Molecular Immunology, Section of Allergy and Clinical Immunology, National Heart and Lung Institute, Imperial College London, London, United Kingdom.
J Allergy Clin Immunol. 2011 Jun;127(6):1515-21.e6. doi: 10.1016/j.jaci.2011.02.045. Epub 2011 Apr 13.
Allergic rhinitis symptoms of itching, sneezing, rhinorrhea, and nasal obstruction significantly decrease patients' quality of life. Compared with histamine and leukotriene receptor antagonists, the petasol butenoate complex Ze 339 displays pharmacologically distinct properties. In vitro it inhibits the biosynthesis of leukotrienes and mediator release from activated eosinophils.
This study aimed to assess the efficacy and mode of action of Ze 339, desloratadine, and placebo on allergic rhinitis symptoms, nasal airflow, and local mediator levels after unilateral nasal allergen provocation.
In this double-blind, randomized, crossover study 18 subjects with allergic rhinitis to grass pollen received Ze 339, desloratadine, and placebo for 5 days before nasal allergen challenge with grass pollen extract. Rhinomanometry, symptom assessment, and local inflammatory mediator measurement were performed during the 24 hours after allergen challenge.
With Ze 339, the patient's time to recovery (5.4 ± 1.6 hours) from nasal obstruction after allergen challenge (time for return to 90% of baseline value ± SEM) was significantly shorter than with placebo (9.1 ± 2.3 hours, P = .035) and desloratadine (10.7 ± 2.5 hours, P = .022). Likewise, Ze 339's standardized symptom assessment for nasal obstruction (3.2 ± 1.3 hours) showed significantly faster relief (time for return to baseline value ± SEM compared with placebo, 8.3 ± 2.4 hours; P = .027) and desloratadine (4.5 ± 1.2 hours, P = .030). One interesting finding was that Ze 339 significantly reduced IL-8 and leukotriene B(4) levels in nasal secretions before challenge.
When compared with desloratadine and placebo, Ze 339 shows better efficacy in relieving nasal obstruction symptoms and inhibiting critical components of the chemokine network and as such represents a novel symptomatic and possible prophylactic treatment for allergic rhinitis.
过敏症的症状包括瘙痒、打喷嚏、流鼻涕和鼻塞，这些症状极大地降低了患者的生活质量。与组胺和白三烯受体拮抗剂相比，petasol 丁烯酸酯复合物 Ze 339 表现出药理上不同的特性。在体外，它抑制白三烯的生物合成和激活的嗜酸性粒细胞释放介质。
本研究旨在评估 Ze 339、地氯雷他定和安慰剂对花粉过敏的患者在单侧鼻过敏原激发后，对过敏症状、鼻气流和局部介质水平的疗效和作用模式。
在这项双盲、随机、交叉研究中，18 名对花粉过敏的患者在接受草花粉提取物鼻过敏原激发前，分别接受 Ze 339、地氯雷他定和安慰剂治疗 5 天。在过敏原激发后 24 小时内进行鼻测压、症状评估和局部炎症介质测量。
与安慰剂相比，Ze 339 组患者在过敏原激发后恢复鼻塞的时间（5.4 ± 1.6 小时）显著缩短（恢复至基线值 90%的时间 ± SEM，P =.035）和地氯雷他定（10.7 ± 2.5 小时，P =.022）。同样，Ze 339 对鼻塞的标准化症状评估（3.2 ± 1.3 小时）显示出更快的缓解（与安慰剂相比，恢复到基线值的时间 ± SEM，8.3 ± 2.4 小时，P =.027）和地氯雷他定（4.5 ± 1.2 小时，P =.030）。一个有趣的发现是，Ze 339 在激发前显著降低了鼻分泌物中的白细胞介素-8 和白三烯 B(4)水平。
与地氯雷他定和安慰剂相比，Ze 339 能更好地缓解鼻塞症状，抑制趋化因子网络的关键成分，因此是一种治疗过敏的新型对症和可能的预防性治疗方法。
