Journal Facts

Journal
BoneKEy Knowledge Environment
ISSN
1940-8692
Volume
5
Year
2008

Article Facts

Title
An update on the pharmacology of bisphosphonates and analogues with lower bone affinity
DOI
10.1138/20080341
Authors

Fraser P Coxon

Online Date
10/00/2008

Article Links

IBMS BoneKEy | Perspective

An update on the pharmacology of bisphosphonates and analogues with lower bone affinity

Fraser P Coxon


DOI:10.1138/20080341

Abstract

It has become clear that the pharmacological characteristics of nitrogen-containing bisphosphonates (N-BPs) are the result of both their ability to inhibit farnesyl diphosphate synthase in osteoclasts and their affinity for bone mineral. Both of these properties differ for every N-BP, helping to explain the differences in both potency and duration of action within this class of drugs. The mechanistic basis for the different characteristics of N-BPs is highlighted in this review. In addition, numerous N-BP analogues have been synthesized that exhibit different target enzyme specificity and much larger variations in bone affinity than can be achieved with N-BPs. These are also discussed, with particular emphasis on the potential applications and advantages that such compounds could offer over existing N-BPs.

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