哮喘病治疗的新希望——白三烯拮抗剂的进展与评价

A New Hope for Asthma Treatment——Evaluation of Progress Made in the Study of Leukotriene Antagonists

白三烯是花生四烯酸经5-脂氧途径的代谢产物,是导致哮喘发作的一类重要炎性介质。白三烯类物质主要分为二羟白三烯(LTB_4)和半胱氨酰白三烯(LTD_4.LTG_4.LTE_4等)两大类。它们和气道中相应的白三烯受体结合后产生效应,在哮喘的发病机制中起着较为关键的作用。因而抑制白三烯的生物合成,或者拮抗白三烯受体,可有效地预防和治疗哮喘。白三烯拮抗剂具有平喘和抗炎的双重作用。美国已将其列入最新的哮喘指导原则,具有广阔的发展前景。目前已上市的白三烯拮抗剂是:Zileuton(zyflo)、Ibudilast、Pran-lukast 和 Zafirlukast(Accolate),接近上市的有 Montelukast(singulair),还有十多个品种正在进行Ⅱ、Ⅲ期临床实验。目前该类药物还没有一个在中国上市。

The Leukotrienes（LTs） which are formed from araehidonic acid via 5-lipoxygenase pathways are important inflammatory mediators in the treatment of asthma.LTs are mainly classified as di-hydroxy-LTs（LT B4） and cysteinyl-LTs and take effect when they bind to specific receptors in the airway.They play an important role in the treatment of asthma,so LTs receptor antagonists and synthesis inhibitors can be effective in treating prophylaxsis and asthma. LTs antagonists showing anti-asthma and anti- inflammation results,have been included in the latest U.S.Asthma Guidelines and will become a new, promising class of drugs in the treatment of asthma. Zileuton（Zyflo）,ibudilast,pranlukast,and Zafir- lukast（Accolate） have been launched in several countries,and Montelukast（singulair） is nearing market introduction,while more than 10 others are being studied and are in the second and third phase of clinical trials,but none have been launched in China.