Drug intelligence / Profile preview

zoledronic acid + alfacalcidol

Development stage
Phase 2
Lead developer
Novartis
Modality
Small Molecules
Administration
Intravenous, Oral
01

Overview

Zoledronic acid + alfacalcidol is a combination therapy consisting of zoledronic acid, a third-generation nitrogen-containing bisphosphonate, and alfacalcidol, a synthetic vitamin D analog. Zoledronic acid acts by inhibiting osteoclast-mediated bone resorption, thereby reducing bone loss and increasing bone mineral density. Alfacalcidol exerts both anabolic and anti-resorptive effects on the skeleton by modulating calcium homeostasis and promoting bone formation. The combination has demonstrated additive or synergistic effects in preclinical models of osteoporosis—improving mechanical strength, preserving trabecular microarchitecture, reducing cortical porosity, correcting biochemical markers of bone turnover more effectively than either agent alone[1][2][3]. This combination is primarily investigated for the treatment of osteoporosis (including postmenopausal and disuse forms), with evidence suggesting it may offer therapeutic advantages over monotherapy.

02

Targets

FDPS (Farnesyl pyrophosphate synthase)RANKL (Receptor Activator for Nuclear Factor-kappa B Ligand)VDR (Vitamin D receptor)

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