Epilepsy affects almost 1% of the general population [1]. Approximately 30-40% of epilepsy patients do not adequately respond to antiseizure medications (ASMs) [2,3]. They are considered ‘drug-resistant’, defined as failure of two tolerated and appropriately prescribed ASMs to achieve sustained seizure freedom [4]. One proposed mechanism for drug-resistance, relevant for epilepsy and many other CNS disorders, like depression, HIV and cancer, is encapsulated by the ‘transporter hypothesis [5-7], postulating that overactivity of drug efflux transporter(s) at the blood-brain barrier (BBB) prevents drugs from reaching therapeutic concentrations at their brain targets [8].
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