Genetic polymorphisms of ABCB1 (P-glycoprotein) as a covariate influencing daptomycin pharmacokinetics: a population analysis in patients with bone and joint infection

J Antimicrob Chemother. 2019 Apr 1;74(4):1012-1020. doi: 10.1093/jac/dky541.

Abstract

Background: Daptomycin has been recognized as a therapeutic option for the treatment of bone and joint infection (BJI). Gene polymorphism of ABCB1, the gene encoding P-glycoprotein (P-gp), may influence daptomycin pharmacokinetics (PK).

Objectives: We aimed to examine population PK of daptomycin and its determinants, including genetic factors, in patients with BJI.

Patients and methods: We analysed data from patients who received daptomycin for BJI between 2012 and 2016 in our regional reference centre and who had measured daptomycin concentrations and P-gp genotyping. A population approach was used to analyse PK data. In covariate analysis, we examined the influence of three single nucleotide variations (SNVs) of ABCB1 (3435C > T, 2677G > T/A and 1236C > T) and that of the corresponding haplotype on daptomycin PK parameters. Simulations performed with the final model examined the influence of covariates on the probability to achieve pharmacodynamic (PD) targets.

Results: Data from 81 patients were analysed. Daptomycin body CL (CLDAP) correlated with CLCR and was 23% greater in males than in females. Daptomycin central V (V1) was allometrically scaled to body weight and was 25% lower in patients with homozygous CGC ABCB1 haplotype than in patients with any other genotype. Simulations performed with the model showed that sex and P-gp haplotype may influence the PTA for high MIC values and that a dosage of 10 mg/kg/24 h would optimize efficacy.

Conclusions: Daptomycin dosages higher than currently recommended should be evaluated in patients with BJI. Gender and P-gp gene polymorphism should be further examined as determinants of dosage requirements.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • ATP Binding Cassette Transporter, Subfamily B / genetics
  • Aged
  • Alleles
  • Anti-Bacterial Agents / pharmacokinetics*
  • Area Under Curve
  • Arthritis, Infectious / drug therapy
  • Arthritis, Infectious / epidemiology
  • Arthritis, Infectious / genetics
  • Bone Diseases, Infectious / drug therapy
  • Bone Diseases, Infectious / epidemiology
  • Bone Diseases, Infectious / genetics
  • Daptomycin / pharmacokinetics*
  • Drug Monitoring
  • Female
  • Genotype
  • Glomerular Filtration Rate
  • Humans
  • Male
  • Middle Aged
  • Pharmacogenetics / methods
  • Pharmacogenomic Variants*
  • Polymorphism, Single Nucleotide*
  • Population Surveillance

Substances

  • ABCB1 protein, human
  • ATP Binding Cassette Transporter, Subfamily B
  • Anti-Bacterial Agents
  • Daptomycin