1,25-dihydroxyvitamin D3-3-bromoacetate

1,25-dihydroxyvitamin D3-3-bromoacetate (1,25(OH)2D3-3-BE) is a synthetic, covalent-binding analog of calcitriol (1,25-dihydroxyvitamin D3). It is designed to irreversibly bind to the ligand-binding pocket of the nuclear Vitamin D Receptor (VDR), which increases the half-life of the receptor-ligand complex and enhances its anti-proliferative and pro-apoptotic activities while potentially minimizing the systemic hypercalcemia associated with high doses of native calcitriol. Developed by researchers at Boston University, the compound has shown significant growth-inhibitory effects in preclinical models of prostate, pancreatic, and renal cancers. It acts through VDR-mediated pathways and the inhibition of Akt phosphorylation, leading to cell cycle arrest, apoptosis, and autophagy. A liposomal formulation has also been investigated to further improve its therapeutic efficacy and tumor targeting.

Other names

1α,25-dihydroxyvitamin D3-3-bromoacetate