In vitro transport profile of carbamazepine, oxcarbazepine, eslicarbazepine acetate, and their active metabolites by human P-glycoprotein
Chunbo Zhang, Zhong Zuo, Patrick Kwan, Larry Baum
Epilepsia | WILEY | Published : 2011
PURPOSE: Antiepileptic drugs (AEDs) are widely used not only in the treatment of epilepsy but also as treatments for psychiatric disorders. Pharmacoresistance of AEDs in the treatment of epilepsy and psychiatric disorders is a serious problem. Transport of antiepileptic drugs by P-glycoprotein (Pgp, ABCB1, or MDR1), which is overexpressed in the blood-brain barrier, may be a mechanism for resistance of AEDs. For most AEDs, conflicting evidence precludes consensus on whether they are substrates of Pgp. The objective of this study was to evaluate whether analogs and metabolites of the AED carbamazepine are substrates of human Pgp. METHODS: Polarized cell lines MDCKII and LLC transfected with t..View full abstract
Awarded by CUHK
Cell lines were kindly provided by Prof. P. Borst, The Netherlands Cancer Institute. Financial support was provided by CUHK Direct Grant 2008.1.078.Dr. Patrick Kwan has received research grants and/or honoraria/consultancy fees from Eisai, Johnson & Johnson Pharmaceutical Research & Development, Pfizer Inc., and UCB Pharma SA. The other authors declare no conflicts of interest. We confirm that we have read the Journal's position on issues involved in ethical publication and affirm that this report is consistent with those guidelines.