Method for treating cancer harboring egfr mutations

A - Human Necessities – 61 – K

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A61K 31/517 (2006.01) A61P 35/00 (2006.01)

Patent

CA 2663599

The present invention relates to a method of treatment of patients suffering from cancer and harbouring mutations of EGFR in the tumour, 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 effect ive 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 tumour 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 harbouring mutations of EGFR in the tumour.

La présente invention concerne un procédé de traitement de patients souffrant de cancer et présentant des mutations de l'EGFR dans la tumeur; il peut s'agir par exemple d'une mutation d'activation de l'EGFR ou d'une mutation responsable de la résistance ou de l'émergence d'une résistance acquise aux traitements utilisant des inhibiteurs réversibles de l'EGFR et/ou du HER2, ou des inhibiteurs irréversibles, tels que CI-1033, EKB-569, HKI-272 ou HKI-357. Ledit procédé consiste à administrer une quantité efficace de l'inhibiteur irréversible de l'EGFR, BIBW2992, (1) 4-[(3-chloro-4-fluorophényle)amino]-6-{[4-(N,N-diméthylamino)-1-oxo-2-butén-1-yle]amino}-7-((S)-tétrahydrofuran-3-yloxy)-quinazoline, à une personne ayant besoin d'un tel traitement. Cet inhibiteur est éventuellement associé à l'administration d'un autre agent chimiothérapeutique, en combinaison avec la radiothérapie, la radio-immunothérapie et/ou la résection tumorale par chirurgie. La présente invention concerne également l'utilisation de BIBW 2992 (1) dans la préparation d'une composition pharmaceutique destinée au traitement de patients souffrant de cancer et présentant des mutations de l'EGFR dans la tumeur.

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