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Compound class: Synthetic organic
Comment: Odanacatib, a cathepsin K inhibitor, has clinically shown prevention of bone loss in osteoporosis. However, in Sept 2016 Merck ceased development because of an increased risk of stroke in the Phase 3 results (see the In the Pipeline commentary)
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
1. Brixen K, Chapurlat R, Cheung AM, Keaveny TM, Fuerst T, Engelke K, Recker R, Dardzinski B, Verbruggen N, Ather S et al.. (2013)
Bone density, turnover, and estimated strength in postmenopausal women treated with odanacatib: a randomized trial.
J Clin Endocrinol Metab, 98 (2): 571-80. [PMID:23337728]
2. Gauthier JY, Chauret N, Cromlish W, Desmarais S, Duong le T, Falgueyret JP, Kimmel DB, Lamontagne S, Léger S, LeRiche T et al.. (2008)
The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K.
Bioorg Med Chem Lett, 18 (3): 923-8. [PMID:18226527]