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)
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