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Bone Resorption Inhibitor
No.165(April 2015)
Zoledronic acid (1) is a bisphosphonate (BP), which inhibits bone resorption, and is classified as a third-generation heterocyclic nitrogen-containing BP.1,2) The third-generation BPs inhibit farnesyl pyrophosphate synthetase.2) As well as other BPs, 1 binds to the calcium phosphate bone mineral hydroxyapatite with high affinity and, when compared with other BPs in vitro, 1 has the highest affinity for hydroxyapatite (1 > alendronate > ibandronate > risedronate > etidronate > clodronate).3) 1 has been used in the treatment of osteoporosis,4) Paget’s disease,5) and hypercalcemia of malignancy.6)
References
- 1)Bisphosphonates: From bench to bedside
- 2)Computational insights into binding of bisphosphates to farnesyl pyrophosphate synthase
- 3)Novel insights into actions of bisphosphonates on bone: Differences in interactions with hydroxyapatite
- 4)Role of zoledronic acid in the prevention and treatment of osteoporosis
- 5)Emerging strategies and therapies for treatment of Paget’s disease of bone
- 6)The use of zoledronic acid, a novel, highly potent bisphosphonate, for the treatment of hypercalcemia of malignancy
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