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Zoledronic acid, a bisphosphonate, is an inhibitor of osteoclastic bone resorption. The action of bisphosphonates on bone is based on their high affinity for mineralized bone. Intravenously administered Zoledronic acid is rapidly distributed to bone. The main molecular target of Zoledronic acid in the osteoclast is the enzyme farnesyl pyrophosphate synthase, but this does not exclude other mechanisms. Clinical studies in tumor-induced hypercalcemia demonstrated that the effect of Zoledronic acid is characterized by decrease in serum calcium and urinary calcium excretion. In addition to its inhibitory activity against bone resorption, Zoledronic acid also possess anti-tumor activity, anti-angiogenic activity, anti-pain activity, pro-apoptic activity on tumor cells and synergistic cytostatic effect with other anti-cancer drugs.
Zoledronic acid is not metabolized and is excreted unchanged via the kidney.
Hypercalcemia of malignancy (HCM): Zoledronic acid is indicated for the treatment of hypercalcemia of malignancy defined as albumin-corrected serum calcium (cCa 12.0 mg/dL or 3.3 mmol/L).
Multiple myeloma and bone metastases of solid tumors: Zoledronic acid is indicated for the treatment of patients with multiple myeloma and patients with bone metastases from solid tumors (breast cancer, lung cancer, and prostate cancer etc.) in conjugation with standard anti-neoplastic therapy. It prevents skeletal related events ( pathological fractures, spinal compression, rediation or surgery to bone, tumor induced hypercalcemia) in patients with advanced malignancies envolving bone.
Zoclast concentrated solution for i.v. infusion: Each pack contains a vial of Zoledronic acid 4 mg as a 5 mL liquid concentrated solution for i.v. infusion.