Development of darunavir over the entire spectrum of HIV infection.

Abstract

Darunavir is the gold standard protease inhibitor in antiretroviral treatment. It has undergone complete development through randomised clinical trials throughout the entire spectrum of HIV infection, with 2 different dosages and clear indications of when to use each one of them. It has been studied in mono, dual and triple therapy. It can also be administered boosted with either ritonavir or cobicistat. The data indicate that it is the antiretroviral with the greatest barrier against resistance development and that it is the drug with the longest residence time bound to its receptor (protease), thus having the longest dissociation time. Its limited impact on selected mutations in the protease by other inhibitors and its high barrier against resistance have resulted in its widespread commercial use being associated with a steady decrease in the mutations circulating in the protease having an impact on its activity. Supplement information: This article is part of a supplement entitled "Co-formulated cobicistat-boosted darunavir, emtricitabine, and tenofovir alafenamide for the treatment of HIV infection", which is sponsored by Janssen.

• Authors: Josep M Llibre
• Journal: Enfermedades infecciosas y microbiologia clinica (English ed.) (Enferm Infecc Microbiol Clin (Engl Ed)) Vol. 36 Suppl 2 Pg. 3-9 (Dec 2018) ISSN: 2529-993X [Electronic] Spain
• Vernacular Title: Desarrollo de darunavir en todo el espectro de la infección por el VIH.
• PMID: 30545469 (Publication Type: Journal Article, Review)
• Copyright: Copyright © 2018 Elsevier España, S.L.U. All rights reserved.

Chemical References

• HIV Protease Inhibitors
• Darunavir

Topics

• Darunavir (therapeutic use)
• Drug Resistance, Viral
• HIV Infections (drug therapy)
• HIV Protease Inhibitors (therapeutic use)
• Humans