Despite the known benefits and the experienced use of lopinavir/ritonavir (LPV/r) in the management of HIV infection, important
interindividual variability in the pharmacokinetics (PKs) and the response to treatment with standard doses of this drug has been observed.
Host genetic factors have been recently suggested as being responsible for part of this variability as they may affect the expression
and functional activity of many proteins involved in the kinetic behavior, the immune recovery or the adverse effects related to
Here, we present a genetic association study in 106 HIV-infected individuals collected over a period of 5 years with the aim of identifying
and confirming single nucleotide polymorphisms (SNPs) with a significant influence on the PK parameters of LPV/r, the immunovirological
response or toxicity derived from treatment with the studied drug. Genotyping was performed by MALDI-TOF and KASPar;
LPV/r plasma concentrations were quantified using high-performance liquid chromatography with an ultraviolet detection system and the
PK parameters were estimated using Bayesian algorithms. Genetic association analysis was performed with SPSS.
The most significant associations were found between SNPs in the dopamine receptor D3 gene and the PK of LPV/r. Additionally, other
suggestive relationships were established between genetic factors and the response during treatment with this drug. Thereby, identifying
HIV-infected individuals who are at increased risk of achieve non-optimal LPV/r plasma concentrations with the emergence of toxicity,
drug resistance or absence of clinical response could be helpful as a tool to optimize the LPV/r-based antiretroviral therapy.