*February 2021*
Highlights from Dr. Collin Blakely’s presentation: EGFR TKI Combination Therapies: C797S, MEK, AURORA Kinase at the 2021 Targeted Therapies Conference:
- EGFR C797S is the predominant on-target resistance mutation
- Osimertinib + gefitinib prevents acquired second-site EGFR resistance mutations in preclinical models
- 1 st line Osimertinib + Gefitinib is well-tolerated with ~ 90% ORR
- 4 th Generation EGFR Inhibitors (BLU-945) can target both T790M and C797S
- Limited activity of osimertinib + selumetinib after 3rd gen. EGFR TKI
- ~ 60% of resistance to 1st line osimertinib remains undefined
- Aurora kinase A drives the evolution of resistance to thirdgeneration EGFR inhibitors in lung cancer
- Activation of Aurora Kinase A is an early pro-tumor cell survival mechanism induced by EGFR TKI treatment
- Aurora kinase A inhibitor alisertib overcomes resistance to osimertinib in PDX models of EGFR lung cancer
