Profiling of hepatic clearance pathways of Pittsburgh compound B and human liver cytochrome p450 phenotyping

Findings: We conducted CYP phenotyping in recombinantly expressed systems, and in human liver microsomes, to evaluate CYP isozyme contributions to the metabolism of PiB (carrier) and profiled microsomal and hepatocyte incubations for metabolites. The metabolism of PiB appears to be polyzymic, with direct conjugation via UDP-glucuronosyltransferases (UGTs) also occurring.It is unlikely that CYP inhibition or induction will significantly influence the clearance of 11C-PiB.