Development of the PC-NSAID technology: From contact angle to Vazalore?

Lichtenberger L.M.

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Development of the PC-NSAID technology: From contact angle to Vazalore?

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? 2022 Elsevier LtdWe describe strategies in drug development to reduce the gastrointestinal (GI) toxicity of nonsteroidal anti-inflammatory drugs (NSAIDs). We then provide an overview of the experiments that led to the development of PC-NSAIDs, a novel family of NSAIDs associated with phosphatidylcholine (PC) that have reduced GI toxicity and full therapeutic activity. Furthermore, we describe the evidence showing: that the stomach possesses hydrophobic properties that are attributable to phospholipids lining the mucus gel layer; and that NSAIDs chemically associate with intrinsic PC, thereby attenuating the tissue's hydrophobic properties. Further, pre-associating NSAIDs with PC reduces the GI toxicity of these drugs, both in rodent ulcer models and in human subjects, without affecting the drugs’ therapeutic activity. Finally, we discuss the commercialization and launch of Aspirin-PC, an over-the-counter (OTC) drug with the brand name Vazalore?.

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《Drug discovery today》 |2023年第1期|103411-103411|共9页
作者
Lichtenberger L.M.;
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Department of Integrative Biology & Pharmacology McGovern Medical School The University of Texas;

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正文语种英语
中图分类药学;
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aspirin; COX; cyclo-oxygenase; hydrophobicity; ibuprofen; inflammation; nonsteroidal anti-inflammatory drugs; phosphatidylcholine; phospholipids; Platelet; ulcer;

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Development of the PC-NSAID technology: From contact angle to Vazalore?

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