Darunavir: an effective protease inhibitor for HIV-infected patients.

Darunavir is a new-generation nonpeptidic HIV protease inhibitor (PI), used with low doses of ritonavir for pharmacologic enhancement (boosting). It has demonstrated potent activity against multidrug-resistant HIV, with a robust resistance profile and a distinct set of mutations. In heavily treatment-experienced patients with HIV infection, darunavir administered twice daily with ritonavir has shown higher rates of efficacy than the control PI. In less treatment-experienced patients, boosted darunavir was noninferior to boosted lopinavir. In treatment-naive patients, boosted darunavir administered once daily was noninferior to boosted lopinavir, and showed higher virologic and immunological response rates in patients with high baseline viral load and low baseline CD4(+) cell counts. Monotherapy with boosted darunavir is an acceptable option in some specific conditions. Boosted darunavir was generally well tolerated, with lower incidence of diarrhea and a more favorable lipid profile than boosted lopinavir in treatment-naive patients.
AuthorsBao-Chau Phung, Patrick Yeni
JournalExpert review of anti-infective therapy (Expert Rev Anti Infect Ther) Vol. 9 Issue 6 Pg. 631-43 (Jun 2011) ISSN: 1744-8336 [Electronic] England
PMID21692667 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't, Review)
Chemical References
  • HIV Protease Inhibitors
  • RNA, Viral
  • Sulfonamides
  • Lopinavir
  • Ritonavir
  • Darunavir
  • Darunavir
  • Drug Administration Routes
  • Drug Administration Schedule
  • Drug Resistance, Viral (drug effects)
  • Drug Therapy, Combination (methods)
  • HIV Infections (drug therapy, immunology, virology)
  • HIV Protease Inhibitors (pharmacokinetics, therapeutic use)
  • HIV-1 (drug effects, physiology)
  • Humans
  • Lopinavir (adverse effects, pharmacokinetics, therapeutic use)
  • Multicenter Studies as Topic
  • RNA, Viral (analysis)
  • Randomized Controlled Trials as Topic
  • Ritonavir (adverse effects, pharmacokinetics, therapeutic use)
  • Sulfonamides (pharmacokinetics, therapeutic use)
  • Treatment Outcome
  • Viral Load (drug effects)
  • Virus Replication (drug effects)

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