Neuropharmacokinetics: a bridging tool between CNS drug development and therapeutic outcome. Issue 5 (May 2019) - Chaturvedi, Swati
Highlights: Neuropharmacokinetics predicts novel drug brain penetration, accumulation and excretion. The BBB is the principal route and major hurdle for the entry and exit of most neuropharmaceuticals into the CNS. Drug transport is a result of the combined action of efflux and influx pumps (transporters) extensively located in the BBB membrane. Abstract : WHO classified neurological disorders to be among 6.3% of the global disease burden. Among the most central aspects of CNS drug development is the ability of novel molecules to cross the blood–brain barrier (BBB) to reach the target site over a desired time period for therapeutic action. Based on various aspects, brain pharmacokinetics is considered to be one of the foremost perspectives for the higher attrition rate of CNS biologics. Although drug traits are important, the BBB and blood–cerebrospinal fluid barrier together with transporters become the mechanistic approach behind CNS drug delivery. The present review emphasizes neuropharmacokinetic parameters, their importance, an assessment approach and the vast effect of transporters to brain drug distribution for CNS drug discovery.