Drug intelligence / Profile preview

zoledronate

Development stage
Approved
Lead developer
Novartis
Modality
Small Molecules
Administration
Intravenous
01

Overview

Zoledronate (also known as zoledronic acid) is a third-generation, nitrogen-containing bisphosphonate used to treat and prevent bone complications. It works by inhibiting osteoclast-mediated bone resorption, thereby increasing bone density and reducing the risk of fractures. Its mechanism involves binding to hydroxyapatite in bone and inhibiting farnesyl pyrophosphate synthase in the mevalonate pathway within osteoclasts, leading to impaired prenylation of small GTPase signaling proteins and ultimately inducing apoptosis in these cells. Zoledronate is primarily indicated for osteoporosis (in postmenopausal women, men, or those on glucocorticoids), Paget’s disease of bone, hypercalcemia of malignancy, multiple myeloma-related bone disease, and prevention/treatment of skeletal-related events from solid tumor metastases[2][3][4][5][7].

Brand names
ReclastZometaAclastaOrazol
Other names
zoledronic acid(1-hydroxy-2-imidazol-1-ylethylidene)diphosphonic acidphosphonic acid, [1-hydroxy-2-(1H-imidazol-1-yl)ethylidene]bis-Zoledronic Acid AnhydrousAnhydrous Zoledronic Acid
02

Targets

FDPS (Farnesyl pyrophosphate synthase)GGPPS1 (Geranylgeranyl pyrophosphate synthase)

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