生物活性

• 描述AMG-232 is a highly potent, selective and orally bioavailable piperidinone inhibitor of the MDM2-p53 interaction ((SPR KD= 0.045 nM, SJSA-1 EdU IC50=9.1 nM).
• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT02110355	Advanced Malignancy ... more >> Advanced Solid Tumors Cancer Oncology Oncology Patients Tumors Melanoma Collapse <<	Phase 1 Phase 2	Completed	-	United States, California ... more >> Research Site Los Angeles, California, United States, 90095 United States, Colorado Research Site Aurora, Colorado, United States, 80045 United States, Massachusetts Research Site Boston, Massachusetts, United States, 02114 United States, North Carolina Research Site Chapel Hill, North Carolina, United States, 27599 United States, Tennessee Research Site Nashville, Tennessee, United States, 37232 Australia, New South Wales Research Site North Sydney, New South Wales, Australia, 2060 Australia, Victoria Research Site Melbourne, Victoria, Australia, 3000 Collapse <<
  NCT02016729	Advanced Malignancy ... more >> Cancer Oncology Oncology Patients Acute Myeloid Leukemia Collapse <<	Phase 1	Completed	-	United States, Alabama ... more >> Research Site Birmingham, Alabama, United States, 35294 United States, New York Research Site Buffalo, New York, United States, 14263 United States, North Carolina Research Site Charlotte, North Carolina, United States, 28204 United States, Utah Research Site Salt Lake City, Utah, United States, 84112 United States, Washington Research Site Seattle, Washington, United States, 98101 Collapse <<
  NCT03031730	Hypercalcemia ... more >> Plasmacytoma Recurrent Plasma Cell Myeloma Refractory Plasma Cell Myeloma Collapse <<	Phase 1	Suspended(Temporarily stopped ... more >>for assessment. Contact ctsucontact@westat.com for specifics) Collapse <<	March 31, 2019	United States, California ... more >> University of California Davis Comprehensive Cancer Center Sacramento, California, United States, 95817 United States, Colorado University of Colorado Hospital Aurora, Colorado, United States, 80045 United States, Texas M D Anderson Cancer Center Houston, Texas, United States, 77030 Collapse <<

• 更多
• 参考文献

• [1] Canon J, Osgood T, et al. The MDM2 Inhibitor AMG 232 Demonstrates Robust Antitumor Efficacy and Potentiates the Activity of p53-Inducing Cytotoxic Agents. Mol Cancer Ther. 2015 Mar;14(3):649-58.

  [2] Rew Y, Sun D. Discovery of a small molecule MDM2 inhibitor (AMG 232) for treating cancer. J Med Chem. 2014 Aug 14;57(15):6332-41.