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Characterization and Prediction of Organic Anion Transporting Polypeptide 1B Activity in Prostate Cancer Patients on Abiraterone Acetate Using Endogenous Biomarker Coproporphyrin I.

Drug Metab Dispos

October 2024

Department of Pharmacy and Pharmaceutical Sciences (Zite.W., K.H.Y.L., E.J.Y.C., E.C.Y.C.) and Department of Surgery, Yong Loo Lin School of Medicine (S.M.T., R.P., E.C.), National University of Singapore, Singapore; Department of Urology (P.C.T., Ziti.W., Q.H.W., W.C.T., A.K., E.C.) and Department of Pharmacy (P.T.W., F.L.), National University Hospital, National University Health System, Singapore; Department of Haematology-Oncology, National University Cancer Institute, Singapore (A.S.C.W.); and National University Cancer Institute, Singapore (P.T.W.)

Article Synopsis
  • This study investigates how the cancer treatment drug abiraterone affects the liver transport proteins OATP1B1 and OATP1B3, focusing on the use of coproporphyrin I (CP-I) as a biomarker to measure these effects.
  • The results showed that abiraterone inhibits the uptake of CP-I through OATP1B3 but not OATP1B1, with in vitro tests revealing a moderate inhibition constant and clinical simulations indicating no significant drug interaction.
  • Overall, the findings suggest that the risk of interaction between abiraterone and other drugs that rely on OATP1B transporters is low, meaning that OATP1B3 does
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