Beclometasone dipropionate 是 Beclometasone 的前体活性分子，是口服有效的糖皮质激素受体激动剂。Beclometasone dipropionate 通过糖皮质激素受体发挥作用，抑制炎症和过度增殖。Beclometasone dipropionate 可用于哮喘研究。
Beclometasone dipropionate is a potent glucocorticoid agonist; it is a prodrug of the free form, beclometasone. IC50 Value: 0.2 nM (Inhibiting thymidine incorporation) [1]Target: glucocorticoid receptorin vitro: Cortisol and beclomethasone dipropionate were more potent than salbutamol in inhibiting thymidine incorporation with IC50 values of 5 nM and 0.2 nM respectively. Cortisol 100 nM led to a 16.6 +/- 6.5% reduction and beclomethasone dipropionate 3 nM led to a 17.8 +/- 5.8% reduction in cell number [1]. in vivo: Controlled trials involving 497 adults and children demonstrated similar clinical efficacy between nebulized BDP and either nebulized fluticasone propionate or nebulized budesonide. Meta-analyses show that BDP, like other inhaled corticosteroids, has no major influence on patient height, urinary cortisol concentration, or bone metabolism [2]. Beclometasone dipropionate (BDP) 800 microgday(-1) suspension for nebulization and budesonide (BUD) 750 microg day(-1) given by nebulization in a twice-daily regimen, and when used in addition to the usual maintenance therapy, resulted in comparable clinical efficacy across all parameters [3]. Clinical trial: Efficacy and Tolerability of Beclometasone/Formoterol Single Inhaler in Patients With Moderate to Severe Persistent Asthma. Phase 3
[1]. Young PG, Skinner SJ, Black PN. Effects of glucocorticoids and beta-adrenoceptor agonists on the proliferation of airway smooth muscle. Eur J Pharmacol. 1995 Jan 24;273(1-2):137-43. [2]. Nicolini G, Cremonesi G, Melani AS. Inhaled corticosteroid therapy with nebulized beclometasone dipropionate. Pulm Pharmacol Ther. 2010 Jun;23(3):145-55. [3]. Delacourt C, et al. Comparison of the efficacy and safety of nebulized beclometasone dipropionate and budesonide in severe persistent childhood asthma. Respir Med. 2003 Feb;97 Suppl B:S27-33.
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