Title : In vitro evaluation of the inhibition and induction potential of olaparib, a potent poly(ADP-ribose) polymerase inhibitor, on cytochrome P450.

Pub. Date : 2018 Jun

PMID : 28657402






3 Functional Relationships(s)
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1 In a further study, olaparib (2-200 muM) functioned as a time-dependent inhibitor of CYP3A4/5 (KI, 72.2 muM and Kinact, 0.0675 min-1). olaparib latexin Homo sapiens
2 In a further study, olaparib (2-200 muM) functioned as a time-dependent inhibitor of CYP3A4/5 (KI, 72.2 muM and Kinact, 0.0675 min-1). olaparib latexin Homo sapiens
3 Assessment of the CYP induction potential of olaparib (0.061-44 muM) showed minor concentration-related increases in CYP1A2 and more marked increases in CYP2B6 and CYP3A4 mRNA, compared with positive control activity; however, no significant change in CYP3A4/5 enzyme activity was observed. olaparib latexin Homo sapiens