tcsc1503 Beclometasone dipropionate

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 receptor

in 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