Abstract
Despite its controversial past, thalidomide is currently under investigation for the treatment of several disease types, ranging from inflammatory conditions to cancer. The mechanism of action of thalidomide is complex and not yet fully understood, but there is some evidence to suggest that metabolism may play a role. Consequently, there has been a considerable effort to characterize the metabolism of thalidomide in recent years. Thalidomide undergoes biotransformation by non-enzymatic hydrolysis and enzyme-mediated hydroxylation to form a multitude of metabolites. Metabolite identification and reaction phenotyping studies have been performed and will be discussed in this review in addition to interspecies differences in thalidomide metabolism.
Keywords: Hydrolysis, hydroxylation, CYP2C19, pharmacokinetics
Current Drug Metabolism
Title: Thalidomide Metabolism and Hydrolysis: Mechanisms and Implications
Volume: 7 Issue: 6
Author(s): Erin R. Lepper, Nicola F. Smith, Michael C. Cox, Charity D. Scripture and William D. Figg
Affiliation:
Keywords: Hydrolysis, hydroxylation, CYP2C19, pharmacokinetics
Abstract: Despite its controversial past, thalidomide is currently under investigation for the treatment of several disease types, ranging from inflammatory conditions to cancer. The mechanism of action of thalidomide is complex and not yet fully understood, but there is some evidence to suggest that metabolism may play a role. Consequently, there has been a considerable effort to characterize the metabolism of thalidomide in recent years. Thalidomide undergoes biotransformation by non-enzymatic hydrolysis and enzyme-mediated hydroxylation to form a multitude of metabolites. Metabolite identification and reaction phenotyping studies have been performed and will be discussed in this review in addition to interspecies differences in thalidomide metabolism.
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Lepper R. Erin, Smith F. Nicola, Cox C. Michael, Scripture D. Charity and Figg D. William, Thalidomide Metabolism and Hydrolysis: Mechanisms and Implications, Current Drug Metabolism 2006; 7 (6) . https://dx.doi.org/10.2174/138920006778017777
DOI https://dx.doi.org/10.2174/138920006778017777 |
Print ISSN 1389-2002 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5453 |
Call for Papers in Thematic Issues
Interaction between drugs and endocrine diseases
The introduction of highly active antiretroviral therapy accelerated studies and our understanding on the interaction between pharmacological therapies and endocrine diseases. Drugs can precipitate endocrine via different mechanisms, including direct alteration of hormone production and secretion, dysregulation of hormonal axis, effects on hormonal transport, receptor-binding, and cellular signalling. Common drug-induced ...read more
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