Application of EGFR/HER2 (epidermal growth factor receptor/type-2 human epidermal growth factor receptor) receptor tyrosine kinase inhibitors to preparing medicines for treating cancer

A technology for use and cancer, applied in drug combinations, antibodies, anti-tumor drugs, etc., can solve the problems of undisclosed cancer use of the compound of formula I, combined use of antibody-drug conjugates with undisclosed anti-HER2 effects, etc.

Active Publication Date: 2018-01-30
JIANGSU HENGRUI MEDICINE CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0015] However, none of the above documents discloses the use of the compound of formula I for the treatment of cancers that have failed or resistant to anti-HER2 treatment, nor discloses the combined use of the compound of formula (I) and the antibody-drug conjugate with anti-HER2 effect

Method used

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  • Application of EGFR/HER2 (epidermal growth factor receptor/type-2 human epidermal growth factor receptor) receptor tyrosine kinase inhibitors to preparing medicines for treating cancer
  • Application of EGFR/HER2 (epidermal growth factor receptor/type-2 human epidermal growth factor receptor) receptor tyrosine kinase inhibitors to preparing medicines for treating cancer
  • Application of EGFR/HER2 (epidermal growth factor receptor/type-2 human epidermal growth factor receptor) receptor tyrosine kinase inhibitors to preparing medicines for treating cancer

Examples

Experimental program
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Embodiment 1

[0027]Example 1: The effect of compound (I), T-DM1 alone or both in combination on Herceptin drug-resistant human breast cancer BT-474 / T721 subcutaneously transplanted tumors in nude mice

[0028] 1. Test drugs

[0029] Drug name and batch number: Compound (I) is a yellow powder with a content of 98.8%, batch number S0915100514; T-DM1 is a white freeze-dried powder, specification 80mg / bottle, batch number P07A113010711.

[0030] Drug source: Compound (I) is administered in the form of its dimaleate, which is prepared according to the method disclosed in CN102933574B; T-DM1 is prepared according to the method disclosed in CN101087611A.

[0031] Preparation method: Compound (I) was prepared with distilled water; T-DM1 was first reconstituted with distilled water to form a 20 mg / ml solution, subpackaged and stored at -80°C, and diluted with 0.1% BSA saline to the corresponding concentration before use.

[0032] 2. Experimental animals

[0033] BALB / cA-nude nude mice, 6-7 weeks ...

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Abstract

The invention relates to application of EGFR / HER2 (epidermal growth factor receptor / type-2 human epidermal growth factor receptor) receptor tyrosine kinase inhibitors to preparing medicines for treating cancer, and particularly relates to application of compounds of EGFR / HER2 receptor tyrosine kinase inhibitors to preparing anti-HER2 medicines for treating medicine-resistant cancer. The compoundsof the EGFR / HER2 receptor tyrosine kinase inhibitors are shown as a formula (I).

Description

technical field [0001] The invention relates to the use of an EGFR / HER2 receptor tyrosine kinase inhibitor in the preparation of a drug for treating drug-resistant cancers resistant to HER2 therapy. Background technique [0002] Breast cancer is one of the most common malignant tumors in women. According to the statistics of the World Health Organization, about 1.2 million women are diagnosed with breast cancer every year in the world, and the annual incidence of breast cancer is increasing at a rate of 5% to 20%. [0003] Its incidence is often related to genetics, and the incidence rate of women between the ages of 40 and 60 and before and after menopause is higher. Only about 1 to 2% of breast cancer patients are men. Malignant tumors usually occurring in the glandular epithelium of the breast. It is one of the most common malignant tumors that seriously affects women's physical and mental health and even threatens their lives. [0004] It is known that there are many...

Claims

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Application Information

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IPC IPC(8): A61K31/4709A61K45/06A61K39/395A61P35/00
Inventor 杨昌永曹国庆唐蜜孙星孙扬飞张连山
Owner JIANGSU HENGRUI MEDICINE CO LTD
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