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Use of lapatinib for reversing multi-drug resistance of tumor

A drug-resistant, tumor cell technology, applied in the field of lapatinib, can solve problems such as affecting function

Inactive Publication Date: 2009-04-15
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Recently, it has been reported that the compound OC144-093 has a strong reversal activity and may not be a substrate of P-pg. Its mechanism of action is mainly to bind with P-gp, thereby affecting the "drug pump" function of P-gp

Method used

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  • Use of lapatinib for reversing multi-drug resistance of tumor
  • Use of lapatinib for reversing multi-drug resistance of tumor
  • Use of lapatinib for reversing multi-drug resistance of tumor

Examples

Experimental program
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Effect test

Embodiment Construction

[0016] 1. Lapatinib reverses MDR in vitro

[0017] Multiple pairs of characteristic cell lines include multidrug-resistant cell lines and their corresponding sensitive lines KBv200 and KB, MCF-7 / adr and MCF-7, KB-CV60 and KB-3-1, SW1573 / 2R-120 and SW1573 , S1-M1-80 and S1 cells, and MTT method was used to study the effect of Lapatinib on reversing MDR in vitro. In the presence of lapatinib or no lapatinib, the cells in the logarithmic growth phase were treated with different concentrations of the test drug for 72 hours, and the absorbance was measured. The concentration of the drug that inhibited cell growth up to 50% was calculated respectively, expressed as IC50 value. The reversal factor was IC50 (chemotherapy drug) / IC50 (chemotherapy drug+lapatinib). The results are shown in Table 1, figure 1 shown. The results showed that Lapatinib had strong MDR-reversal activity against a variety of multidrug-resistant cell lines, and even at a low concentration of 0.625 μmol / L, the...

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Abstract

The invention relates to the multi-drug resistance (MDR) of Lapatinib (formula 1) in reversing tumour cells which are mediated by membrane transport proteins (ABC) families such as P-glycoprotein (P-gp), multi-drug resistance related protein (MRP1), breast cancer multi-drug resistance related proteins (ABCG2 and BCRP) and the like. The Lapatinib is used together with anti-cancer drugs such as anthracyclines, catharanthines, taxols, podophyllotoxins, camptothecins and the like to restore the sensitivity of MDR tumor cells to the anticancer drugs. The Lapatinib is applied to combination chemotherapy of drug-resistant patients in clinical chemotherapy or the prevention of drug-resistance generation for the tumor cells.

Description

[technical field] [0001] The present invention relates to a new application of lapatinib, specifically, lapatinib is used to reverse multidrug resistance (MDR) of tumor cells and restore the sensitivity of MDR tumor cells to anticancer drugs. [Background technique] [0002] Tumor is the main disease that threatens human life and health, and is the second killer of human beings. The main means of treating tumors are surgery, radiotherapy and chemotherapy. Both surgery and radiotherapy cannot remove all tumor cells accurately and tend to recur after treatment, so it is a local treatment. Chemotherapy is a systemic treatment, but the main reasons for the failure of chemotherapy are: first, dose-limiting toxic and side effects. Due to the low selectivity of anticancer drugs to tumor cells, they also have a killing effect on normal tissue cells while killing tumor cells, which limits the application dose of anticancer drugs. Second, tumor cells develop resistance to anticancer...

Claims

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Application Information

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IPC IPC(8): A61K31/517A61P35/00A61P43/00
Inventor 符立梧梁永钜
Owner SUN YAT SEN UNIV
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