Metabolism studies of a small-molecule tumor necrosis factor-alpha (TNF-α) inhibitor, UTL-5b (GBL-5b).
Metabolism studies of a small-molecule tumor necrosis factor-alpha (TNF-α) inhibitor, UTL-5b (GBL-5b).
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小分子肿瘤坏死因子-α (TNF-α) 抑制剂 UTL-5b (GBL-5b) 的代谢研究。
DOI：
10.1007/s13318-011-0072-7
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发表时间：
2012
影响因子：
1.9
通讯作者：
Chen,Ben
中科院分区：
文献类型：
--
作者：
Shaw,Jiajiu;Shay,Brian;Jiang,Jack;Valeriote,Frederick;Chen,Ben
UTL-5b is an anti-inflammatory and anti-arthritic small-molecule tumor necrosis factor-alpha inhibitor and a structural analogue of the anti-arthritic drug, leflunomide. Leflunomide is known to be metabolized to teriflunomide, but the metabolites of UTL-5b have not been reported. The objective of this study was to investigate whether UTL-5b has a similar metabolic behavior as leflunomide. Preliminary studies showed that when exposed to microsomes in vitro with or without NADPH, UTL-5b disappeared within 30 min. To further investigate the microsomal metabolism, liquid chromatography-ultraviolet (LC-UV) and LC/tandem mass spectrometry (LC–MS/MS) were employed to, respectively, monitor the microsomal metabolites and identify the structure of the metabolites using LC-full scan MS and LC combined with multiple-ion monitoring MS. Fragmentation determination was analyzed by two types of scans: product ion scans and precursor ion scan. The in vitro microsomal treatment of UTL-5b resulted in two major metabolites: 5-methylisoxazole-3-carboxylic acid and 2-chloroaniline. Thus, the in vitro metabolic behavior of UTL-5b appears to be different from that of leflunomide in that the isoxazole ring is cleaved.
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期刊：
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