Member-only story

Molecular Characterization and Role in Drug Disposition: A Comprehensive Guide to Drug Discovery

Jared Powell

·13.6k Followers· Follow

Published in Drug Transporters: Molecular Characterization And Role In Drug Disposition (Wiley In Drug Discovery And Development)

4 min read · 3 weeks before

64 View Claps

16 Respond

Save

Listen

Drug disposition, encompassing absorption, distribution, metabolism, and excretion (ADME),plays a pivotal role in determining the efficacy and safety of therapeutic agents. Understanding the molecular mechanisms underlying these processes is crucial for effective drug discovery and development. This comprehensive guide delves into the intricate world of molecular characterization and its profound impact on drug disposition, providing invaluable insights for researchers and practitioners alike.

Molecular Characterization of Drug-Metabolizing Enzymes

Drug-metabolizing enzymes (DMEs),primarily located in the liver, are responsible for transforming drugs into metabolites, rendering them more water-soluble and excretable. Key DMEs include cytochrome P450 (CYP) enzymes, UDP-glucuronosyltransferases (UGTs),and sulfotransferases (SULTs).

Drug Transporters: Molecular Characterization and Role in Drug Disposition (Wiley in Drug Discovery and Development)

Drug Transporters: Molecular Characterization and Role in Drug Disposition (Wiley Series in Drug Discovery and Development)

by Nancy T. Hatfield

4.4 out of 5

Language	:	English
File size	:	37035 KB
Text-to-Speech	:	Enabled
Screen Reader	:	Supported
Enhanced typesetting	:	Enabled
Print length	:	548 pages
Lending	:	Enabled

Molecular characterization of these enzymes involves identifying their genetic variants, understanding their substrate specificity, and determining their expression levels. This knowledge enables the prediction of drug metabolism rates, potential drug-drug interactions, and inter-individual variability in drug response.

Molecular Characterization of Drug Transporters

Drug transporters facilitate the movement of drugs across biological membranes, influencing their absorption, distribution, and excretion. Key transporters include P-glycoprotein (P-gp),breast cancer resistance protein (BCRP),and organic anion transporting polypeptides (OATPs).

Molecular characterization of these transporters involves determining their substrate specificity, expression levels, and tissue distribution. This information aids in predicting drug-drug interactions, identifying potential delivery barriers, and optimizing drug formulations for targeted delivery.

Role of Molecular Characterization in Drug Development

Predicting Drug Disposition: Molecular characterization enables the prediction of drug absorption, distribution, metabolism, and excretion properties, guiding dose selection and dosing regimens.
Identifying Drug-Drug Interactions: By understanding the molecular basis of drug metabolism and transport, potential drug-drug interactions can be identified, preventing adverse effects and suboptimal drug efficacy.
Optimizing Drug Delivery: Molecular characterization of transporters aids in designing drug formulations that bypass barriers to delivery, ensuring optimal drug bioavailability and efficacy.
Personalizing Drug Therapy: Genetic variations in DMEs and transporters can influence drug response. Molecular characterization enables personalized drug dosing and selection, tailoring treatments to individual patient profiles.
Evaluating Drug Safety: Understanding the molecular mechanisms of drug disposition helps identify potential toxic metabolites and predict adverse drug reactions, ensuring patient safety.

Emerging Technologies and Future Directions

Advancements in molecular characterization techniques, such as high-throughput genotyping, mass spectrometry-based metabolomics, and computational modeling, are revolutionizing drug discovery and development. These technologies facilitate a deeper understanding of the molecular determinants of drug disposition, paving the way for more precise and personalized therapies.

Molecular characterization of drug-metabolizing enzymes and transporters is a cornerstone of effective drug discovery and development. By deciphering the intricate mechanisms underlying drug disposition, researchers can predict drug behavior, identify potential risks, and optimize drug formulations for maximum efficacy and safety. This comprehensive guide provides a foundation for understanding the molecular basis of drug disposition, empowering researchers and practitioners to advance the field of drug discovery and improve patient outcomes.

Drug Transporters: Molecular Characterization and Role in Drug Disposition (Wiley Series in Drug Discovery and Development)

by Nancy T. Hatfield

4.4 out of 5