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Third-generation
EGFR Mutant-Selective TKI
Covalent
(irreversible)
Overcome
T790M
RR
(%)
PFS
(mo)
OSIMERTINIB (
AZD9291
)
1-2
Yes
Yes
T790M +
71%
T790M –
21%
10.1
2.8
ROCILETINIB (
CO-1686
)
3-4
Yes
Yes
T790M +
45%
T790M –
17%
6.1
1.8
OLMUTINIB (
HM6171
3)
5-6
Yes
Yes
T790M +
54%
T790M –
11.8%
8.3
2.5
NAZARTINIB (
EGF816
)
7
Yes
Yes
T790M +
44%
9.2
NAQUOTINIB (ASP8273)
8
Yes
Yes
T790M +
37%
6.7
Acquired resistance to EGFR TKI: T790M
1
Jänne PA. N. Engl. J. Med. 2015;372:1689-99.
2
Mok T. N Engl J Med 2016, December 6
3
Sequist LV. N. Engl. J. Med. 2015;372:1700-9
4
Sequist LV. N. Engl. J. Med 2016;374:2296-7.
5
Park K. J Clin Oncol. 2016;34(15 Suppl).
6
Kim DW. ASCO 2014.
7
Tan DS. J Clin Oncol. 2016;34(suppl; abstr 9044).
8
Yu H. J Clin Oncol. 2016;34(suppl; abstr 9050)