Bisphosphonates: Mechanism of Action and Role in Clinical Practice

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Bisphosphonates: Mechanism of Action and Role in Clinical Practice Matthew T. Drake, MD, PhD, Bart L. Clarke, MD, Sundeep Khosla, MD Mayo Clinic Proceedings Volume 83, Issue 9, Pages 1032-1045 (September 2008) DOI: 10.4065/83.9.1032 Copyright © 2008 Mayo Foundation for Medical Education and Research Terms and Conditions

FIGURE 1 Bisphosphonate structures and approximate relative potencies6 for osteoclast inhibition. Mayo Clinic Proceedings 2008 83, 1032-1045DOI: (10.4065/83.9.1032) Copyright © 2008 Mayo Foundation for Medical Education and Research Terms and Conditions

FIGURE 2 A, Nitrogen-containing bisphosphonates selectively inhibit farnesyl pyrophosphate synthase (FPPS) within osteoclasts. B, Osteoclast endocytosis of bisphosphonate from the bone surface leads to FPPS inhibition and osteoclast apoptosis. BP = nitrogen-containing bisphosphonate; HMG-CoA = 3-hydroxy-3-methylglutaryl coenzyme A. Mayo Clinic Proceedings 2008 83, 1032-1045DOI: (10.4065/83.9.1032) Copyright © 2008 Mayo Foundation for Medical Education and Research Terms and Conditions