Pharmacokinetics of gemcitabine in non-small-cell lung cancer patients: impact of the 79A>C cytidine deaminase polymorphism

Eur J Clin Pharmacol. 2010 Jun;66(6):611-7. doi: 10.1007/s00228-010-0799-0. Epub 2010 Mar 6.

Abstract

Objective: To study the impact of the 79A>C polymorphism in the cytidine deaminase (CDA) gene on the pharmacokinetics of gemcitabine and its metabolite 2',2'-difluorodeoxyuridine (dFdU) in non-small-cell lung cancer (NSCLC) patients.

Patients and methods: Patients (n = 20) received gemcitabine 1,125 mg/m(2) as a 30 min i.v. infusion as part of treatment for NSCLC. Plasma samples were collected during 0-6 h after gemcitabine administration. Gemcitabine and dFdU were quantified by high performance liquid chromatography with ultraviolet detection. The CDA 79A>C genotype was determined with PCR and DNA sequencing.

Results: Gemcitabine was rapidly cleared from plasma and undetectable after 3 h. The allele frequency of the 79A>C polymorphism was 0.40. Diplotypes were distributed as A/A n = 8, A/C n = 8 ,and C/C n = 4. No significant differences were found between the different CDA genotypes and gemcitabine or dFdU AUC, clearance, or half-life.

Conclusion: The 79A>C polymorphism in the CDA gene does not have a major consistent and signficant impact on gemcitabine pharmacokinetics.

Publication types

  • Clinical Trial, Phase III

MeSH terms

  • Adult
  • Aged
  • Antimetabolites, Antineoplastic / administration & dosage
  • Antimetabolites, Antineoplastic / pharmacokinetics*
  • Antineoplastic Combined Chemotherapy Protocols / therapeutic use
  • Carcinoma, Non-Small-Cell Lung / blood*
  • Carcinoma, Non-Small-Cell Lung / drug therapy
  • Cytidine Deaminase / genetics*
  • Deoxycytidine / administration & dosage
  • Deoxycytidine / analogs & derivatives*
  • Deoxycytidine / pharmacokinetics
  • Female
  • Floxuridine / analogs & derivatives
  • Floxuridine / pharmacokinetics
  • Gemcitabine
  • Gene Frequency
  • Genotype
  • Humans
  • Lung Neoplasms / blood*
  • Lung Neoplasms / drug therapy
  • Male
  • Metabolic Clearance Rate
  • Middle Aged
  • Polymorphism, Single Nucleotide*

Substances

  • Antimetabolites, Antineoplastic
  • Floxuridine
  • Deoxycytidine
  • Cytidine Deaminase
  • 2',2'-difluoro-2'-deoxyuridine
  • Gemcitabine