Minimizing Drug Exposure in the CNS while Maintaining Good Oral Absorption.

ACS Med Chem Lett

Pfizer Neusentis , Portway Building, Granta Park, Great Abington, Cambridge CB21 6GS, United Kingdom.

Published: December 2012

AI Article Synopsis

  • In drug discovery, scientists sometimes want to keep certain drugs from reaching the brain to avoid side effects.
  • By picking the right chemical properties, they can make sure the drugs don’t easily access the brain but still get absorbed well in the body.
  • There are some risks to this approach that need to be thought about carefully.

Article Abstract

In some drug discovery approaches, it is advantageous to restrict the access of compounds to the CNS to minimize the risk of side effects. By choosing appropriate physicochemical properties and building in the ability to act as substrates for active efflux transporters, it is possible to achieve CNS restriction and still retain sufficient absorption through the intestinal epithelium to retain good oral bioavailability. Potential risks in employing this approach are considered.

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Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4025750PMC
http://dx.doi.org/10.1021/ml300378nDOI Listing

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