Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C27H32N4O6S |
Molecular Weight | 540.631 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 3 / 3 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CC(C)C[C@H](NC(=O)C1=CC2=C(O1)C=CC=C2)C(=O)N[C@H]3CC[C@@H](C)N(CC3=O)S(=O)(=O)C4=NC=CC=C4
InChI
InChIKey=BWYBBMQLUKXECQ-GIVPXCGWSA-N
InChI=1S/C27H32N4O6S/c1-17(2)14-21(30-27(34)24-15-19-8-4-5-9-23(19)37-24)26(33)29-20-12-11-18(3)31(16-22(20)32)38(35,36)25-10-6-7-13-28-25/h4-10,13,15,17-18,20-21H,11-12,14,16H2,1-3H3,(H,29,33)(H,30,34)/t18-,20+,21+/m1/s1
Relacatib (SB-462795) is a potent and orally bioavailable small molecule inhibitor of cathepsin K that inhibits bone resorption. This has been shown in vitro in human tissue and in vivo in cynomolgus monkeys. The drug was developed for treatment in (postmenopausal) osteoporosis, osteoarthritis and potentially other bone disorders. Interactions with other drugs have been reported, and were subject of investigation of a phase I clinical trial (evaluating interactions of relacatib with ibuprofen, acetaminophen, and atorvastatin).
Approval Year
PubMed
Title | Date | PubMed |
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Structure activity relationships of 5-, 6-, and 7-methyl-substituted azepan-3-one cathepsin K inhibitors. | 2006 Mar 9 |
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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. | 2007 Jan |
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[Prevention of joint destruction by osteoclast-targeting therapy in search of new tools, such as OPG or cathepsin K inhibitor]. | 2009 Mar |
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Treatment with a potent cathepsin K inhibitor preserves cortical and trabecular bone mass in ovariectomized monkeys. | 2009 Oct |
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Emerging targets in osteoporosis disease modification. | 2010 Jun 10 |
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Odanacatib, a new drug for the treatment of osteoporosis: review of the results in postmenopausal women. | 2010 Jun 14 |
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Bisphosphonate use and hip fracture epidemiology: ecologic proof from the contrary. | 2010 Nov 19 |
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NCI_THESAURUS |
C783
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C66512
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C509706
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362505-84-8
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ACTIVE MOIETY