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Role of the efflux transporters Abcb1 and Abcg2 in the brain distribution of olaparib in mice

24 Mar 2022

Abstract excerpt

Olaparib is a first-in-class poly (ADP-ribose) polymerase oral inhibitor used to treat various tumors. In this study, we clarified the roles of ABCB1/Abcb1 and ABCG2/Abcg2 transporters in restricting olaparib distribution to the brain. Olaparib was efficiently transported by human ABCG2, human ABCB1, and mouse Abcg2 in vitro. In the in vivo disposition study of olaparib using single or combination knockout mice,...

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PMID: 35341895
DOI: 10.1016/j.ejps.2022.106177

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