Maleate salts of (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy)anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide and crystalline forms thereof
US-9630946-B2 · Apr 25, 2017 · US
US10596162B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-10596162-B2 |
| Application number | US-201615207349-A |
| Country | US |
| Kind code | B2 |
| Filing date | Jul 11, 2016 |
| Priority date | Feb 3, 2005 |
| Publication date | Mar 24, 2020 |
| Grant date | Mar 24, 2020 |
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The present invention is directed to methods for the treatment of gefitinib and/or erlotinib resistant cancer. An individual with cancer is monitored for cancer progression following treatment with gefitinib and/or erlotinib. Progression of the cancer is indicative that the cancer is resistant to gefitinib and/or erlotinib. Once progression of cancer is noted, the subject is administered a pharmaceutical composition comprising an irreversible epidermal growth factor receptor (EGFR) inhibitor. In preferred embodiments, the irreversible EGFR inhibitor is EKB 569, HKI-272 and HKI-357.
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The invention claimed is: 1. A method of treating gefitinib and/or erlotinib resistant non-small cell lung cancer having a T790M mutation in SEQ ID NO: 1 in a patient, comprising administering daily to the patient having gefitinib and/or erlotinib resistant non-small cell lung cancer having a T790M mutation in SEQ ID NO: 1 a pharmaceutical composition comprising a unit dosage of 2-500 mg of an irreversible EGFR inhibitor that covalently binds to cysteine 773 of the catalytic domain within the SEQ ID NO: 1 having a T790M mutation; wherein the irreversible EGFR inhibitor is not CL-387,785. 2. The method of claim 1 , wherein the irreversible EGFR inhibitor is selected from the group consisting of EKB-569, HKI-272 and HKI-357. 3. The method of claim 1 , wherein the irreversible EGFR inhibitor is HKI-272. 4. The method of claim 1 , wherein the irreversible EGFR inhibitor covalently binds to cysteine 805 in the ligand-binding pocket of ERBB2.
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