Bisphosphonate mechanism of action

Title

Bisphosphonate mechanism of action

Creator

Reszka AA; Rodan GA

Publisher

Current Rheumatology Reports

Date

2003

Subject

Humans; Clodronate; Apoptosis; Bone Resorption/metabolism; Diphosphonates/chemistry/metabolism/pharmacology; Mevalonic Acid/antagonists & inhibitors; Osteoclasts/drug effects/metabolism/physiology; Osteoporosis/metabolism

Description

The nitrogen-containing bisphosphonates (N-BPs), alendronate and risedronate, are the only pharmacologic agents shown to prevent spine and nonvertebral fractures associated with postmenopausal and glucocorticoid-induced osteoporosis. At the tissue level, this is achieved through osteoclast inhibition, which leads to reduced bone turnover, increased bone mass, and improved mineralization. The molecular targets of bisphosphonates (BPs) have recently been identified. This review will discuss the mechanism of action of BPs, focusing on alendronate and risedronate, which are the two agents most widely studied. They act on the cholesterol biosynthesis pathway enzyme, farnesyl diphosphate synthase. By inhibiting this enzyme in the osteoclast, they interfere with geranylgeranylation (attachment of the lipid to regulatory proteins), which causes osteoclast inactivation. This mechanism is responsible for N-BP suppression of osteoclastic bone resorption and reduction of bone turnover, which leads to fracture prevention.
2003

Rights

Article information provided for research and reference use only. PedPalASCNET does not hold any rights over the resource listed here. All rights are retained by the journal listed under publisher and/or the creator(s).

Type

Journal Article

Citation List Month

Backlog

Pages

65-74

Issue

1

Volume

5

Citation

Reszka AA; Rodan GA, “Bisphosphonate mechanism of action,” Pediatric Palliative Care Library, accessed December 6, 2021, https://pedpalascnetlibrary.omeka.net/items/show/13069.

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