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. © Springer Science+Business Media, LLC 2011.
CITATION STYLE
Boonen, S., Rosenberg, E., Claessens, F., Vanderschueren, D., & Papapoulos, S. (2012). Inhibition of cathepsin K for treatment of osteoporosis. Current Osteoporosis Reports, 10(1), 73–79. https://doi.org/10.1007/s11914-011-0085-9
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