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Osteoporosis Therapy: Mechanistic Antiresorptives

Pulmonary, Bone, Vitamins and Autocoid Therapeutic Agents

  1. Jeffrey A. Dodge,
  2. Henry U. Bryant

Published Online: 29 JAN 2010

DOI: 10.1002/0471266949.bmc197

Burger's Medicinal Chemistry and Drug Discovery

Burger's Medicinal Chemistry and Drug Discovery

How to Cite

Dodge, J. A. and Bryant, H. U. 2010. Osteoporosis Therapy: Mechanistic Antiresorptives. Burger's Medicinal Chemistry and Drug Discovery. 711–734.

Author Information

  1. Eli Lilly and Company, Lilly Research Laboratories, Indianapolis, IN

Publication History

  1. Published Online: 29 JAN 2010


Osteoporosis is defined as the thinning of bone resulting from the imbalance between bone resorption and bone formation, the two cellular mechanisms that regulate the remodeling of skeletal tissue. This loss of bone ultimately results in an increased risk of fracture. One therapeutic approach to treating patients with osteoporosis is to inhibit the process of bone resorption. This has been clinically manifested by the development of a number of large and small molecules that include calcitonin, integrin inhibitors, cathepsin K inhibitors, OPG/RANKL inhibitors, bisphosponates, and SERMS. This chapter describes recent advances in the anti-resorptive field with a focus on clinically validated targets and the molecules that have been developed to regulate these pathways.


  • Osteoporosis;
  • Osteoclast;
  • Osteoblast;
  • Calcitonin;
  • Cathepsin K Inhibitors;
  • Osteoprotegerin;
  • RANKL;
  • Bisphosponates;
  • Selective Estrogen Receptor Modulators;
  • SERMs