生物活性

• 描述ASP8273 is a third-generation, irreversible and mutant-selective EGFR inhibitor which inhibited mutant EGFR containing del ex19 or L858R activating mutations as well as the T790M resistance mutation with lower IC50 values than WT EGFR. ASP8273 exhibited growth inhibition of PC-9(del ex19), HCC827(del ex19), NCI-H1975(del ex19/T790M) and PC-9ER(del ex19/T790M) with IC50 values ranging in 8-33nM, with more potency to the endogenously EGFR-dependent cells than that of NCI-H1666 (WT EGFR, IC50 230nM), while inhibition of phosphorylation of EGFR and its down-stream signal pathway ERK and Akt could be observed. Consistent with this in vitro effect, ASP8273 regressed the tumor in HCC827 and NCI-H1975 xenograft models at dose of 10, 30 and 100mg/kg, as well as inhibited tumor growth of the NSCLC patient derived tumor xenograft LU1868 (T790M/L858R) at dose of 10mg/kg.

• 动物研究
  剂量	Mice: 50 mg/kg[2] (p.o.)
  给药途径	p.o.

• 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
  NCT02113813	Non-Small-Cell Lung Cancer (NS... more >>CLC) Epidermal Growth Factor Receptor Mutations Collapse <<	Phase 1	Active, not recruiting	December 2018	United States, District of Col... more >>umbia Site US10010 Washington, District of Columbia, United States, 20007-2113 United States, Maryland Site US10006 Baltimore, Maryland, United States, 21231 United States, Massachusetts Site US10012 Boston, Massachusetts, United States, 02114 Site US10001 Boston, Massachusetts, United States, 02215 Site US10011 Boston, Massachusetts, United States, 02215 United States, New York Site US10008 New York, New York, United States, 10065 United States, North Carolina Site US10004 Chapel Hill, North Carolina, United States, 27599 United States, Ohio Site US10005 Cleveland, Ohio, United States, 44106 United States, Pennsylvania Site US10009 Philadelphia, Pennsylvania, United States, 19104 United States, Tennessee Site US10002 Nashville, Tennessee, United States, 37232 United States, Virginia Site US10003 Fairfax, Virginia, United States, 22031 United States, Washington Site US10007 Seattle, Washington, United States, 98104 Collapse <<
  NCT02674555	Epidermal Growth Factor Recept... more >>or (EGFR) Mutations Solid Tumors Collapse <<	Phase 1	Withdrawn(Following recommenda... more >>tion by SOLAR Study IDMC, Astellas closed enrollment in ASP8273 studies.) Collapse <<	-	-
  NCT03082300	Non-small Cell Lung Cancer (NS... more >>CLC) Epidermal Growth Factor Receptor (EGFR) Mutations Collapse <<	Phase 1	Terminated(Following recommend... more >>ation by SOLAR Study IDMC, Astellas closed enrollment in ASP8273 studies.) Collapse <<	-	United States, California ... more >> Beverly Hills Cancer Center Beverly Hills, California, United States, 90211 United States, Texas Renovatio Clinical The Woodlands, Texas, United States, 77380 United States, Virginia US Oncology - Virginia Cancer Specialists, P.C. (VCS) Fairfax, Virginia, United States, 22031 Collapse <<

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