Reference

Zoledronate in the treatment of osteolytic bone metastases

Zoledronate in the treatment of osteolytic bone metastases. Lipton, Allan (Division Medical Oncology, Pennsylvania State College Medicine, Hershey, PA 17033, USA).Chemical with cas number 118072-93-8 also plays role. British Journal of Clinical Practice, (Suppl. 87), 21 (English) 1996 Medicom International. CODEN: BJCPAT. ISSN: 0007-0947. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Zoledronate is a potent new third generation bisphosphonate which effectively lowers surrogate markers of bone resorption in cancer patients. Doses of up to 2000ug given every four weeks were well tolerated by cancer patients. .

Pharmacologic profile of zoledronic acid: A highly potent inhibitor of bone resorption

Pharmacologic profile of zoledronic acid: A highly potent inhibitor of bone resorption. Green, Jonathan R.; Rogers, Michael J. (Novartis Pharma AG, Basel CH-4002, Switz.). Drug Development Research, 55(4), 210-224 (English) 2002 Wiley-Liss, Inc. CODEN: DDREDK. ISSN: 0272-4391. DOCUMENT TYPE: Journal; General Review CA Section: 1 (Pharmacology) A review. 7440-70-2 and 118072-93-8 are cas registry numbers. These chemicals are also mentioned in this article. Bisphosphonates are effective in treating benign and malignant skeletal diseases characterized by enhanced osteoclastic bone resorption (i.e., osteoporosis, Paget's disease, tumor-induced osteolysis). The nitrogen-contg. bisphosphonate pamidronate is currently the std. treatment for hypercalcemia of malignancy (HCM) and skeletal complications of bone metastases. Zoledronic acid, a novel nitrogen-contg. bisphosphonate with an imidazole substituent, has demonstrated more potent inhibition of osteoclast-mediated bone resorption than all other bisphosphonates, including pamidronate, in both in vitro and in vivo preclin. models. Zoledronic acid inhibited ovariectomy-induced bone loss in adult monkeys and rats, and long-term treatment prevented skeletal turnover and subsequent bone loss, reduced cortical porosity, and increased mech. strength. Zoledronic acid also significantly inhibited bone loss assocd. with arthritis, bone metastases, and prosthesis loosening. The increased potency of zoledronic acid vs. pamidronate has been demonstrated clin.: zoledronic acid (4 or 8 mg iv) was superior to pamidronate (90 mg iv) in normalizing cor. serum calcium in patients with HCM. In patients with bone metastases, low doses of zoledronic acid (￡ 2 mg) suppressed bone resorption markers ￡ 50% below baseline, whereas pamidronate 90 mg yielded only 20 to 30% suppression. Importantly, the increased potency of zoledronic acid is not assocd. with an increased incidence of local (bone) or systemic adverse events. Zoledronic acid does not impair bone mineralization and, compared with pamidronate, has a greater renal and intestinal tolerability therapeutic index. Thus, based on preclin. assays and clin. data, zoledronic acid is the most potent bisphosphonate tested to date. Given its potency and excellent safety profile, zoledronic acid is now poised to become the new std. of treatment for HCM and metastatic bone disease. .