Fexofenadine and Rosuvastatin Pharmacokinetics in Mice with Targeted Disruption of Organic Anion Transporting Polypeptide 2B1

• Published in: Drug metabolism and disposition Vol. 47; no. 8; pp. 832 - 842
• Main Authors: Medwid, Samantha, Li, Mandy M.J., Knauer, Michael J., Lin, Kathleen, Mansell, Sara E., Schmerk, Crystal L., Zhu, Catherine, Griffin, Katelyn E., Yousif, Mohamed D., Dresser, George K., Schwarz, Ute I., Kim, Richard B., Tirona, Rommel G.
• Format: Journal Article
• Language: English
• Published: United States Elsevier Inc 01.08.2019; American Society for Pharmacology and Experimental Therapeutics, Inc
• Subjects: Absorption; Administration, Intravenous; Administration, Oral; Animal models; Animals; Anions; Area Under Curve; Disruption; Fexofenadine; Food-Drug Interactions; Fruit and Vegetable Juices; Fruit juices; Grapefruit; HEK293 Cells; HeLa Cells; Hepatocytes; Humans; In vivo methods and tests; Intestinal Absorption; Intestinal Mucosa - metabolism; Intestine; Intravenous administration; Juices; Male; Mice; Mice, Knockout; Organic Anion Transporters - genetics; Organic Anion Transporters - metabolism; Organic anion transporting polypeptide; Pharmacokinetics; Pharmacology; Polypeptides; Rodents; Rosuvastatin Calcium - administration & dosage; Rosuvastatin Calcium - pharmacokinetics; Substrate specificity; Substrates; Terfenadine - administration & dosage; Terfenadine - analogs & derivatives; Terfenadine - pharmacokinetics; Transportation; BCRP; HEK293T; mOCT; OCT; KO; KOMP; AJ; GFJ; OATP; rOATP; CLplasma; LC-MS/MS; HEK293; AUC0–last; t1/2; Tmax; mPMAT; m/z; MDCKII; WT; AUC0; mOATP

Organic anion transporting polypeptide 2B1 (OATP2B1) is a widely expressed membrane transporter with diverse substrate specificity. In vitro and clinical studies suggest a role for intestinal OATP2B1 in the oral absorption of medications. Moreover, OATP2B1 is highly expressed in hepatocytes where it...