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Application of a composition in the preparation of drugs for the treatment of gefitinib hepatotoxicity

A technology of gefitinib and composition, applied in the field of application of composition in the preparation of drugs for the treatment of gefitinib hepatotoxicity

Active Publication Date: 2020-06-05
INNOVATION INST FOR ARTIFICIAL INTELLIGENCE IN MEDICINE OF ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

So far there is no report on its protective effect against gefitinib-induced hepatotoxicity

Method used

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  • Application of a composition in the preparation of drugs for the treatment of gefitinib hepatotoxicity
  • Application of a composition in the preparation of drugs for the treatment of gefitinib hepatotoxicity
  • Application of a composition in the preparation of drugs for the treatment of gefitinib hepatotoxicity

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Experimental program
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Effect test

Embodiment 1

[0014] Twelve female ICR mice were randomly divided into control group and gefitinib-administered group, with 6 mice in each group. The control group was given the same amount of 0.9% normal saline; the gefitinib treatment group was given gefitinib solution by intragastric administration at a dose of 200 mg / kg / day for 4 consecutive weeks, and the body weight of the mice was recorded every day. After 4 weeks, the mice were sacrificed and the liver was dissected, weighed to calculate the organ coefficient, and the eyeballs were removed to obtain blood, and the ALT and AST values ​​in the serum were detected. It was found that the organ coefficient of the liver in the gefitinib administration group was significantly increased, and the ALT and AST values ​​were significantly higher than those in the control group. It shows that gefitinib can cause abnormal liver function in mice and has significant liver toxicity. See results figure 1 .

Embodiment 2

[0016] Twenty-four female ICR mice were randomly divided into 4 groups, namely blank control group, gefitinib-administered group, BI-2536-administered group and gefitinib+BI-2536-administered group, with 6 mice in each group. Oral administration of gefitinib solution at a dose of 200 mg / kg / day, and / or intraperitoneal injection of BI-2536 solution twice a week at a dose of 5 mg / kg for 4 consecutive weeks, and daily record of mice weight. After 4 weeks, the mice were sacrificed and the liver was dissected, weighed to calculate the organ coefficient, and the eyeballs were removed to obtain blood, and the ALT and AST values ​​in the serum were detected. It was found that BI-2536 could reverse the increase in liver organ coefficient caused by gefitinib. In addition, the ALT and AST values ​​of the gefitinib monotherapy group were significantly increased, and BI-2536 can reverse this change to a certain extent, suggesting that BI-2536 can intervene in the decline of liver function ...

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Abstract

The invention provides application of a composition in preparation of a drug for inhibiting gefitinib hepatotoxicity. The composition consists of a PLK1 inhibitor BI-2536 and the gefitinib, wherein adose ratio of the gefitinib to the BI-2536 is 40:1. In vitro and in vivo studies have shown that PLK1 inhibitor BI-2536 has a significant protective effect on liver toxicity induced by the gefitinib.The PLK1 inhibitor can be used for preventing and reducing gefitinib-induced hepatotoxicity, thereby expanding the clinical application of the gefitinib. The significance of the composition is to provide an effective gefitinib liver toxicity-resisting protective agent against gefitinib-induced hepatotoxicity. A in vivo experimental study proves that the composition has a significant protective effect against liver toxicity caused by the gefitinib, thus expanding the clinical application range of the gefitinib, reducing the liver toxicity caused by the gefitinib in a cancer patient, and providing a brand-new liver toxicity protection mechanism.

Description

technical field [0001] The invention belongs to the field of medicine and relates to a new application of a PLK1 inhibitor, in particular to an application of a composition in the preparation of a drug for treating hepatotoxicity of gefitinib, which can alleviate the hepatotoxic effect caused by gefitinib. Background technique [0002] Gefitinib belongs to the tyrosine kinase molecular targeting drug and is currently the first-line drug for advanced non-small cell lung cancer. Because of its effectiveness and compliance advantages, gefitinib has become one of the most widely used molecular targeted drugs in clinical practice. However, reports of clinical hepatotoxicity of gefitinib have emerged one after another after it was launched on the market, which has become one of the important obstacles limiting its long-term clinical application. Severe liver toxicity caused by gefitinib can lead to death of patients not from tumors but from liver toxicity. At present, there is n...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/525A61K31/5377A61P1/16A61P35/00
CPCA61K31/525A61K31/5377A61P1/16A61P35/00A61K2300/00
Inventor 罗沛华何俏军杨波
Owner INNOVATION INST FOR ARTIFICIAL INTELLIGENCE IN MEDICINE OF ZHEJIANG UNIV
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