Methods for Treating EGFR Mutant Cancers

Abstract

Methods for the treatment of EGFR mutated cancer. For example, treatment of non-small cell lung cancer (NSCLC) with activating EGFR mutations (e.g., L858R and ex19del), the acquired or resistant “gatekeeper” T790M mutation, or any combination of these mutations.

1 - 16 . (canceled) 
     
     
         17 . A method of treating NSCLC in a patent comprising administering to the patent a therapeutically effective amount of (R,E)-N-(7-chloro-1-(1-(4-(dimethylamino)but-2-enoyl)azepan-3-yl)-1Hbenzo[d]imidazol-2-yl)-2-methylisonicotinamide (Compound A), or a pharmaceutically acceptable salt thereof,
 wherein the NSCLC harbors an EGFR Exon 19 deletion and/or L858R and/or T790M mutation,   and wherein the patient has progressed on or after EGFR tyrosine kinase inhibitor (TKI) therapy with a third-generation TKI other than Compound A;   or   wherein the patient is intolerant to EGFR tyrosine kinase inhibitor (TKI) therapy with a third-generation TKI other than Compound A.   
     
     
         18 . The method according to  claim 17 , wherein the third-generation TKI is osimertinib (mereletinib), rociletinib, ASP8273, HM61713 or PF06747775. 
     
     
         19 . The method according to  claim 18 , wherein the third-generation TKI is osimertinib (mereletinib). 
     
     
         20 . The method according to  claim 17 , wherein the patient has received prior treatment with (i) one or more first-generation TKIs, and/or (ii) one or more second-generation TKIs;
 and the patient has progressed on or after such therapy.   
     
     
         21 . The method according to  claim 20 , wherein the first generation TKI is erlotinib, gefitinib or icotinib. 
     
     
         22 . The method according to  claim 20 , wherein the second generation TKI is afatinib or dacomitinib. 
     
     
         23 . The method according to  claim 17 , wherein the NSCLC is locally advanced or metastatic NSCLC. 
     
     
         24 . The method according to  claim 17 , wherein Compound A is administered in a dose ranging from 50-250 mg. 
     
     
         25 . The method according to  claim 17 , wherein Compound A is administered once daily. 
     
     
         26 . The method according to  claim 17 , wherein the pharmaceutically acceptable salt of Compound A is the mesylate salt.