Thalidomide metabolism and hydrolysis: Mechanisms and implications

Erin R. Lepper; Nicola F. Smith; Michael C. Cox; Charity D. Scripture; William D. Figg

doi:10.2174/138920006778017777

Thalidomide metabolism and hydrolysis: Mechanisms and implications

Erin R. Lepper, Nicola F. Smith, Michael C. Cox, Charity D. Scripture, William D. Figg^*

^*Corresponding author for this work

Research output: Contribution to journal › Review article › peer-review

82 Scopus citations

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.

Original language	English
Pages (from-to)	677-685
Number of pages	9
Journal	Current Drug Metabolism
Volume	7
Issue number	6
DOIs	https://doi.org/10.2174/138920006778017777
State	Published - Aug 2006
Externally published	Yes

Keywords

CYP2C19
Hydrolysis
Hydroxylation
Pharmacokinetics

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title = "Thalidomide metabolism and hydrolysis: Mechanisms and implications",

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 = "CYP2C19, Hydrolysis, Hydroxylation, Pharmacokinetics",

author = "Lepper, {Erin R.} and Smith, {Nicola F.} and Cox, {Michael C.} and Scripture, {Charity D.} and Figg, {William D.}",

year = "2006",

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T2 - Mechanisms and implications

AU - Lepper, Erin R.

AU - Smith, Nicola F.

AU - Cox, Michael C.

AU - Scripture, Charity D.

AU - Figg, William D.

PY - 2006/8

Y1 - 2006/8

N2 - 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.

AB - 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.

KW - CYP2C19

KW - Hydrolysis

KW - Hydroxylation

KW - Pharmacokinetics

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M3 - Review article

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SN - 1389-2002

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SP - 677

EP - 685

JO - Current Drug Metabolism

JF - Current Drug Metabolism

IS - 6

ER -

Thalidomide metabolism and hydrolysis: Mechanisms and implications

Abstract

Keywords

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