Impact of brain tissue binding and plasma protein binding of drugs in DMPK

Introduction

The impression of brain tissue binding (BTB) or plasma protein binding (PPB) in Drug Metabolism and Pharmacokinetics is critical to understanding the distribution, efficacy, and potential toxicity of drugs that target the central nervous system (CNS). BTB and high PPB influence the distribution of drugs in the body and their pharmacokinetic properties. Drugs with high PPB may have reduced bioavailability and prolonged half-lives, leading to potential drug interactions and toxicity. Drugs that exhibit high BTB may have limited distribution to target sites in the brain, impacting their efficacy in treating CNS disorders. Understanding the relationship between BTB and PPB is essential for optimizing drug dosing regimens and predicting therapeutic efficacy. Imbalances in BTB and PPB can contribute to adverse effects and toxicity. This thematic issue emphasizes advances in analytical techniques and new methods that have enabled the measurement and prediction of BTB and PPB, allowing researchers to understand the pharmacokinetics of CNS drugs.

Keywords

Brain Tissue Binding, Plasma Protein Binding, Unbound fractions (fu), Blood-Brain Barriers, Brain to plasma Ratio, Pharmacokinetics, Metabolism, Bioanalysis, LC-MS/MS

Sub-topics

Ø  Quantitative analysis of CNS drugs.

Ø  Drug metabolism and pharmacokinetics of CNS drugs.

Ø  New methods to quantify the drug in the brain and fraction of unbound.

Ø  Extrahepatic metabolism of CNS drugs