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The epoxyketone-based proteasome inhibitors carfilzomib and orally bioavailable oprozomib have anti-resorptive and bone-anabolic activity in addition to anti-myeloma effects.
Hurchla MA, Garcia-Gomez A, Hornick MC, Ocio EM, Li A, Blanco JF, Collins L, Kirk CJ, Piwnica-Worms D, Vij R, Tomasson MH, Pandiella A, San Miguel JF, Garayoa M, Weilbaecher KN. Hurchla MA, et al. Among authors: kirk cj. Leukemia. 2013 Feb;27(2):430-40. doi: 10.1038/leu.2012.183. Epub 2012 Jul 5. Leukemia. 2013. PMID: 22763387 Free PMC article.
Clinical activity of carfilzomib correlates with inhibition of multiple proteasome subunits: application of a novel pharmacodynamic assay.
Lee SJ, Levitsky K, Parlati F, Bennett MK, Arastu-Kapur S, Kellerman L, Woo TF, Wong AF, Papadopoulos KP, Niesvizky R, Badros AZ, Vij R, Jagannath S, Siegel D, Wang M, Ahmann GJ, Kirk CJ. Lee SJ, et al. Among authors: kirk cj. Br J Haematol. 2016 Jun;173(6):884-95. doi: 10.1111/bjh.14014. Epub 2016 Apr 12. Br J Haematol. 2016. PMID: 27071340 Free PMC article. Clinical Trial.
A novel Bruton's tyrosine kinase inhibitor CC-292 in combination with the proteasome inhibitor carfilzomib impacts the bone microenvironment in a multiple myeloma model with resultant antimyeloma activity.
Eda H, Santo L, Cirstea DD, Yee AJ, Scullen TA, Nemani N, Mishima Y, Waterman PR, Arastu-Kapur S, Evans E, Singh J, Kirk CJ, Westlin WF, Raje NS. Eda H, et al. Among authors: kirk cj. Leukemia. 2014 Sep;28(9):1892-901. doi: 10.1038/leu.2014.69. Epub 2014 Feb 12. Leukemia. 2014. PMID: 24518207
204 results