dose combination allows for a once-daily treatment regimen with a reduced pill burden. This new co formulation makes this compound easier to take, thus improving adherence.

Keywords: HIV; cobicistat; darunavir; drug–drug interactions; efficacy; fixed-dose combination; pharmacokinetics; safety.