Odanacatib, also known as MK-0822, is an inhibitor of cathepsin K with potential anti-osteoporotic activity. Odanacatib selectively binds to and inhibits the activity of cathepsin K, which may result in a reduction in bone resorption, improvement of bone mineral density, and a reversal in osteoporotic changes. Cathepsin K, a tissue-specific cysteine protease that catalyzes degradation of bone matrix proteins such as collagen I/II, elastin, and osteonectin plays an important role in osteoclast function and bone resorption. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).
Chemical Formula: C25H27F4N3O3S
Exact Mass: 525.17093
Molecular Weight: 525.56
Elemental Analysis: C, 57.13; H, 5.18; F, 14.46; N, 8.00; O, 9.13; S, 6.10
Chemical Name: (S)-N-(1-cyanocyclopropyl)-4-fluoro-4-methyl-2-(((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)-[1,1'-biphenyl]-4-yl)ethyl)amino)pentanamide
InChi Code: InChI=1S/C25H27F4N3O3S/c1-23(2,26)14-20(22(33)32-24(15-30)12-13-24)31-21(25(27,28)29)18-6-4-16(5-7-18)17-8-10-19(11-9-17)36(3,34)35/h4-11,20-21,31H,12-14H2,1-3H3,(H,32,33)/t20-,21-/m0/s1
Appearance: white solid powder, m.p. = 223 - 224 oC
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
Odanacatib is a weak inhibitor of antigen presentation, measured in a mouse B cell line (IC50=1.5±0.4 μM), compared to the Cat S inhibitor LHVS (IC50=0.001 μM) in the same assay. Odanacatib also shows weak inhibition of the processing of the MHC II invariant chain protein Iip10 in mouse splenocytes compared to LHVS (minimum inhibitory concentration 1-10 μM versus 0.01 μM, respectively). Odanacatib reduces resorption activity as measured by CTx release (IC50=9.4 nM) or resorption area (IC50=6.5 nM), but has no impact on OC activation. Odanacatib dose-dependently reduces CTx release with an IC50=9.4±1.0 nM. Odanacatib treated OC accumulates labeled degraded bone matrix proteins in CatK containing vesicles.
Odanacatib (30 mg/kg, orally, once daily) persistently suppresses bone resorption markers and serum bone formation markers versus vehicle-treated OVX monkeys. Odanacatib displays compartment-specific effects on trabecular versus cortical bone formation, with treatment resulting in marked increases in periosteal bone formation and cortical thickness in ovariectomized monkeys whereas trabecular bone formation is reduced. The bone volume/total volume (BV/TV) and bone mineral density (BMD) of the OVX + ODN-h group is significantly higher than that of the OVX + Veh group (p < 0.05). The expressions of Runx2, Collagen-1, BSP, Osterix, OPN and SPP1 are significantly lower in the OVX + ODN-h group than in the OVX + Veh group (p < 0.01). Compared with the OVX + Veh group, the expressions of Collagen-I, BSP, Osterix, OPN and ALP reduce in the OVX + ODN-l group, but are upregulated in the OVX + ODN-h group.
1. Chapurlat RD. Treatment of postmenopausal osteoporosis with odanacatib. Expert Opin Pharmacother. 2014 Jan 24. [Epub ahead of print] PubMed PMID: 24456412.
2. Odanacatib, a cathepsin K inhibitor, superior to alendronate. Bonekey Rep. 2013 Sep 4;2:426. doi: 10.1038/bonekey.2013.160. eCollection 2013. PubMed PMID: 24422127; PubMed Central PMCID: PMC3789222.
3. Retraction notice: Odanacatib for the treatment of postmenopausal osteoporosis. Expert Opin Pharmacother. 2014 Jan;15(1):151. doi: 10.1517/14656566.2014.868399. Epub 2013 Nov 30. PubMed PMID: 24289716.
4. Anderson MS, Gendrano IN, Liu C, Jeffers S, Mahon C, Mehta A, Mostoller K, Zajic S, Morris D, Lee J, Stoch SA. Odanacatib, a selective cathepsin K inhibitor, demonstrates comparable pharmacodynamics and pharmacokinetics in older men and postmenopausal women. J Clin Endocrinol Metab. 2013 Dec 20:jc20131688. [Epub ahead of print] PubMed PMID: 24276460.
5. Chapurlat RD. Odanacatib for the treatment of postmenopausal osteoporosis. Expert Opin Pharmacother. 2014 Jan;15(1):97-102. doi: 10.1517/14656566.2014.853038. Epub 2013 Oct 25. Retraction in: Expert Opin Pharmacother. 2014 Jan;15(1):151. PubMed PMID: 24156249.
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