Colon-specific prodrugs of 4-aminosalicylic acid for inflammatory bowel disease
Colon-specific prodrugs of 4-aminosalicylic acid for inflammatory bowel disease
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DOI：
10.3748/wjg.v20.i13.3564
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发表时间：
2014-04-07
影响因子：
4.3
通讯作者：
Dhaneshwar, Suneela S.
中科院分区：
文献类型：
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作者：
Dhaneshwar, Suneela S.
尽管出现了生物制品，如抗肿瘤坏死因子-α单抗(英夫利昔单抗和阿达单抗)，用于治疗中到重度炎症性肠病(IBD)，但大多数患者依赖氨基水杨酸盐作为传统治疗选择。近年来，随着对IBD复杂病理生理过程认识的增加，一些较新的药物如低分子肝素、omega-3脂肪酸、益生菌和创新制剂如大剂量一次性多基质美沙拉明被设计为通过抑制不同的靶点来最大限度地减少炎症过程。使用前药方法优化现有药物的结肠给药是另一个有吸引力的替代方案，已用于柳氮磺胺吡啶、巴柳氮特、奥沙拉嗪和伊普沙拉秦形式的5-氨基水杨酸(ASA)，但很少用于其位置异构体4-ASA-一种成熟的抗结核药物，对IBD，更具体地说，溃疡性结肠炎的效力是5-ASA的两倍。本文综述了4-ASA的完整概况及其相对于5-ASA和迄今报道的治疗IBD的结肠靶向药物的优势。审查还强调有必要重新评估这一前景看好但尚未探索的实体作为IBD的潜在治疗选择。(C)2014年白石登出版集团有限公司。版权所有。
Despite the advent of biological products, such as antitumor necrosis factor-alpha monoclonal antibodies (infliximab and adalimumab), for treatment of moderate to severe cases of inflammatory bowel disease (IBD), most patients depend upon aminosalicylates as the conventional treatment option. In recent years, the increased knowledge of complex pathophysiological processes underlying IBD has resulted in development of a number of newer pharmaceutical agents like low-molecular-weight heparin, omega-3 fatty acids, probiotics and innovative formulations such as high-dose, oncedaily multi-matrix mesalamine, which are designed to minimize the inflammatory process through inhibition of different targets. Optimization of delivery of existing drugs to the colon using the prodrug approach is another attractive alternative that has been utilized and commercialized for 5-aminosalicylic acid (ASA) in the form of sulfasalazine, balsalazide, olsalazine and ipsalazine, but rarely for its positional isomer 4-ASA -a wellestablished antitubercular drug that is twice as potent as 5-ASA against IBD, and more specifically, ulcerative colitis. The present review focuses on the complete profile of 4-ASA and its advantages over 5-ASA and colon-targeting prodrugs reported so far for the management of IBD. The review also emphasizes the need for reappraisal of this promising but unexplored entity as a potential treatment option for IBD. (C) 2014 Baishideng Publishing Group Co., Limited. All rights reserved.