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VEL-0230, also known as NC-2300, is a small molecule cathepsin K inhibitor originally discovered by Nippon Chemiphar and later investigated by Veloci for veterinary applications, particularly in equine medicine. Cathepsin K is a cysteine protease primarily expressed in osteoclasts, where it plays a critical role in the degradation of type I collagen and other bone matrix proteins during bone resorption. By inhibiting this enzyme, VEL-0230 reduces the resorptive activity of osteoclasts without necessarily inducing their apoptosis, which may allow for the maintenance of bone formation—a potential advantage over traditional antiresorptive therapies like bisphosphonates. Preclinical studies in horses have demonstrated that VEL-0230 significantly reduces levels of the bone resorption biomarker CTX-1 (carboxy-terminal cross-linking telopeptide of type I collagen), suggesting potential therapeutic utility in treating equine bone diseases such as navicular syndrome and osteochondrosis.
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