A vitamin D3 analog with diverse biological activities
BXL-628 is an analog of vitamin D3 cells via induction of apoptosis in a dose-dependent manner. In vivo, BXL-628 completely inhibits androgen-stimulated prostate overgrowth in a rat model of BPH. It reduces expression of IL-13 and IgE/mast cell-derived protease 1 (MMCP1) and decreases edema and leukocyte infiltration in the bladder wall in a mouse model of allergen-induced interstitial cystitis. BXL-628 also reduces the number of adherent endometrial stromal cells and decreases the total weight of endometrial lesions in a mouse model of endometriosis. Formulations containing BXL-628 are under clinical investigation for the treatment of BPH.
参考文献:
[1].Crescioli, C., Ferruzzi, P., Caporali, A., et al. Inhibition of prostate cell growth by BXL-628, a calcitriol analogue selected for a phase II clinical trial in patients with benign prostate hyperplasia Eur. J. Endocrinol. 150(4), 591-603 (2004).
[2].Benigni, F., Baroni, E., Zecevic, M., et al. Oral treatment with a vitamin D3 analogue (BXL628) has anti-inflammatory effects in rodent model of interstitial cystitis BJU Int. 97(3), 617-624 (2006).
[3]. Mariani, M., Viganò, P., Gentilini, D., et al. The selective vitamin D receptor agonist, elocalcitol, reduces endometriosis development in a mouse model by inhibiting peritoneal inflammation Hum. Reprod. 27(7), 2010-2019 (2012).
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