Pharmacogenetics and Treatment Response in Narcolepsy Type 1: Relevance of the Polymorphisms of the Drug Transporter Gene ABCB1

Clin Neuropharmacol. 2016 Jan-Feb;39(1):18-23. doi: 10.1097/WNF.0000000000000119.

Abstract

Objective: Narcolepsy type 1 (NT1) is a chronic hypersomnia clinically characterized by daytime sleepiness and cataplexy. Narcolepsy type 1 treatments target individual symptoms: wake-promoting agents (eg, modafinil) are effective for sleepiness, antidepressants (eg, venlafaxine) on cataplexy, whereas sodium oxybate on both. Narcolepsy type 1 patients variably respond to modafinil and venlafaxine independently of individual clinical features.Given the potential influence of drug transmembrane transport (glycoprotein-P) on drug response, we explored the relation between genetic polymorphisms in the ABCB1 gene and clinical response to modafinil/venlafaxine in NT1.

Methods: Individual drug response and genotypes were assessed in 107 NT1 patients (males/females, 64/43; mean age, 38 ± 21 years) treated with modafinil and/or venlafaxine at stable doses for at least 3 months. Minisequencing was performed to detect single-nucleotide polymorphisms in ABCB1. Patients with different responses to treatment were contrasted by Fisher exact test and multivariate analysis.

Results: The ABCB1 diplotype was significantly associated with clinical response to modafinil, with the CGC-TTT (1236/2677/3435) being more frequent in the modafinil responder versus nonresponder group (P = 0.013). Conversely, no significant associations with clinical response to venlafaxine were found.

Conclusions: The ABCB1 variants modulate therapeutic response to modafinil and may partly explain pharmacoresistance in NT1 patients.

MeSH terms

  • ATP Binding Cassette Transporter, Subfamily B / genetics
  • Adult
  • Antidepressive Agents, Second-Generation / therapeutic use*
  • Benzhydryl Compounds / therapeutic use*
  • Cytochrome P-450 CYP3A Inducers / therapeutic use*
  • DNA Mutational Analysis
  • Female
  • Genotype
  • Humans
  • Male
  • Middle Aged
  • Modafinil
  • Narcolepsy / drug therapy*
  • Narcolepsy / genetics
  • Pharmacogenetics*
  • Polymorphism, Single Nucleotide / genetics*
  • Severity of Illness Index
  • Venlafaxine Hydrochloride / therapeutic use*

Substances

  • ABCB1 protein, human
  • ATP Binding Cassette Transporter, Subfamily B
  • Antidepressive Agents, Second-Generation
  • Benzhydryl Compounds
  • Cytochrome P-450 CYP3A Inducers
  • Venlafaxine Hydrochloride
  • Modafinil

Supplementary concepts

  • Narcolepsy 1