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.