Abstract
Drug-induced phospholipidosis is characterised by an excessive accumulation of polar phospholipids in cells or tissues. However, from a toxicological perspective the functional consequences of phospholipidosis remain uncertain and a regulatory position unclear. As a consequence, to minimize compound development risk pharmaceutical companies are beginning to proactively address phospholipidosis within drug discovery programs, and implement strategies to identify compounds predicted to show no phospholipidosis. Examples of optimization of compounds to minimize phospholipidosis, and the status of current in silico prediction models, are presented and discussed.
Keywords: Drug-induced phospholipidosis, in silico models, toxicology, physicochemical, medicinal chemistry, strategies, prediction, cationic amphiphilic drugs
Current Medicinal Chemistry
Title: Medicinal Chemistry Strategies to Minimize Phospholipidosis
Volume: 16 Issue: 22
Author(s): Andrew J. Ratcliffe
Affiliation:
Keywords: Drug-induced phospholipidosis, in silico models, toxicology, physicochemical, medicinal chemistry, strategies, prediction, cationic amphiphilic drugs
Abstract: Drug-induced phospholipidosis is characterised by an excessive accumulation of polar phospholipids in cells or tissues. However, from a toxicological perspective the functional consequences of phospholipidosis remain uncertain and a regulatory position unclear. As a consequence, to minimize compound development risk pharmaceutical companies are beginning to proactively address phospholipidosis within drug discovery programs, and implement strategies to identify compounds predicted to show no phospholipidosis. Examples of optimization of compounds to minimize phospholipidosis, and the status of current in silico prediction models, are presented and discussed.
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Cite this article as:
Ratcliffe J. Andrew, Medicinal Chemistry Strategies to Minimize Phospholipidosis, Current Medicinal Chemistry 2009; 16 (22) . https://dx.doi.org/10.2174/092986709788803213
DOI https://dx.doi.org/10.2174/092986709788803213 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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