title: [Not Available].
abstract: The human immunodeficiency virus (HIV) protease inhibitor saquinavir displays a large inter-individual variability in its pharmacokinetic parameters, related to a low absorption rate and an important hepatic metabolism. Based on literature, is the saquinavir therapeutic drug monitoring relevant? In naïve HIV-infected patients, the probability of achieving an undetectable HIV viral load at W48 was significantly associated with a saquinavir plasma trough concentration > 100 ng/mL. Two studies in HIV-infected pre-treated patients reported that the genotypic inhibitory quotient was a predictive factor of virologic response with a threshold value around 40 ng/mL/mutation. Concerning the exposure-toxicity relationship, the risk of occurrence of grade 3-4 abdominal pains was more frequently associated with high concentrations of saquinavir, but without threshold value determination. Several studies, one of which was randomized, have reported the interest of saquinavir therapeutic drug monitoring to optimize the virologic response. Therefore, the level of evidence of the interest of saquinavir therapeutic drug monitoring is "recommended".
authors.affiliation: UMR 645, IFR 133, Laboratoire de Pharmacologie Clinique et Toxicologie, CHU Minjoz, Besançon, France. Electronic address: patrice.muret@univ-fcomte.fr.
authors.forename: Patrice
authors.initials: P
authors.lastname: Muret
authors.affiliation: Laboratoire de Pharmacocinétique et Toxicologie, Hôpital de La Timone, Marseille, France.
authors.forename: Caroline
authors.initials: C
authors.lastname: Solas
keywords: level of evidence; niveau de preuve; saquinavir; suivi thérapeutique pharmacologique; therapeutic drug monitoring