Bone Resorption Inhibitor

No.165(April 2015)

Z0031: Zoledronic Acid Monohydrate (1)

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⁾

This product is for research purpose only.

References

1)Bisphosphonates: From bench to bedside
- R. Graham, G. Russell, Ann. N.Y. Acad. Sci. 2006, 1068, 367.
2)Computational insights into binding of bisphosphates to farnesyl pyrophosphate synthase
- K. Ohno, K. Mori, M. Orita, M. Takeuchi, Curr. Med. Chem. 2011, 18, 220.
3)Novel insights into actions of bisphosphonates on bone: Differences in interactions with hydroxyapatite
- G. H. Nancollas, R. Tang, R. J. Phipps, Z. Henneman, S. Gulde, W. Wu, A. Mangood, R. G. G. Russell, F. H. Ebetino, Bone 2006, 38, 617.
4)Role of zoledronic acid in the prevention and treatment of osteoporosis
- A. Räkel, A. Boucher, L.-G. Ste-Marie, Clin. Interv. Aging 2011, 6, 89.
5)Emerging strategies and therapies for treatment of Paget’s disease of bone
- L. Michou, J. P. Brown, Drug Des. Devel. Ther. 2011, 5, 225.
6)The use of zoledronic acid, a novel, highly potent bisphosphonate, for the treatment of hypercalcemia of malignancy
- P. Major, Oncologist 2002, 7, 481.

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Bone Resorption Inhibitor

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