Odanacatib

Structural formula
General
Non-proprietary name	Odanacatib
other names	(2 S ) - N - (1-Cyanocyclopropyl) -4-fluoro-4-methyl-2 - {[(1 S ) -2,2,2-trifluoro-1- [4- (4-methylsulfonylphenyl) phenyl] ethyl] amino} pentanamide ( IUPAC )
Molecular formula	C 25 H 27 F 4 N 3 O 3 S
External identifiers / databases
CAS number 603139-19-1 EC number 682-460-8 ECHA InfoCard 100.207.747 PubChem 10152654 Wikidata Q2014070
Drug information
Drug class	Enzyme inhibitor
properties
Molar mass	525.56 g · mol -1
safety instructions
GHS hazard labeling no classification available
As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions .

Odanacatib , development code MK-0822 , is an experimental compound for the treatment of osteoporosis and bone metastases .

Mechanism of action

Odanacatib selectively blocks the enzyme cathepsin K. This enzyme plays a key role in the breakdown of the bone matrix by osteoclasts .

The active ingredient was developed by MSD Sharp & Dohme .

Clinical testing

Odanacatib is not an approved medicine . The substance was in clinical phase III for the treatment of osteoporosis. Odanacatib was in clinical phase II for bone metastases caused by breast cancer . In 2016, MSD announced the discontinuation of further testing. Approval was not granted due to an increased risk of stroke.

further reading

• B. Hellwig: Odanacatib for the therapy of osteoporosis. In: Deutsche Apotheker Zeitung of December 21, 2010
• E. Isabel, C. Mellon, et al. a. Difluoroethylamines as an amide isostere in inhibitors of cathepsin K. In: Bioorganic & medicinal chemistry letters Volume 21, Number 3, February 2011, pp. 920-923, doi : 10.1016 / j.bmcl.2010.12.070 . PMID 21232956 .
• JL Pérez-Castrillón, F. Pinacho, D. De Luis, M. Lopez-Menendez, A. Dueñas Laita: Odanacatib, a new drug for the treatment of osteoporosis: review of the results in postmenopausal women. In: Journal of osteoporosis Volume 2010, 2010, S., doi : 10.4061 / 2010/401581 . PMID 20948576 . PMC 2951121 (free full text).
• WC Black: Peptidomimetic inhibitors of cathepsin K. In: Current Topics in Medicinal Chemistry Volume 10, Number 7, 2010, pp. 745-751, PMID 20337585 . (Review).
• C. Le Gall, E. Bonnelye, P. Clézardin: Cathepsin K inhibitors as treatment of bone metastasis. In: Current opinion in supportive and palliative care Volume 2, Number 3, September 2008, pp. 218-222, doi : 10.1097 / SPC.0b013e32830baea9 , PMID 18685424 .

Individual evidence

1. ↑ This substance has either not yet been classified with regard to its hazardousness or a reliable and citable source has not yet been found.
2. ↑ JY Gauthier, N. Chauret, u. a .: The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K. In: Bioorganic & medicinal chemistry letters Volume 18, number 3, February 2008, pp. 923-928, doi : 10.1016 / j.bmcl. 2007.12.047 . PMID 18226527 .
3. ↑ clinicaltrials.gov: BMD Efficacy and Safety of Odanacatib in Postmenopausal Women. Retrieved March 27, 2011.
4. ↑ clinicaltrials.gov: A Study to Examine the Effects of an Experimental Drug on Women With Breast Cancer and Metastatic Bone Disease (MBD). Retrieved March 27, 2011.
5. ↑ Merck Provides Update on Odanacatib Development Program . In: Business Wire , September 2, 2016. 

Web links

• New data on odanacatib, Merck's Investigational Cathepsin K Inhibitor for Osteoporosis, Presented at American Society for Bone and Mineral Research Annual Meeting (English)

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