A multiplex HRMS assay for quantifying selected human plasma bile acids as candidate OATP biomarkers

Aim: Selected bile acids (BAs) in plasma have been proposed as endogenous probes for assessing drug–drug interactions involving hepatic drug transporters such as the organic anion-transporting polypeptides (OATP1B1 and OATP1B3). The cost and time required to advance a new chemical entity (NCE) to market is well documented, which encompasses clinical studies aimed at providing absorption, distribution, metabolism and excretion information to support registration [1–4]. In particular, NCEs are studied as drug–drug interaction (DDI) victims and perpetrators, especially when a specific NCE–drug combination impacts efficacy and patient safety in a clinically meaningful manner [1]. Therefore, the industry has relied increasingly on...