In-vitro Assessment of BCRP-Mediated Efflux of Antiseizure Medications in Human Blood-Brain Barrier Cell Model.

ABSTRACT: Drug-resistant epilepsy (DRE), where current antiseizure medications (ASMs) are ineffective in controlling seizures, affects approximately one-third of epilepsy patients. One potential mechanism that explains DRE is the presence of efflux transporters, like breast cancer resistance protein (BCRP) at the blood-brain barrier (BBB), that hamper the exposure of several ASMs to the brain. Here, we employed ATPase assay, competitive substrate efflux assay, and bidirectional transport assay to explore the interaction of BCRP with frequently prescribed eight ASMs. Immortalized human cerebral microvascular endothelial cells (hCMEC/D3) were used as a human BBB cell model. The obtained ATPase assay data revealed N-desmethyl clobazam at 12 µM and oxcarbazepine at 40 µM stimulated baseline ATPase activ

SUBMITTER: Bora S 

PROVIDER: S-EPMC12555108 | biostudies-literature | 2025 Nov

REPOSITORIES: biostudies-literature