Cookies on this website
We use cookies to ensure that we give you the best experience on our website. If you click 'Continue' we'll assume that you are happy to receive all cookies and you won't see this message again. Click 'Find out more' for information on how to change your cookie settings.

Over the past three decades, changes to the chemical structures of the bisphosphonates have resulted in progressive improvements in their antiresorptive potencies. Ibandronate is a potent, nitrogen-containing bisphosphonate that possesses a tertiary nitrogen group on its R2 side chain and a hydroxyl group on its R1 side chain, which together confer one of the highest antiresorptive potencies of all bisphosphonates. In common with other nitrogen-containing bisphosphonates, ibandronate is a strong inhibitor of farnesyl pyrophosphate synthase, which probably accounts for its major effects on osteoclast activity. In addition, it binds strongly to hydroxyapatite. The pharmacological efficacy and safety of various continuous and intermittent regimens of ibandronate have been extensively investigated in experimental models of osteoporosis in several animal species, including rats, dogs, and monkeys. In ovariectomized (OVX) rats, intermittent (dosing interval 2, 4, and 6 weeks) and continuous ibandronate regimens provided equivalent results per total dose irrespective of the dosing regimen. Similar results were obtained in OVX dogs and monkeys. High doses of ibandronate many times those used therapeutically were well tolerated and did not impair bone quality or mineralization in rats. Moreover, bone mass, architecture, and strength were maintained or improved, and bone healing was not adversely affected in animal models, regardless of whether ibandronate was administered intermittently or daily. The findings from all these studies demonstrate the efficacy and safety of intermittent ibandronate regimens and support the development of such regimens for the clinical management of postmenopausal osteoporosis.

Original publication

DOI

10.1016/j.bone.2006.01.151

Type

Journal article

Journal

Bone

Publication Date

04/2006

Volume

38

Pages

S7 - 12

Addresses

The Botnar Research Centre, Nuffield Department of Orthopaedic Surgery, University of Oxford, Headington, Oxford OX3 7LD, UK. graham.russell@ndos.ox.ac.uk

Keywords

Animals, Humans, Osteoporosis, Bone Resorption, Disease Models, Animal, Diphosphonates, Ovariectomy, Drug Evaluation, Preclinical, Bone Density, Bone Density Conservation Agents