Darunavir: A comprehensive profile

Profiles Drug Subst Excip Relat Methodol. 2021:46:1-50. doi: 10.1016/bs.podrm.2020.07.001. Epub 2020 Aug 21.

Abstract

Darunavir: (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl [(2S,3R)-4-{[(4-aminophenyl)sulfonyl] (isobutyl)amino}-3-hydroxy-1-phenyl-2-butanyl]carbamate is a synthetic non-peptide protease inhibitor. On June 2006, it was first approved by the Food and Drug administration (FDA) for treatment of resistant type-1 of the human immunodeficiency virus (HIV). In July 2016, the FDA expanded the approval for use of darunavir in pregnant women with HIV infection. Darunavir prevents the replication of HIV virus by inhibiting the catalytic activity of the HIV-1 protease enzyme, and selectively inhibits the cleavage of HIV encoded Gag-Pol polyproteins in virus-infected cells, which prevents the formation of mature infectious virus particles. Darunavir is unique among currently available protease inhibitors because it maintains antiretroviral activity against a variety of multidrug-resistant HIV strains. This article discusses, by a critical extensive review of the literature, the description of darunavir in terms of its names, formulae, elemental composition, appearance, and use in the treatment of HIV-infected patients. The article also discusses the methods for preparation of darunavir, its physical-chemical properties, analytical methods for its determination, pharmacological properties, and dosing information.

Keywords: Chromatographic analysis; Darunavir; Dosing information; Enzyme-linked immunosorbent assay; Human immunodeficiency virus; Methods of preparation; Pharmacological properties; Physical-chemical properties; Spectrometric analysis.

Publication types

  • Review

MeSH terms

  • Darunavir* / pharmacology
  • Darunavir* / therapeutic use
  • Drug Resistance, Viral
  • Female
  • HIV Infections* / drug therapy
  • HIV Protease Inhibitors* / pharmacology
  • HIV Protease Inhibitors* / therapeutic use
  • HIV-1* / drug effects
  • Humans
  • Pregnancy
  • United States

Substances

  • HIV Protease Inhibitors
  • Darunavir