Drug intelligence / Profile preview

liposomal calcitriol

Development stage
Preclinical
Lead developer
Boston University
Modality
Small Molecules, Lipid-based Nanoparticles → Nanoparticles → Drug Delivery Systems
Administration
Intravenous
01

Overview

Liposomal calcitriol is a specialized formulation of calcitriol (1,25-dihydroxyvitamin D3), the biologically active form of vitamin D, encapsulated within liposomes. This delivery system is designed to enhance the therapeutic index of calcitriol for oncology indications, including prostate, pancreatic, and renal cancers. While calcitriol exhibits potent anti-proliferative, pro-apoptotic, and anti-tumor effects by activating the vitamin D receptor (VDR), its clinical utility is limited by the risk of systemic hypercalcemia at pharmacological doses. Liposomal encapsulation aims to improve tumor-specific targeting and reduce systemic toxicity, allowing for the administration of higher, more effective doses. Research at institutions such as Boston University and the University of Colorado has also explored liposomal formulations of calcitriol derivatives, such as 1,25-dihydroxyvitamin D3-3-bromoacetate, which may offer enhanced stability or potency through covalent binding to the VDR.

Other names
liposomal calcitriolliposomal 1,25-dihydroxyvitamin D3liposomal 1,25(OH)2D3Lipo-Calcitriol
02

Targets

VDR (Vitamin D receptor)

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