Medicinal Chemistry Strategies to Minimize Phospholipidosis

Author(s): Andrew J. Ratcliffe.

Journal Name: Current Medicinal Chemistry

Volume 16 , Issue 22 , 2009

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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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Article Details

Year: 2009
Page: [2816 - 2823]
Pages: 8
DOI: 10.2174/092986709788803213
Price: $58

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