Influence of Intestinal Transporter Genetic Variants on the Bioavailability of Gabapentin

The current study is part of a large multi-investigator grant to look at the
pharmacogenetics of a number of membrane transporters. Previously, we have recruited a
cohort of healthy volunteers (Studies of Pharmacogenetics in Ethnically-diverse Populations,
or SOPHIE) and have resequenced the coding region of a number of membrane transporter genes
to identify genetic polymorphisms in these genes. We plan to take a genotype-to-phenotype
approach to study the influence of specific polymorphisms in the intestinal transporters,
such as the novel organic cation transporters 1 and 2 (OCTN1 and OCTN2) genes on the
bioavailabilty of gabapentin in healthy subjects. Eligible subjects will have a single
inpatient study visit, during which they will take a single dose of gabapentin, and provide
blood and urine samples over the course of 36 hours (5 terminal elimination gabapentin
half-lives) for pharmacokinetic analysis.