Plasma protein binding, pharmacokinetics, tissue distribution and CYP450 biotransformation studies of fidarestat by ultra high performance liquid chromatography-high resolution mass spectrometry

- First bioanalytical method has been developed and validated for fidarestat.
- 9.5% of the free form of the drug may be available for the pharmacological action.
- CYP1A2 and CYP2D6 appeared to be the key enzymes for the biotransformation.
- It is a weak inhibitor of CYP1A2, CYP2C19, CYP2C9, CYP2D6 and CYP3A4.
- It may not alter the pharmacokinetic and clearance of other co-administered drug.