Neuropharmacokinetics: a bridging tool between CNS drug development and therapeutic outcome.

Drug Discov Today

Academy of Scientific and Innovative Research, New Delhi, India; Pharmaceutics and Pharmacokinetics Division, CSIR - Central Drug Research Institute, Lucknow, Uttar Pradesh, India. Electronic address:

Published: May 2019

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.

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http://dx.doi.org/10.1016/j.drudis.2019.02.007DOI Listing

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