文档介绍：晚期非小细胞肺癌EGFR-TKI获得性耐药
的热点研究及进展
主要内容:
EGFR-TKI作用机制、耐药机制
新药临床研究
前景展望
k
k
k
EGFR
P
P
ERBB3
P
P
P
P
AKT
KRAS
Jak/Stat
P
EGFR信号传导的分子机制J
k
k
k
EGFR
P
P
P
TKI
Gefitinib
Erlotinib
KRAS
X
Jak/Stat
X
AKT
X
EGFR-TKI作用机制
主要内容:
EGFR-TKI作用机制、耐药机制
新药研究
前景展望
EGFR-TKI耐药机制
49%
5%
3%
2%
11%
23%
2%
3%
T790
k
k
k
EGFR
P
ERBB3
P
P
AKT
KRAS
Jak/Stat
P
T790
Gefitinib
Erlotinib
T790M介导EGFR-TKI耐药机制
EGFR-TKI耐药热点研究梳理
EGFR-tki耐药
其他
T790突变
MET扩增
3代TKI
2代TKI
MET抑制剂
Tivantinib
onartuzmab
Afatinib
itinib
CO1686/
AZD9291
RR10%
PFS小于4m
C01686——Rociletinib
Rociletinib in EGFR-Mutated Non–Small-Cell Lung Cancer(NCT01526928)
N=130 TKI AR NSCLC
T790突变情况
March 2012 and April 2014
N=130
突变阳性(46)
突变阴性(17)
DCR
93%
59%
RR
59%
29%
PFS
N Engl J Med 2015; 372:1700-1709April 30, 2015DOI:
Best Response to Rociletinib:Each bar represents an individual patient, and the amplitude and direction of the bar represent the percent change in tumor burden during treatment pared with baseline. Tumor burden was measured as the sum of thel ongest diameters of the target lesions, according to the Response Evaluation Criteria in Solid Tumors, version . The dashed line at 20% represents the boundary for determination of progressive disease, and the dashed line at −30% represents the boundary for determination of partial response. FB denotes free base, and HBr hydrogen bromide salt.
Rociletinib in EGFR-Mutated Non–Small-Cell Lung Cancer(NCT01526928)