relacatib

a cathepsin K inhibitor; structure in first source

Also Known As:

N-((1S)-3-methyl-1-((((4S,7R)-7-methyl-3-oxo-1-(2-pyridinylsulfonyl)hexahydro-1H-azepin-4-yl)amino)carbonyl)-butyl)-1-benzofuran-2-carboxamide; SB 462795; SB-462795; SB462795

Networked: 5 relevant articles (0 outcomes, 2 trials/studies)

Bio-Agent Context: Research Results

Heterocyclic Compounds: 198
- 1-Ring Heterocyclic Compounds
  - Azepines: 11
    - relacatib: 5
Organic Chemicals: 133
- Sulfur Compounds: 278
  - Sulfones: 534
    - relacatib: 5

Experts

1.	Kumar, S: 2 articles (10/2009 - 01/2007)
2.	Duong, Le T: 1 article (04/2016)
3.	Langdahl, Bente: 1 article (04/2016)
4.	Leung, Albert T: 1 article (04/2016)
5.	Jerome, C P: 1 article (10/2009)
6.	Stroup, G B: 1 article (10/2009)
7.	Blake, S M: 1 article (01/2007)
8.	Dare, L: 1 article (01/2007)
9.	Gowen, M: 1 article (01/2007)
10.	Hwang, S-M: 1 article (01/2007)

Related Diseases

1.	Bone Resorption 01/01/2007 - "Administration of SB-462795 to medically ovariectomized or normal monkeys resulted in an acute reduction in both serum and urinary markers of bone resorption within 1.5 h after dosing, and this effect lasted up to 48 h depending on the dose administered. " 10/01/2009 - "By histomorphometry, relacatib reduced indices of bone resorption and formation at cancellous sites as did alendronate. " 01/01/2007 - "Our data indicate that SB-462795 potently inhibits human cathepsin K in osteoclasts, resulting in a rapid inhibition of bone resorption both in vitro and in vivo in the monkey. " 01/01/2007 - "SB-462795 inhibited endogenous cathepsin K in situ in human osteoclasts and human osteoclast-mediated bone resorption with IC50 values of approximately 45 nM and approximately 70 nM, respectively. " 01/01/2007 - "A highly potent inhibitor of cathepsin K (relacatib) reduces biomarkers of bone resorption both in vitro and in an acute model of elevated bone turnover in vivo in monkeys."
2.	Postmenopausal Osteoporosis 01/01/2007 - "These studies also demonstrate the therapeutic potential of relacatib in the treatment of postmenopausal osteoporosis and serves to model the planned clinical trials in human subjects." 04/01/2016 - "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. "
3.	Pycnodysostosis 05/31/2023 - "Unravelling the Relacatib activity against the CTSK proteins causing pycnodysostosis: a molecular docking and dynamics approach."
4.	Osteoporosis 05/31/2023 - "A structural investigation was performed to understand and gain a better knowledge about the interaction profile for the native (1BY8) and variant (Y283C) with Relacatib (a small-molecule drug that blocks the function of Cathepsin K, an enzyme that has been linked to osteoporosis, osteoarthritis, and other bone-degrading diseases). "
5.	Osteoarthritis 05/31/2023 - "A structural investigation was performed to understand and gain a better knowledge about the interaction profile for the native (1BY8) and variant (Y283C) with Relacatib (a small-molecule drug that blocks the function of Cathepsin K, an enzyme that has been linked to osteoporosis, osteoarthritis, and other bone-degrading diseases). "

Related Drugs and Biologics

1.	relacatib
2.	Cathepsin K
3.	Alendronate (Alendronate Sodium)
4.	Biomarkers (Surrogate Marker)
5.	Proteins (Proteins, Gene)
6.	Enzymes
7.	ONO-5334
8.	balicatib
9.	odanacatib