199798-84-0

BXL-628 is an analog of vitamin D₃ that has diverse biological activities. It increases death of androgen-stimulated human benign prostatic hyperplasia (BPH) 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.

Elocalcitol (BXL-628) is a selective, orally active vitamin D receptor (VDR) agonist. Elocalcitol shows anti-inflammatory activity. Elocalcitol inhibits growth of prostate cancer cells[1][2].

[1] Mariani M, et al. The selective vitamin D receptor agonist, elocalcitol, reduces endometriosis development in a mouse model by inhibiting peritoneal inflammation. Hum Reprod. 2012 Jul;27(7):2010-9. DOI:10.1093/humrep/des150
[2] Marchiani S, et al. The vitamin D analogue BXL-628 inhibits growth factor-stimulated proliferation and invasion of DU145 prostate cancer cells. J Cancer Res Clin Oncol. 2006 Jun;132(6):408-16. DOI:10.1007/s00432-006-0086-8