The role of Pharmacokinetics in drug development

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Hauptverfasser: Sandhya, Kalthuri, Ramesh, Yerikala, Penabaka, Venugopalaiah, Chandra, Yadala Prapurna
Format: Recurso digital
Veröffentlicht: Zenodo 2025
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author Sandhya, Kalthuri
Ramesh, Yerikala
Penabaka, Venugopalaiah
Chandra, Yadala Prapurna
author_facet Sandhya, Kalthuri
Ramesh, Yerikala
Penabaka, Venugopalaiah
Chandra, Yadala Prapurna
contents <p>This review aims to summarize the present status of Pharmacokinetics in Drug Discovery. The review is structured into four sections. The first section is a general overview of what we understand by Pharmacokinetics and the different LADMET aspects: Liberation, Absorption, Distribution, Metabolism, Excretion, and Toxicity. The second section highlights the different computational or in silico approaches to estimate/predict one or several aspects of the pharmacokinetic profile of a discovery lead compound. The third section discusses the most commonly used in vitro methodologies. The fourth and last section examines the various approaches employed towards the pharmacokinetic assessment of discovery molecules, including all the LADME processes, discussing the different mathematical methodologies available to establish the PK profile of a test compound, what the main differences are, and what should be the criteria for using one or another mathematical approach. The primary conclusion of this review is that the use of the appropriate preclinical assays has a key role in the long-term viability of a pharmaceutical company since applying the right tools early in discovery will play a key role in determining the company's ability to discover novel safe and effective therapeutics to patients as quickly as possible.</p>
format Recurso digital
id zenodo_https___doi_org_10_5281_zenodo_16931128
institution Zenodo
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publishDate 2025
publisher Zenodo
record_format zenodo
spellingShingle The role of Pharmacokinetics in drug development
Sandhya, Kalthuri
Ramesh, Yerikala
Penabaka, Venugopalaiah
Chandra, Yadala Prapurna
Structure-Activity Relationship (SAR)
Population Pharmacokinetics
Pharmacokinetic/Pharmacodynamic Models
Biopharmaceutics Classification System (BCS)
Bioequivalence
ADME
<p>This review aims to summarize the present status of Pharmacokinetics in Drug Discovery. The review is structured into four sections. The first section is a general overview of what we understand by Pharmacokinetics and the different LADMET aspects: Liberation, Absorption, Distribution, Metabolism, Excretion, and Toxicity. The second section highlights the different computational or in silico approaches to estimate/predict one or several aspects of the pharmacokinetic profile of a discovery lead compound. The third section discusses the most commonly used in vitro methodologies. The fourth and last section examines the various approaches employed towards the pharmacokinetic assessment of discovery molecules, including all the LADME processes, discussing the different mathematical methodologies available to establish the PK profile of a test compound, what the main differences are, and what should be the criteria for using one or another mathematical approach. The primary conclusion of this review is that the use of the appropriate preclinical assays has a key role in the long-term viability of a pharmaceutical company since applying the right tools early in discovery will play a key role in determining the company's ability to discover novel safe and effective therapeutics to patients as quickly as possible.</p>
title The role of Pharmacokinetics in drug development
topic Structure-Activity Relationship (SAR)
Population Pharmacokinetics
Pharmacokinetic/Pharmacodynamic Models
Biopharmaceutics Classification System (BCS)
Bioequivalence
ADME
url https://doi.org/10.5281/zenodo.16931128