Pharmacokinetic drug evaluation of ritonavir (versus cobicistat) as adjunctive therapy in the treatment of HIV

Expert Opin Drug Metab Toxicol. 2019 Nov;15(11):927-935. doi: 10.1080/17425255.2019.1685495. Epub 2019 Nov 3.

Abstract

Introduction: Ritonavir and cobicistat are pharmacoenhancers used to improve the disposition of other HIV antiretrovirals. These drugs are, however, characterized by important pharmacokinetic differences.Areas covered: Here, the authors firstly update the available information on the pharmacokinetics of ritonavir and cobicistat. Subsequently, the review focuses on the description of drug-drug interactions (DDIs) involving cobicistat and comedications that might beneficiate from a shift-back to ritonavir. A MEDLINE Pubmed search for articles published from January 1995 to April 2019 was completed matching the term ritonavir or cobicistat with pharmacokinetics, DDIs, and pharmacology. Moreover, additional studies were identified from the reference list of retrieved articles.Expert opinion: Despite more than 20 years after its introduction on the market, ritonavir still represents a valid option for the treatment of selected HIV-infected patients. The large-scale switch to cobicistat may result in some unexpected DDIs not previously reported for ritonavir. Besides the issue of DDIs, additional advantage of ritonavir over cobicistat is its use in pregnancy, and its availability as single component of pharmaceutical formulations allowing the fine-tuning of antiretroviral regimens in patients with heavy polypharmacy when other unboosted-based therapeutic options cannot be used.

Keywords: Drug-drug interactions; HIV; cobicistat; pharmacokinetics; polypharmacy; ritonavir.

Publication types

  • Comparative Study
  • Review

MeSH terms

  • Anti-HIV Agents / administration & dosage*
  • Anti-HIV Agents / pharmacokinetics
  • Cobicistat / administration & dosage*
  • Cobicistat / pharmacokinetics
  • Drug Interactions
  • Drug Therapy, Combination
  • HIV Infections / drug therapy
  • Humans
  • Ritonavir / administration & dosage*
  • Ritonavir / pharmacokinetics

Substances

  • Anti-HIV Agents
  • Cobicistat
  • Ritonavir