Effects of ONO-5334, a novel orally-active inhibitor of cathepsin K, on bone metabolism

Bone

Volumn 49, Issue 6, 2011, Pages 1351-1356

  Ochi, Yasuo ^a   Yamada, Hiroyuki ^a   Mori, Hiroshi ^a   Nakanishi, Yasutomo ^a   Nishikawa, Satoshi ^a   Kayasuga, Ryoji ^a   Kawada, Naoki ^a   Kunishige, Akiko ^a   Hashimoto, Yasuaki ^a   Tanaka, Makoto ^a   Sugitani, Masafumi ^a   Kawabata, Kazuhito ^a  

^a ONO PHARMACEUTICAL CO   (Japan)

Author keywords

Bone formation; Bone resorption; Cathepsin K inhibitor; ONO 5334; Osteoporosis

Indexed keywords

ALENDRONIC ACID; ALKALINE PHOSPHATASE; CARBOXY TERMINAL TELOPEPTIDE; CATHEPSIN B; CATHEPSIN K INHIBITOR; CATHEPSIN L; CATHEPSIN S; COLLAGEN TYPE 1; ONO 5334; OSTEOCALCIN; UNCLASSIFIED DRUG;

ARTICLE; BONE METABOLISM; CELL VIABILITY; CONCENTRATION (PARAMETERS); CONTROLLED STUDY; DOSE RESPONSE; DRUG DOSE COMPARISON; DRUG EFFICACY; DRUG INHIBITION; ENZYME ACTIVITY; ENZYME INHIBITION; FEMALE; HAPLORHINI; HUMAN; HUMAN CELL; IN VITRO STUDY; IN VIVO STUDY; MALE; METABOLIC BONE DISEASE; NONHUMAN; OSTEOCLAST; OSTEOLYSIS; PROTEIN BLOOD LEVEL; PROTEIN URINE LEVEL; RAT;

ACTINS; ADMINISTRATION, ORAL; ANIMALS; BIOLOGICAL MARKERS; BONE AND BONES; BONE REMODELING; BONE RESORPTION; CALCIUM; CATHEPSIN K; COLLAGEN TYPE I; FEMALE; HAPLORHINI; HUMANS; MALE; OSTEOGENESIS; PARATHYROIDECTOMY; PEPTIDES; PROTEASE INHIBITORS; RATS; THIAZOLIDINES;

EID: 81355148559     PISSN: 87563282     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bone.2011.09.041     Document Type: Article

References (34)

1. Osteoporosis prevention, diagnosis, and therapy. JAMA 2001, 285:785-795.
2. Black D.M., Cummings S.R., Karpf D.B., Cauley J.A., Thompson D.E., Nevitt M.C., et al. Randomised trial of effect of alendronate on risk of fracture in women with existing vertebral fractures. Lancet 1996, 348:1535-1541.
3. Harris S.T., Watts N.B., Genant H.K., McKeever C.D., Hangartner T., Keller M., et al. Effects of risedronate treatment on vertebral and nonvertebral fractures in women with postmenopausal osteoporosis: a randomized controlled trial. JAMA 1999, 282:1344-1352.
4. Chesnut C.H., Skag A., Christiansen C., Recker R., Stakkestad J.A., Hoiseth A., et al. Effects of oral ibandronate administered daily or intermittently on fracture risk in postmenopausal osteoporosis. J Bone Miner Res 2004, 19:1241-1249.
5. Black D.M., Delmas P.D., Eastell R., Reid I.R., Boonen S., Cauley J.A., et al. Once-yearly zoledronic acid for treatment of postmenopausal osteoporosis. N Engl J Med 2007, 356:1809-1822.
6. Watts N.B., Diab D.L. Long-term use of bisphosphonates in osteoporosis. J Clin Endocrinol Metab 2010, 95:1555-1565.
7. Yasuda Y., Kaleta J., Brömme D. The role of cathepsins in osteoporosis and arthritis: rationale for the design of new therapeutics. Adv Drug Deliv Rev 2005, 57:973-993.
8. Inaoka T., Bilbe G., Ishibashi O., Tezuka K., Kumegawa M., Kokubo T. Molecular cloning of human cDNA for cathepsin K: novel cysteine proteinase predominantly expressed in bone. Biochem Biophys Res Commun 1995, 206:89-96.
9. Drake F.H., Dodds R.A., James I.E., Connor J.R., Debouck C., Richardson S., et al. Cathepsin K, but not cathepsins B, L, or S, is abundantly expressed in human osteoclasts. J Biol Chem 1996, 271:12511-12516.
10. Garnero P., Borel O., Byrjalsen I., Ferreras M., Drake F.H., McQueney M.S., et al. The collagenolytic activity of cathepsin K is unique among mammalian proteinases. J Biol Chem 1998, 273:32347-32352.
11. Gelb B.D., Shi G.P., Chapman H.A., Desnick R.J. Pycnodysostosis, a lysosomal disease caused by cathepsin K deficiency. Science 1996, 273:1236-1238.
12. Johnson M.R., Polymeropoulos M.H., Vos H.L., Ortiz de Luna R.I., Francomano C.A. A nonsense mutation in the cathepsin K gene observed in a family with pycnodysostosis. Genome Res 1996, 6:1050-1055.
13. Gowen M., Lazner F., Dodds R., Kapadia R., Feild J., Tavaria M., et al. Cathepsin K knockout mice develop osteopetrosis due to a deficit in matrix degradation but not demineralization. J Bone Miner Res 1999, 14:1654-1663.
14. Li C.Y., Jepsen K.J., Majeska R.J., Zhang J., Ni R., Gelb B.D., et al. Mice lacking cathepsin K maintain bone remodeling but develop bone fragility despite high bone mass. J Bone Miner Res 2006, 21:865-875.
15. Pennypacker B., Shea M., Liu Q., Masarachia P., Saftig P., Rodan S., et al. Bone density, strength, and formation in adult cathepsin K (-/-) mice. Bone 2009, 44:199-207.
16. Kiviranta R., Morko J., Uusitalo H., Aro H.T., Vuorio E., Rantakokko J. Accelerated turnover of metaphyseal trabecular bone in mice overexpressing cathepsin K. J Bone Miner Res 2001, 16:1444-1452.
17. Morko J., Kiviranta R., Hurme S., Rantakokko J., Vuorio E. Differential turnover of cortical and trabecular bone in transgenic mice overexpressing cathepsin K. Bone 2005, 36:854-865.
18. Karsdal M.A., Martin T.J., Bollerslev J., Christiansen C., Henriksen K. Are nonresorbing osteoclasts sources of bone anabolic activity?. J Bone Miner Res 2007, 22:487-494.
19. Bossard M.J., Tomaszek T.A., Thompson S.K., Amegadzie B.Y., Hanning C.R., Jones C., et al. Proteolytic activity of human osteoclast cathepsin K. Expression, purification, activation, and substrate identification. J Biol Chem 1996, 271:12517-12524.
20. Falgueyret J.P., Black W.C., Cromlish W., Desmarais S., Lamontagne S., Mellon C., et al. An activity-based probe for the determination of cysteine cathepsin protease activities in whole cells. Anal Biochem 2004, 335:218-227.
21. Brömme D., Bonneau P.R., Lachance P., Wiederanders B., Kirschke H., Peters C., et al. Functional expression of human cathepsin S in Saccharomyces cerevisiae. Purification and characterization of the recombinant enzyme. J Biol Chem 1993, 268:4832-4838.
22. Yasuma T., Oi S., Choh N., Nomura T., Furuyama N., Nishimura A., et al. Synthesis of peptide aldehyde derivatives as selective inhibitors of human cathepsin L and their inhibitory effect on bone resorption. J Med Chem 1998, 41:4301-4308.
23. Barrett A.J., Kirschke H. Cathepsin B, Cathepsin H, and cathepsin L. Methods Enzymol 1981, 80:535-561.
24. Sasaki T., Kikuchi T., Yumoto N., Yoshimura N., Murachi T. Comparative specificity and kinetic studies on porcine calpain I and calpain II with naturally occurring peptides and synthetic fluorogenic substrates. J Biol Chem 1984, 259:12489-12494.
25. Kam C.M., Götz M.G., Koot G., McGuire M., Thiele D., Hudig D., et al. Design and evaluation of inhibitors for dipeptidyl peptidase I (Cathepsin C). Arch Biochem Biophys 2004, 427:123-134.
26. Susa M., Luong-Nguyen N.H., Cappellen D., Zamurovic N., Gamse R. Human primary osteoclasts: in vitro generation and applications as pharmacological and clinical assay. J Transl Med 2004, 2:6.
27. Nishi Y., Atley L., Eyre D.E., Edelson J.G., Superti-Furga A., Yasuda T., et al. Determination of bone markers in pycnodysostosis: effects of cathepsin K deficiency on bone matrix degradation. J Bone Miner Res 1999, 14:1902-1908.
28. Dunford J.E., Thompson K., Coxon F.P., Luckman S.P., Hahn F.M., Poulter C.D., et al. Structure-activity relationships for inhibition of farnesyl diphosphate synthase in vitro and inhibition of bone resorption in vivo by nitrogen-containing bisphosphonates. J Pharmacol Exp Ther 2001, 296:235-242.
29. 3 integrin inhibits osteoclast-mediated bone resorption in the thyroparathyroidectomized rat. Endocrinology 1996, 137:918-924.
30. Kim M.K., Kim H.D., Park J.H., Lim J.I., Yang J.S., Kwak W.Y., et al. An orally active cathepsin K inhibitor, furan-2-carboxylic acid, 1-{1-[4-fluoro-2-(2-oxo-pyrrolidin-1-yl)-phenyl]-3-oxo-piperidin-4-ylcarbamoyl}-cyclohexyl)-amide (OST-4077), inhibits osteoclast activity in vitro and bone loss in ovariectomized rats. J Pharmacol Exp Ther 2006, 318:555-562.
31. Saftig P., Hunziker E., Wehmeyer O., Jones S., Boyde A., Rommerskirch W., et al. Impaired osteoclastic bone resorption leads to osteopetrosis in cathepsin-K-deficient mice. Proc Natl Acad Sci USA 1998, 95:13453-13458.
32. McQueney M.S., Feild J., Hanning C.R., Brun K., Ramachandran K., Connor J., et al. Cynomolgus monkey (Macaca fascicularis) cathepsin K: cloning, expression, purification, and activation. Protein Expr Purif 1998, 14:387-394.
33. Rizzoli R., Greenspan S.L., Bone G., Schnitzer T.J., Watts N.B., et al. Two-year results of once-weekly administration of alendronate 70 mg for the treatment of postmenopausal osteoporosis. J Bone Miner Res 2002, 17:1988-1996. The Alendronate Once-Weekly Study Group.
34. Brown J.P., Prince R.L., Deal C., Recker R.R., Kiel D.P., de Gregorio L.H., et al. Comparison of the effect of denosumab and alendronate on BMD and biochemical markers of bone turnover in postmenopausal women with low bone mass: a randomized, blinded, phase 3 trial. J Bone Miner Res 2009, 24:153-161.