Zoledronic acid belongs to the class of nitrogen-containing bisphosphonates that acts primarily on bones.
It is indicated for the treatment of osteoporosis in adult men and post-menopausal osteoporosis in women - at increased risk of fracture, including those with a recent low-trauma hip fracture, for the treatment of osteoporosis associated with long-term systemic glucocorticoid therapy in post-menopausal women and adult men, as well as the treatment of Paget’s disease of the bone in adults.
It is formulated as injection solution, powder for solution and concentrate solution for intravenous route of administration.
Mechanism of action:
Zoledronic acid is farnesyl diphosphate synthase inhibitor. It binds to hydroxyapatite crystals in the bone matrix and inhibits farnesyl pyrophosphate (diphosphate) synthase, thereby preventing protein prenylation within the mevalonate pathway. This leads to the loss of downstream metabolites essential for osteoclast function, leading to the induction of apoptosis and eventually, osteoclast-cell death. By preventing osteoclast-mediated bone resorption, zoledronic acid decreases bone turnover and stabilizes the bone matrix.