Method for treating cancer harboring EGFR mutations

Abstract

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.

Description

[0001] The present invention relates to a method of treating a patient suffering from cancer and carrying a mutation in the EGFR gene in the tumor. The method comprises administering to a human in need thereof an effective amount of an irreversible EGFR inhibitor BIBW2992 ( 1 ), optionally in combination with other chemotherapeutic agents ( 2 ), and optionally in combination with radiotherapy, radioimmunotherapy and / or tumor surgical resection (tumor insection by surgery). The EGFR mutations include at least all amplifications or increased expression (such as CA-repeated (CA: cytosine-adenosine) reduction in the first intron or other specific polymorphisms), sensitivity to activation Activating gene mutations associated with sex gain or genuinely activating mutations (such as L858R or G719S point mutations or specific exon 19 deletions). It also includes those mutations associated with resistance (e.g. D761Y, insertion D770_N771insNPG) or acquired resistance (e.g. T790M) to tr...

AI Technical Summary

Problems solved by technology

The precise mechanism of the RESSA response is not fully understood, however, studies have shown that the presence of EGFR is a prerequisite for its action

[0007] A significant limitation of the use of these compounds is that their recipients may develop resistance to their therapeutic effects after initially responding to treatment, or they may not respond to EGFR-tyrosine kinase inhibitors at all to any measurable extent (TKI)

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