The impact of the BBB on the pharmacokinetics of drugs: Investigations by PET

Jashvant D. Unadkat, Ban Ke, Sara Eyal

Research output: Chapter in Book/Report/Conference proceedingChapterpeer-review

Abstract

The blood brain barrier (BBB) impedes many neuropharmaceuticals from eliciting their desirable pharmacological or toxicological effect. A crucial component of this barrier is the ATP-driven drug efflux pump P-glycoprotein, which prevents the entry of xenobiotics into the brain. P-gp’s activity is also implicated in pathologies such as neurodegenerative disorders and refractory brain diseases. PET allows non-invasive in vivo assessment of P-gp’s impact on drug disposition in the CNS. Recently, a number of P-gp ligands have been synthesized for PET studies. Using the most-established P-gp ligand [11C]-verapamil, as an example, methods to quantify P-gp activity at the BBB are discussed and compared. Drug-drug interaction (DDI) studies in the CNS following modulation of P-gp activity are also presented. Finally, the application of PET methodology to study P-gp function in the diseased brain is discussed.

Original languageAmerican English
Title of host publicationTrends on the Role of PET in Drug Development
PublisherWorld Scientific Publishing Co.
Pages575-614
Number of pages40
ISBN (Electronic)9789814317740
ISBN (Print)981431773X, 9789814317733
DOIs
StatePublished - 1 Jan 2012

All Science Journal Classification (ASJC) codes

  • General Pharmacology, Toxicology and Pharmaceutics
  • General Medicine

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