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Current Drug Targets


ISSN (Print): 1389-4501
ISSN (Online): 1873-5592

Cathepsin K Inhibitors: A Novel Target but Promising Approach in the Treatment of Osteoporosis

Author(s): Asadul Mazid Helali, Farhana Matin Iti and Isa Naina Mohamed

Volume 14, Issue 13, 2013

Page: [1591 - 1600] Pages: 10

DOI: 10.2174/13894501113149990202

Price: $65


Osteoporosis is a pathologic process characterized by low bone mass with skeletal fragility and an increased risk of fracture. It occurs due to an imbalance between bone resorption and formation. Although current antiresorptive therapy halts bone loss, it does not cure the condition as it also inhibits bone formation. Recent preclinical and clinical trials suggest that the inhibition of resorption by cathepsin K inhibitors increases bone formation. Cathepsin K is a papainlike cysteine protease with high potent collagenase activity and predominantly expressed in osteoclasts. While allowing demineralization, cathepsin K inhibitors suppress the degradation of type I collagen (the major organic matrix of bone) and thus enhancing bone formation. Many of these inhibitors have passed preclinical studies and are presently in clinical trials at different stages of advancement. This review explores the promising role of cathepsin K as a novel antiresorptive for the treatment of osteoporosis.

Keywords: Bone remodeling, bone resorption, bone turnover markers, cathepsin K, selective cathepsin K inhibitors, osteoporosis, osteoclast.

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