Ibandronate: A Clinical Pharmacological and Pharmacokinetic Update

Ibandronate is a potent nitrogen‐containing bisphosphonate. It has a strong affinity for bone mineral and potently inhibits osteoclast‐mediated bone resorption. Ibandronate is effective for the treatment of hypercalcemia of malignancy, metastatic bone disease, postmenopausal osteoporosis, corticoste...

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Bibliographic Details
Published in:Journal of clinical pharmacology 2004-09, Vol.44 (9), p.951-965
Main Authors: Barrett, Joanne, Worth, Eric, Bauss, Frieder, Epstein, Solomon
Format: Article
Language:English
Subjects:
Biological Availability
Biotransformation
bisphosphonates
Diphosphonates - administration & dosage
Diphosphonates - adverse effects
Diphosphonates - chemistry
Diphosphonates - pharmacokinetics
Diphosphonates - pharmacology
Dose-Response Relationship, Drug
drug interactions
Humans
Ibandronate
Injections, Intravenous
Intestinal Absorption
Osteoporosis - drug therapy
pharmacodynamics
pharmacokinetics
postmenopausal osteoporosis
Tissue Distribution
tolerability
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Summary:Ibandronate is a potent nitrogen‐containing bisphosphonate. It has a strong affinity for bone mineral and potently inhibits osteoclast‐mediated bone resorption. Ibandronate is effective for the treatment of hypercalcemia of malignancy, metastatic bone disease, postmenopausal osteoporosis, corticosteroid‐induced osteoporosis, and Paget's disease. Oral ibandronate is rapidly absorbed (tmax < 1 hour), with a low bioavailability (0.63%) that is further reduced (by up to 90%) in the presence of food. Ibandronate has a wide therapeutic index and is not metabolized and, therefore, has a low potential for drug interactions. Given its metabolic stability, ibandronate is eliminated from the blood by partitioning into bone (40%‐50%) and through renal clearance (CLR ∼60 mL/min). The CLR of ibandronate is linearly related to creatinine clearance. The sequestration of ibandronate in bone (VD > 90 L) results in a multiphasic elimination (t1/2 range ∼10–60 hours), characterized by the slow release of ibandronate from the bone compartment. The potency of ibandronate and its sequestration into bone allow ibandronate to be developed as oral and intravenous injection formulations that can be administered with convenient extended between‐dose intervals.
ISSN:0091-2700
1552-4604
DOI:10.1177/0091270004267594