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We aimed to investigate the effect of the ABCB1 gene on the pharmacokinetics of amlodipine.

Based on polymorphisms of the ABCB1 gene at positions 2677 and 3435, 26 healthy male participants were divided into three groups: subjects with 2677GG/3435CC (n = 9), 2677GT/3435CT (n = 9) and 2677TT/3435TT (n = 8). After a single‐dose administration of 5 mg amlodipine, plasma concentrations of amlodipine were measured and its pharmacokinetic characteristics were compared according to ABCB1 genotype.

The area under the plasma concentration–time curve was significantly lower in subjects with 2677TT/3435TT (140.8 ± 35.6 ng h⁻¹ ml⁻¹) and 2677GT/3435CT (149.8 ± 40.1 ng h⁻¹ ml⁻¹) than in those with 2677GG/3435CC (208.6 ± 39.2 ng h⁻¹ ml⁻¹) [95% confidence interval (CI) on the difference, 2677GG/3435CC vs. 2677GT/3435CT 12.0, 105.6, P < …