| 摘要 |
The present invention relates to a method of treatment of patients suffering from cancer and harboring mutations of EGFR in the tumor, for instance an activating mutation of the EGFR or a mutation responsible for resistance or the emergence of acquired resistance to treatment with reversible EGFR and/or HER2 inhibitors or irreversible inhibitors such as CI-1033, EKB-569, HKI-272 or HKI-357, comprising administering an effective amount of the irreversible EGFR inhibitor BIBW2992 (1) 4-[(3-chloro-4-fluorophenyl)amino]-6-{[4-(N,N-dimethylamino)-1-oxo-2-buten-1-yl]amino}-7-((S)-tetrahydrofuran-3-yloxy)-quinazoline, to a person in need of such treatment, optionally in combination with the administration of a further chemotherapeutic agent, in combination with radiotherapy, radio-immunotherapy and/or tumor resection by surgery, and to the use of a BIBW 2992 (1) for preparing a pharmaceutical composition for the treatment of patients suffering from cancer and harboring mutations of EGFR in the tumor. |
| 主权项 |
1. A method of treating patients suffering from cancer selected from the group consisting of
Central nervous system tumours selected from the group consisting of: Astrocytoma, glioblastoma, meningeoma, neurinoma, schwannoma, ependymoma, hypophysoma, oligodendroglioma and medulloblastoma; Ovarian cancers selected from the group consisting of: Epithelial tumours, stroma tumours, germ cell tumours and undifferentiated tumours; Prostate cancers selected from the group consisting of: AC, small cell and SCC; said cancers harbouring a mutation of the EGFR gene in the tumour, wherein the EGFR mutation is an activating mutation selected from the group of mutations identified in table 1 under No. 1 to 29, 57 to 65, 73, 75, 76, 77, 79 and 80-91, wherein the cancer shows resistance or acquired resistance to treatment with reversible EGFR and HER2 inhibitors or to other irreversible inhibitors selected from CI-1033, EKB-569, HKI-272 or HKI-357, said method consisting of administering a therapeutically effective amount of the single irreversible EGFR inhibitor BIBW 2992 (1) to a patient in need thereof, optionally in combination with radiotherapy, radio-immunotherapy and/or tumour resection by surgery. |
