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Current Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

Medicinal Chemistry Strategies to Minimize Phospholipidosis

Author(s): Andrew J. Ratcliffe

Volume 16 , Issue 22 , 2009

Page: [2816 - 2823] Pages: 8

DOI: 10.2174/092986709788803213

Price: $65

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


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