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[Not Available].

Patrice Muret1, Caroline Solas2,

  • 1UMR 645, IFR 133, Laboratoire de Pharmacologie Clinique et Toxicologie, CHU Minjoz, Besançon, France.

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Summary
This summary is machine-generated.

Therapeutic drug monitoring of saquinavir is recommended for HIV patients. Maintaining saquinavir plasma trough concentrations above 100 ng/mL is linked to achieving undetectable HIV viral load.

Keywords:
level of evidenceniveau de preuvesaquinavirsuivi thérapeutique pharmacologiquetherapeutic drug monitoring

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Area of Science:

  • Pharmacology
  • Infectious Diseases
  • Clinical Pharmacy

Context:

  • Saquinavir, an HIV protease inhibitor, exhibits significant inter-individual pharmacokinetic variability.
  • This variability stems from low absorption and extensive hepatic metabolism.
  • Understanding these factors is crucial for optimizing treatment efficacy.

Purpose:

  • To evaluate the relevance and evidence level of therapeutic drug monitoring (TDM) for saquinavir in HIV-infected patients.
  • To determine optimal saquinavir plasma concentrations for virologic response and assess exposure-toxicity relationships.

Summary:

  • In treatment-naïve patients, undetectable HIV viral load at 48 weeks was associated with saquinavir trough concentrations > 100 ng/mL.
  • In pre-treated patients, genotypic inhibitory quotient predicted virologic response with a threshold around 40 ng/mL/mutation.
  • High saquinavir concentrations were linked to increased risk of severe abdominal pain, though no specific threshold was identified.

Impact:

  • Saquinavir TDM is recommended to optimize virologic response in HIV management.
  • Evidence from multiple studies, including a randomized trial, supports the utility of saquinavir TDM.
  • This monitoring can aid clinicians in personalizing saquinavir dosing for improved patient outcomes.