Effects of polymorphisms of the SLCO2B1 transporter gene on the pharmacokinetics of montelukast in humans

Kyoung Ah Kim, Hye Mi Lee, Hyun Jin Joo, In Bae Park, Ji Young Park

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    26 Citations (Scopus)


    Montelukast, a leukotriene receptor antagonist, is a substrate of organic anion transporting OATP2B1 encoded by the SLCO2B1. We evaluated the effects of six non]synonymous (c.1175CT, c.1457CT, c.43CT, c.935GA, c.601GA, and c.644AT) polymorphisms and one promoter (g.]282GA) polymorphism on the pharmacokinetics of montelukast. A single dose of 10 mg montelukast was administered in 24 healthy subjects. Its levels were measured up to 24 hours and a pharmacokinetic analysis was performed based on the SLCO2B1 polymorphisms. We did not encounter subjects with c.1175CT, c.43CT, or c.644AT polymorphisms. The remaining SLCO2B1 polymorphisms did not affect plasma levels of montelukast, and pharmacokinetic parameters of montelukast did not differ among genotype groups. Oral clearance results were as follows: (1) 3.3 L/h for c.935GG, 3.0 L/h for c.935GA, and 3.5 L/h for c.935AA; (2) 3.4 L/h for c.1457CC, 2.9 L/h for c.1457CT, and 3.2 L/h for c.1457TT; (3) 3.2 L/h for c.601GG, 3.4 L/h for c.601GA, and 3.4 L/h for c.601AA; (4) 3.2 L/h for g.]282GG, 3.4 L/h for g.]282GA, and 3.2 L/h for g.]282AA. The findings suggest that SLCO2B1 polymorphisms do not affect the pharmacokinetics of montelukast and that SLCO2B1 polymorphisms appear to be a minor determinant of inter]individual variability of montelukast.

    Original languageEnglish
    Pages (from-to)1186-1193
    Number of pages8
    JournalJournal of Clinical Pharmacology
    Issue number11
    Publication statusPublished - 2013 Nov


    • Montelukast
    • OATP2B1
    • Pharmacogenetics
    • Pharmacokinetics
    • SLCO2B1

    ASJC Scopus subject areas

    • Pharmacology
    • Pharmacology (medical)


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