Oral albuterol (salbutamol) can lead to beneficial performance effects but the drug is allowed to be delivered by inhalation in athletes with asthma. Urine levels are used to distinguish between inhalation and oral dosing. There is no information whether genetic variability places some athletes at risk of doping violations while being delivered by inhalation.The study was designed to investigate the effect of a common genetic variation of the main albuterol metabolizing enzyme SULT1A3 (single nucleotide polymorphism 105A>G, rs1975350) on the stereoselective pharmacokinetics of rac-albuterol. Subjects were administered a 400 mg dose of inhaled albuterol via a large volume spacer and blood samples were collected over 4 hours. Plasma levels of (R)- and (S)-albuterol were determined by an enantioselective LC-MS/MS assay. Twenty-five subjects with asthma were recruited and underwent SULT1A3 genotyping, from which four SNP homozygote (GG) subjects and nine wild-type (AA) subjects were selected to participated in the pharmacokinetic investigation. There were no differences in pharmacokinetic parameters (t_1/2, C_max, AUC_0-4h) between SNP and wild-type genotypes for either the R- or S-enantiomer. Observed C_max of R- and S-albuterol [mean (SD)] was 0.64 (0.30) ng/ml and 1.32 (0.98) ng/ml, respectively. The mean t_1/2 of R- and S-albuterol was estimated at 2.94 (1.17) hours and 7.86 (6.14) hours respectively. The AUC_0-4h of R- and S-albuterol was 14.0 (6.8) and 38.3 (19.5) ng/ml.h respectively. In conclusion, the common SULT1A3 SNP 105A>G is not an important determinant of albuterol enantiomer pharmacokinetics and does not place some individuals at greater risk of accumulation in the body.