Future Therapeutics (P Miller, Section Editor)

Current Osteoporosis Reports

, Volume 10, Issue 1, pp 73-79

First online:

Inhibition of Cathepsin K for Treatment of Osteoporosis

  • Steven BoonenAffiliated withLeuven University Division of Geriatric Medicine and Centre for Metabolic Bone Diseases Email author 
  • , Elizabeth RosenbergAffiliated withMerck Sharp & Dohme Corp.
  • , Frank ClaessensAffiliated withLeuven University Department of Molecular Cell Biology
  • , Dirk VanderschuerenAffiliated withLeuven University Department of Andrology and Endocrinology
  • , Socrates PapapoulosAffiliated withLeiden University Medical Center

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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 inhibition Osteoporosis