Zoledronic Acid

Abstract

Zoledronic acid (zoledronate) is a new generation bisphosphonate that inhibits osteoclast bone resorption. It was much more potent than other bisphosphonates at inhibiting 1,25-dihydroxyvitamin D3-induced hypercalcaemia in a rat model and calcium release in vitro. A single 5-minute intravenous infusion of zoledronic acid (4 or 8 mg) was significantly more effective than a 2-hour infusion of pamidronic acid (pamidronic acid disodium, pamidronate disodium) [90 mg] in normalising serum calcium levels in patients with hypercalcaemia of malignancy and resulted in a significantly longer median time to relapse (pooled analysis from 2 randomised, double-blind, parallel-group trials). There were no differences in tolerability between zoledronic acid and pamidronic acid in comparative trials; the most common events in pivotal trials were fever, anaemia, nausea, constipation and dyspnoea. Fever, hypophosphataemia and hypocalcaemia were the most common events in a small phase I trial.

Pamidronate Attenuates Oxidative Stress and Energetic Metabolism Changes but Worsens Functional Outcomes in Acute Doxorubicin-Induced Cardiotoxicity in Rats

“…Regarding the side effects of bisphosphonates, serum calcium can be quantified as pamidronate can induce hypocalcaemia [44]. However, we observed hypocalcaemia in the D group and more pronounced in the DP group.…”

Prophylactic Bisphosphonate Treatment Prevents Bone Fractures After Liver Transplantation

“…We chose bisphosphonate zoledronic acid for prophylaxis because of its high potency, which was just recently introduced for treating Paget's disease, and because it is being evaluated for intermittently (once yearly) treating postmenopausal osteoporosis (15)(16)(17)(18)(19). We investigated whether using zoledronic acid as a prophylactic treatment prevents bone fractures after LT.…”

Zoledronic acid slows down rat primary chondrosarcoma development, recurrent tumor progression after intralesional curretage and increases overall survival

“…Nitrogen-containing BPs act by inhibiting the recruitment, proliferation and differentiation of preosteoclasts, or by impeding the resorptive activity of mature osteoclasts. [10][11][12][13] They also shorten the life span of osteoclasts by inducing their apoptosis. 14 Previous studies revealed that BPs have the ability to reduce the osteolytic bone resorption associated with multiple myeloma and breast cancer 15,16 and also show efficacy in cancer metastases to bone due to prostate cancer and other solid tumors, demonstrating that this BPs can reduce skeletal morbidity in both osteolytic and osteoblastic diseases.…”