吸入皮质类固醇/长效β2激动剂组合用于哮喘治疗的新专利:糠酸氟替卡松/三氟乙酸维兰特罗的药代动力学和全身活性

IF 4.2 Q3 Pharmacology, Toxicology and Pharmaceutics Recent patents on inflammation & allergy drug discovery Pub Date : 2015-07-31 DOI:10.2174/1872213X10666151119144907
O. D. Wolthers
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引用次数: 2

摘要

本文回顾了富马酸氟替卡松/三氟乙酸维兰特罗新专利的药代动力学和全身活性,并总结了儿童、青少年和成人哮喘的疗效数据。糠酸氟替卡松口服沉积的生物利用度约为1%,口服和肺沉积的生物利用度约为15%。糠酸氟替卡松400,600和800µg与成人24小时尿皮质醇排泄减少有关,而糠酸氟替卡松/三氟乙酸维兰特罗100/25µg和200/25µg每日一次的几项研究发现没有抑制作用。成人哮喘患者在吸入三氟乙酸维兰特罗后5分钟至24小时内可检测到支气管扩张。由制造商葛兰素史克(GlaxoSmithKline)赞助的五项大型临床试验提供了证据,证明干粉糠酸氟替卡松/三氟酸维兰特罗100/25µg和200/25µg每日一次对≥12岁的哮喘患者有效。然而,与每日两次相比,每日一次给药可能改善哮喘控制,这一点仍有待证实。糠酸氟替卡松在儿童中的疗效和对下丘脑-垂体-肾上腺和生长抑制的全身活性电位尚未确定。糠酸氟替卡松在儿童体内的潜在全身活性可通过测膝法进行评估。
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Pharmacokinetics and Systemic Activity of a New Patent of an Inhaled Corticosteroid/Long-Acting β2-Agonist Combination for Use in Asthma Therapy: Fluticasone Furoate/Vilanterol Trifenatate.
The present paper reviews pharmacokinetics and systemic activity of a new patent of fluticasone fumarate/vilanterol trifenatate and summarises the efficacy data in children, adolescents and adults with asthma. Bioavailability of oral deposition of fluticasone furoate is approximately 1%, of oral and pulmonary deposition 15%. Fluticasone furoate 400, 600 and 800 µg have been associated with reductions in 24h urine cortisol excretion in adults, whereas several studies on fluticasone furoate/ vilanterol trifenatate 100/25 µg and 200/25 µg once daily found no suppressive effects. Bronchodilation was detected in adults with asthma from 5 minutes after vilanterol trifenatate was inhaled and up to 24 hours after. Five large clinical trials which were sponsored by the manufacturer GlaxoSmithKline provided evidence that dry powder fluticasone furoate/vilanterol trifenatate 100/25 µg and 200/25 µg once daily are efficacious in asthma in patients ≥ 12 years of age. It remains to be proven, however, that once daily dosing may improve asthma control as compared to twice daily dosing. Efficacy and the systemic activity potential for hypothalamic-pituitary-adrenal and growth suppression of fluticasone furoate have not been established in children. The potential for systemic activity of fluticasone furoate in children may be assessed by knemometry.
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期刊介绍: Recent Patents on Inflammation & Allergy Drug Discovery publishes review articles by experts on recent patents in the field of inflammation and allergy drug discovery e.g. on novel bioactive compounds, analogs and targets. A selection of important and recent patents in the field is also included in the journal. The journal is essential reading for all researchers involved in inflammation and allergy drug design and discovery.
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Meet Our Editorial Board Member Diagnosis of Allergic Reactions to Drugs Non-steroidal Anti-inflammatory Drugs Other Antimicrobial Drugs Biologics: Monoclonal Antibodies for Non-cancer Therapy, Cytokines, Fusion Proteins, Enzymes, and Hormones
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