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Source of inhibition constant for CYP3A4 not clear #9

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AndreDlm opened this issue Dec 16, 2020 · 0 comments
Open

Source of inhibition constant for CYP3A4 not clear #9

AndreDlm opened this issue Dec 16, 2020 · 0 comments

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@AndreDlm
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I have some difficulties understanding where the Ki of fluvoxamine for CYP3A4 comes from. In the PK-Sim file (and this publication here) the following sources are given for this value:

Yao et al. report a fu in liver microsomes of, on average, 0.33 but no Ki for CYP3A4.
Olesen et al. report a Ki of 24 ± 1.8 µM (SEM).
In PK-Sim there is a Ki,u 1.6 µM which would correspond to a fu,mic of 0.067.

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