Positron Emission Tomography Imaging of [¹¹ C]Rosuvastatin Hepatic Concentrations and Hepatobiliary Transport in Humans in the Absence and Presence of Cyclosporin A.

ABSTRACT: Using positron emission tomography imaging, we determined the hepatic concentrations and hepatobiliary transport of [¹¹ C]rosuvastatin (RSV; i.v. injection) in the absence (n = 6) and presence (n = 4 of 6) of cyclosporin A (CsA; i.v. infusion) following a therapeutic dose of unlabeled RSV (5 mg, p.o.) in healthy human volunteers. The sinusoidal uptake, sinusoidal efflux, and biliary efflux clearance (CL; mL/minute) of [¹¹ C]RSV, estimated through compartment modeling were 1,205.6 ± 384.8, 16.2 ± 11.2, and 5.1 ± 1.8, respectively (n = 6). CsA (blood concentration: 2.77 ± 0.24 μM), an organic-anion-transporting polypeptide, Na⁺ -taurocholate cotransporting polypeptide, and breast cancer resistance protein inhibitor increased [¹¹ C]RSV systemic bloo

SUBMITTER: Billington S 

PROVIDER: S-EPMC6777999 | biostudies-literature | 2019 Nov

REPOSITORIES: biostudies-literature