Metabolism of the Antituberculosis Drug Ethionamide

被引：50

作者：

Vale, Nuno ^{[1
]}

Gomes, Paula ^{[1
]}

Santos, Helder A. ^{[2
]}

机构：

[1] Univ Porto, Ctr Invest Quim, Dept Chem & Biochem, Fac Sci, P-4169007 Oporto, Portugal

[2] Univ Helsinki, Div Pharmaceut Technol, Fac Pharm, FI-00014 Helsinki, Finland

来源：

CURRENT DRUG METABOLISM | 2013年 / 14卷 / 01期

基金：

芬兰科学院;

关键词：

Ethionamide; ETH-SO; EthA; EthR; ETH-NAD; metabolism; tuberculosis; mycobacterium tuberculosis; multidrug resistance; MYCOTHIOL BIOSYNTHESIS PATHWAY; MYCOBACTERIUM-TUBERCULOSIS; HUMAN FMO1; ACTIVATION; RESISTANCE; ETHR; PROTHIONAMIDE; IDENTIFICATION; THIOAMIDE; MECHANISM;

D O I：

10.2174/138920013804545151

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Ethionamide (ETH) is an important second-line antituberculosis drug used for the treatment of patients infected with multidrug-resistant Mycobacterium. Although ETH is a structural analogue of isoniazid (INH), both are pro-drugs that need to be activated by mycobacterial enzymes to exert their antimicrobial activity. ETH mechanism of action is thought to be identical to INH although the pathway of activation is distinct from that of INH. ETH is activated by an EthA enzyme, leading to the formation of an S-oxide metabolite that has considerably better activity than the parent drug. This review comprehensively examines the aspects related with the metabolism of ETH since its discovery up to today.

引用

页码：151 / 158

页数：8

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