Disease relevance of Beclomethasone 17-monopropionate

• Methods: Plasma concentrations of beclomethasone 17-monopropionate (17-BMP),a major metabolite of BDP, following an inhaled dose of HFA-BDP (200mug as four inhalations from 50mug/actuation) in five Japanese children with bronchial asthma were quantified and analyzed by a non-compartmental analysis to obtain pharmacokinetic parameters [1].

High impact information on Beclomethasone 17-monopropionate

• The metabolism kinetics of BDP and its active metabolite, beclomethasone 17-monopropionate (17-BMP), in human lung 1000 x g supernatant (HLu) and human plasma (HP) at 37 degrees C were compared [2].
• Comparisons were made of maximum plasma concentration of beclomethasone 17-monopropionate (17-BMP) (Cmax), and area under the plasma concentration vs time curve (AUC) [3].
• The recovery of BDP and its metabolite beclomethasone 17-monopropionate (B17P) in ileostomy effluent was investigated in a cross-over study after administration of formulations I or II or a reference capsule containing micronised BDP, and in a second open study after administration of formulation III [4].
• It has an absolute affinity (KD) of 0.5 nM for the glucocorticoid receptor and a relative receptor affinity 1.5- and 3.0-times greater than that of beclomethasone-17-monopropionate (17-BMP) and budesonide, respectively [5].
• Conversion of NA-AAF to DNA binding intermediates and BDP to beclomethasone-17-monopropionate by a common esterase was demonstrated and then further characterized by a broad spectrum of effectors including well-established inhibitors and substrates for the nonspecific esterases [6].

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