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Genomic and Sex Contributions to Interindividual Variability in Pitavastatin Bioavailability
Eva González-Iglesias1,2, Sofía Moreno-Pérez de Villar1, Dolores Ochoa1,2
1Clinical Pharmacology Department, Hospital Universitario de La Princesa, Instituto de Investigación Sanitaria La Princesa (IIS-Princesa), Madrid, Spain.
Basic & Clinical Pharmacology & Toxicology
|May 29, 2026
Summary
Genetic factors significantly influence how the body processes pitavastatin. The SLCO1B1 gene variant is a major determinant of pitavastatin pharmacokinetics, impacting drug exposure in individuals.
Area of Science:
- Pharmacogenetics
- Drug Metabolism and Transport
Background:
- Understanding individual variability in drug response is crucial for personalized medicine.
- Pitavastatin pharmacokinetics can be influenced by genetic factors and demographic variables.
Purpose of the Study:
- To investigate pharmacogenetic determinants of pitavastatin disposition.
- To assess the relationship between genetic variants and pitavastatin pharmacokinetics.
Main Methods:
- A candidate-gene approach was used in 48 healthy volunteers.
- 138 variants across 40 genes involved in drug metabolism and transport were analyzed.
- The influence of sex and biogeographical origin was also considered.
Main Results:
- SLCO1B1 phenotype significantly impacted pitavastatin exposure (50%-65% increase in AUC/DW and Cmax/DW in decreased function individuals).
- Sex differences in pitavastatin disposition were observed but diminished after dose/weight adjustment.
- Variants in ABCB1, ABCC3, and ABCG2 may contribute to variability; CYP4F2 (rs3093200) warrants further investigation.
Conclusions:
- Genetic factors, particularly SLCO1B1 variants, play a significant role in pitavastatin disposition.
- Further functional studies or larger cohorts are needed to confirm these findings.
- This research contributes to understanding interindividual variability in pitavastatin pharmacokinetics.
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