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Summary
Abstract
Ibandronate (ibandronic acid; Bonviva®, Boniva®), a nitrogen-containing bisphosphonate available in once-monthly oral and quarterly intravenous formulations for intermittent administration, has been approved for the treatment of osteoporosis in postmenopausal women in the EU, the US and many other countries worldwide. The once-monthly oral formulation has also been approved for the prevention of postmenopausal osteoporosis in the US.
Ibandronate is an effective and generally well tolerated bisphosphonate that offers an alternative to other bisphosphonates as a first-line treatment for postmenopausal osteoporosis. It occupies a similar position with respect to the prevention of osteoporosis in postmenopausal women at risk for the disease. The once-monthly oral and quarterly intravenous dosage regimens have the potential to improve treatment adherence and persistence, and hence clinical outcomes, compared with more frequently administered oral bisphosphonates. Intravenous ibandronate may be particularly useful for postmenopausal osteoporotic women who are noncompliant with, or are unable to tolerate or receive, oral bisphosphonates. Thus, intermittent ibandronate extends the range of pharmacological therapies for the treatment and prevention of postmenopausal osteoporosis.
Pharmacological Properties
Ibandronate is a potent, nitrogen-containing bisphosphonate and, like other bisphosphonates, it inhibits osteoclast-mediated bone resorption. In clinical trials in postmenopausal women with osteoporosis, approved oral and intravenous ibandronate dosage regimens reduced bone turnover, and increased lumbar spine and proximal femur bone mineral density (BMD) [areal and volumetric] and mechanical strength. Bone newly formed in the presence of ibandronate is normal in terms of quality and mineralization.
As with all bisphosphonates, absorption of oral ibandronate, although rapid, is low (bioavailability 0.63%) and markedly impaired by food and beverages (other than plain water). After initial systemic exposure, ibandronate is either sequestered in bone ([approximate]40-50% of the circulating dose in postmenopausal women) or excreted in the urine (renal clearance of the drug is linearly related to creatinine clearance). The apparent terminal elimination half-life of ibandronate ranged from [approximate] 10 to 72 hours following administration of single oral (150 mg) or intravenous (2 or 4 mg) doses to postmenopausal women. Ibandronate is only moderately bound to plasma proteins and does not undergo hepatic metabolism; hence, it has a low potential for displacement from plasma proteins and metabolic drug-drug interactions with other medications.
Therapeutic Efficacy
Compared with placebo, 3 years' treatment with once-daily oral ibandronate 2.5 mg...