AIM OATP-C is a liver-specific organic anion uptake transporter and shows high affinity for bilirubin uptaking. Rifampicin has been identified as a potent inhibitor of OATP-C both in vitro and in vivo. This study was set to determine the allele frequencies of OATP-C*1a', OATP-C*1b, and OATP-C* 15 in Chinese population, and secondly, to quantitate the contribution of the OATP-C gene polymorphisms and low-dose rifampicin adminstration to the serum bilirubin level in vivo. METHODS Polymerase Chain Reaction-Restriction Fragment Length Polymorphism (PCR-RFLP) and a novel tetreprimers method were used to identify OATP-C*1a, OATP-C*1b, and OATP-C*15 genotypes.