Genetic variations of hOCT1 gene and CYP3A4/A5 genes and their association with imatinib response in Chronic Myeloid Leukemia

Eur J Pharmacol. 2015 Oct 15:765:124-30. doi: 10.1016/j.ejphar.2015.08.034. Epub 2015 Aug 21.

Abstract

There is an increasing body of evidence demonstrating that mechanisms independent of BCR/ABL gene also contribute to imatinib resistance in Chronic Myeloid Leukemia (CML). It has been extensively reported that polymorphisms of the genes associated with imatinib metabolization and imatinib influx/efflux play an important role in the disease resistance. We investigated the impact of 12 genetic variants of the two genes, CYP3A4/A5 and the human cation transporter 1 gene (hOCT1) on the clinical outcome, in a cohort of 106 newly diagnosed CML patients. In the patient cohort investigated, only 6 variant alleles could be detected. The others were not present and could not be investigated. Two polymorphisms, CYP3A5*3 (rs776746)and hOCT1 M408V (rs628031), were significantly associated with the Complete Cytogenetic Response (CCyR) at 6 months and Major Molecular Response (MMR) at 12 months. The presence of favourable alleles at M408V and M420del in combination was associated with a MMR at 12 months. Functional polymorphisms of the genes associated with imatinib influx and metabolization may play a role in predicting primary response to imatinib and treatment outcome.

Keywords: CYP3A4/A5; Chronic myeloid leukemia; Genotyping; Imatinib resistance; hOCT1.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adolescent
  • Adult
  • Aged
  • Aged, 80 and over
  • Antineoplastic Agents / therapeutic use
  • Biomarkers, Tumor / genetics
  • Child
  • Child, Preschool
  • Cohort Studies
  • Cytochrome P-450 CYP3A / genetics*
  • Female
  • Genetic Association Studies / methods
  • Genetic Variation / genetics
  • Humans
  • Imatinib Mesylate / therapeutic use*
  • Leukemia, Myelogenous, Chronic, BCR-ABL Positive / diagnosis
  • Leukemia, Myelogenous, Chronic, BCR-ABL Positive / drug therapy*
  • Leukemia, Myelogenous, Chronic, BCR-ABL Positive / genetics*
  • Male
  • Middle Aged
  • Organic Cation Transporter 1 / genetics*
  • Treatment Outcome
  • Young Adult

Substances

  • Antineoplastic Agents
  • Biomarkers, Tumor
  • Organic Cation Transporter 1
  • Imatinib Mesylate
  • CYP3A5 protein, human
  • Cytochrome P-450 CYP3A
  • CYP3A4 protein, human