Excretion is the terminal phase of pharmacokinetics, encompassing the routes by which a drug and its metabolites are irreversibly eliminated from the body. Renal excretion — via glomerular filtration, active tubular secretion, and tubular reabsorption — and biliary excretion are the predominant pathways, with minor contributions from pulmonary, salivary, and faecal elimination routes.
Our Excretion portfolio provides validated in vitro tools for the characterisation of renal transporter activity, hepatic biliary efflux, tubular secretion mechanisms, and quantification of endogenous biomarkers of renal and hepatic excretory function — supporting mechanistic excretion studies and drug–drug interaction risk assessment at the elimination phase.
Drug excretion determines the rate at which a compound is permanently removed from systemic circulation, directly governing terminal half-life, plasma clearance, and the duration of pharmacological activity. Renal excretion is the dominant elimination route for hydrophilic compounds and polar Phase II conjugates; it proceeds through three sequential mechanisms at the nephron — passive glomerular filtration of unbound drug, active tubular secretion mediated by OAT1, OAT3, OCT2, MATE1, and MATE2-K transporters, and passive or transporter-mediated tubular reabsorption.
Biliary excretion is the principal route for high-molecular-weight compounds (typically >500 Da), lipophilic metabolites, and glucuronide conjugates susceptible to enterohepatic recirculation. Hepatic canalicular efflux is mediated by ABC transporters — principally MRP2 (ABCC2), BCRP (ABCG2), and BSEP (ABCB11) — which actively transport substrates from hepatocytes into bile. Our portfolio encompasses the in vitro tools to characterise both excretion pathways, from renal transporter-expressing cell lines and membrane vesicles to sandwich-cultured hepatocyte biliary efflux systems and validated ELISA kits for excretory biomarkers.
Renal tubular secretion is mediated by a vectorial transport system in proximal tubule cells: basolateral uptake transporters (OAT1, OAT3, OCT2) deliver drug from the blood to the intracellular compartment, while apical efflux transporters (MATE1, MATE2-K) secrete it into the tubular lumen. In vitro cell systems expressing these transporters enable precise measurement of renal uptake clearance, secretory transport, and inhibition constants for DDI prediction.
Biliary excretion of drugs and their metabolites is driven by canalicular ABC transporters expressed on the apical membrane of hepatocytes. Sandwich-cultured hepatocytes (SCH) maintain functional bile canalicular networks and polarised transporter expression, enabling direct measurement of biliary clearance (CLbile) and the biliary excretion index (BEI) in vitro.
Inside-out membrane vesicles derived from cells overexpressing canalicular and renal efflux transporters enable direct measurement of ATP-dependent substrate uptake kinetics and inhibition parameters in the absence of confounding intracellular metabolism. Vesicle systems are the gold-standard in vitro model for BSEP and MRP2 inhibition assessment and for canalicular drug transport characterisation.
Quantification of endogenous biomarkers in plasma, urine, and bile enables non-invasive assessment of renal and hepatic excretory function in both in vitro and in vivo study designs. ELISA kits provide sensitive, species-specific measurements of established and emerging excretion biomarkers, supporting mechanistic studies and safety monitoring applications.
BiliTrack™ is Creative Biolabs' proprietary ELISA kit series for the quantification of endogenous biliary and renal excretion biomarkers across preclinical and translational study designs. Each kit is optimised for plasma, serum, urine, and bile matrices, and validated for use across human and multiple preclinical species. BiliTrack™ kits provide sensitive, specific measurements of bilirubin species, bile acids, and renal injury markers, supporting in vitro hepatotoxicity assessment, in vivo excretion profiling, and biomarker-based drug safety evaluation.
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