Current Osteoporosis Reports

, Volume 10, Issue 1, pp 73–79

Inhibition of Cathepsin K for Treatment of Osteoporosis


    • Leuven University Division of Geriatric Medicine and Centre for Metabolic Bone Diseases
  • Elizabeth Rosenberg
    • Merck Sharp & Dohme Corp.
  • Frank Claessens
    • Leuven University Department of Molecular Cell Biology
  • Dirk Vanderschueren
    • Leuven University Department of Andrology and Endocrinology
  • Socrates Papapoulos
    • Leiden University Medical Center
Future Therapeutics (P Miller, Section Editor)

DOI: 10.1007/s11914-011-0085-9

Cite this article as:
Boonen, S., Rosenberg, E., Claessens, F. et al. Curr Osteoporos Rep (2012) 10: 73. doi:10.1007/s11914-011-0085-9


Cathepsin K is the protease that is primarily responsible for the degradation of bone matrix by osteoclasts. Inhibitors of cathepsin K are in development for treatment of osteoporosis. Currently available antiresorptive drugs interfere with osteoclast function. They inhibit both bone resorption and formation, due to the coupling between these processes. Cathepsin K inhibitors, conversely, target the resorption process itself and may not interfere with osteoclast stimulation of bone formation. In fact, when cathepsin K is absent or inhibited in mice, rabbits, or monkeys, bone formation is maintained or increased. In humans, inhibition of cathepsin K is associated with sustained reductions in bone resorption markers but with smaller and transient reductions in bone formation markers. The usefulness of cathepsin K inhibitors in osteoporosis is now being examined in phase 2 and phase 3 clinical trials of postmenopausal osteoporotic women.


Cathepsin K inhibitionOsteoporosis

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© Springer Science+Business Media, LLC 2011