Balicatib - CAS 354813-19-7
Catalog number: 354813-19-7
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
The cathepsin K inhibitor AAE-581 (balicatib) as the most advanced of them passed Phase II clinical trials in 2005. Eighty adult female Macaca fascicularis underwent bilateral ovariectomies and were dosed twice daily by oral gavage with balicatib at 0, 3, 10, and 50 mg/kg for 18 months (groups O, L, M, H, respectively). Approximately 1 month after treatment initiation, the 50 mg/kg dose was decreased to 30 mg/kg. Twenty animals underwent sham-ovariectomies (group S). Bone mass was measured at 3-6 month intervals. At 18 months, vertebra and femur were collected for histomorphometry.
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Balicatib; AAE581; AAE-581; AAE 581
1.Morphea-like skin reactions in patients treated with the cathepsin K inhibitor balicatib.
Rünger TM1, Adami S, Benhamou CL, Czerwiński E, Farrerons J, Kendler DL, Mindeholm L, Realdi G, Roux C, Smith V. J Am Acad Dermatol. 2012 Mar;66(3):e89-96. doi: 10.1016/j.jaad.2010.11.033. Epub 2011 May 14.
BACKGROUND: In a multicenter clinical trial in North America and Europe that tested the cathepsin K (catK) inhibitor balicatib for the treatment of osteoporosis, several patients developed hardening of the skin.
2.Cathepsin K Inhibition: A New Mechanism for the Treatment of Osteoporosis.
Duong le T1, Leung AT2, Langdahl B3. Calcif Tissue Int. 2016 Apr;98(4):381-97. doi: 10.1007/s00223-015-0051-0. Epub 2015 Sep 3.
Cathepsin K (CatK), a cysteine protease, is highly expressed by osteoclasts and very efficiently degrades type I collagen, the major component of the organic bone matrix. Robust genetic and pharmacological preclinical studies consistently demonstrate that CatK inhibition increases bone mass, improves bone microarchitecture and strength. Recent advances in the understanding of the molecular and cellular mechanisms involved in bone modeling and remodeling suggest that inhibition of CatK decreases bone resorption, but increases the number of cells of osteoclast lineage. This in turn maintains the signals for bone formation, and perhaps may even increase bone formation on some cortical surfaces. Several CatK inhibitors, including relacatib, balicatib, odanacatib and ONO-5334 had entered clinical development for metabolic bone disorders with increased bone resorption, such as postmenopausal osteoporosis. However, odanacatib (ODN) is the only candidate continuing in development.
3.Cathepsin K inhibitors as treatment of bone metastasis.
Le Gall C1, Bonnelye E, Clézardin P. Curr Opin Support Palliat Care. 2008 Sep;2(3):218-22. doi: 10.1097/SPC.0b013e32830baea9.
PURPOSE OF REVIEW: Cancer cells that metastasize to the skeleton are, on their own, rarely able to destroy bone. Instead, they stimulate the function of bone-degrading cells, the osteoclasts, leading to the formation of osteolytic lesions. The purpose of this review is to consider cathepsin K, a cysteine protease produced by osteoclasts, as a therapeutic target for the treatment of patients with osteolytic bone metastases.
4.[Cathepsin K antagonists: preclinical and clinical data].
Gamsjäger M1, Resch H. Wien Med Wochenschr. 2015 Feb;165(3-4):65-70. doi: 10.1007/s10354-014-0336-3. Epub 2015 Jan 9.
Cathepsin K, a cysteine protease, is an essential enzyme in degradation of collagen type I. Since cathepsin K is relatively specific to osteoclasts, it represents a promising candidate for drug development. In the past decades, efforts have been made in developing highly potent, selective and orally applicable cathepsin K inhibitors. In contrast to balicatib and relacatib, whose drug development programmes were stopped due to cutaneous side-effects related to limited drug specificity, the more specific cathepsin K inhibitors odanacatib (ODN) and ONO-5334 have entered clinical trials. Odanacatib progressively increases bone mineral density (BMD) and decreases bone resorption markers in postmenopausal women with low BMD. Its clinical efficacy and safety was confirmed by several clinical studies but indicates that odanacatib is characterized by a resolution-of-effect with increases in bone resorption and rapid decreases in BMD following treatment discontinuation.
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