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Application of composition in preparation of drug for inhibiting 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: 2018-11-23
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 composition in preparation of drug for inhibiting gefitinib hepatotoxicity
  • Application of composition in preparation of drug for inhibiting gefitinib hepatotoxicity

Examples

Experimental program
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Effect test

Embodiment 1

[0013] Twelve female ICR mice were randomly divided into a control group and a gefitinib administration group, each with 6 mice. The control group was given the same amount of 0.9% normal saline; the gefitinib administration group was given gefitinib solution by gavage 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 their livers were cut out, and their organ coefficients were weighed to calculate their organ coefficients. The eyeballs were removed and blood was taken to detect the ALT and AST values ​​in the serum. The results showed that the liver organ coefficient of the gefitinib administration group was significantly increased, and the ALT and AST values ​​were significantly higher than those of 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

[0015] 24 female ICR mice were randomly divided into 4 groups, namely the blank control group, the gefitinib administration group, the BI-2536 administration group and the gefitinib+BI-2536 administration group, each with 6 mice. Gefitinib solution was administered intragastrically at a dose of 200 mg / kg / day, and / or BI-2536 solution was administered by intraperitoneal injection twice a week at a dose of 5 mg / kg for 4 weeks of continuous administration, and the mice’s performance was recorded daily body weight. After 4 weeks, the mice were sacrificed and their livers were cut out, and their organ coefficients were weighed to calculate their organ coefficients. The eyeballs were removed and blood was taken to detect the ALT and AST values ​​in the serum. It was found that BI-2536 can reverse the increase in liver organ coefficient caused by gefitinib. In addition, the ALT and AST values ​​of the gefitinib single-use group were significantly increased, and BI-2536 can reverse thi...

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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 the new use of PLK1 inhibitors, in particular to the application of a composition in the preparation of a drug for treating gefitinib liver toxicity, which can reduce the liver toxicity caused by gefitinib. Background technique [0002] Gefitinib is a tyrosine kinase molecular targeted 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, after the launch of gefitinib, reports of its clinical hepatotoxicity have emerged one after another, which has become one of the important obstacles restricting its long-term and safe clinical application. The severe liver toxicity caused by gefitinib can cause the patient to die not from the tumor but from the liver toxicity. At present, in response to this problem, ther...

Claims

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Application Information

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Patent Type & Authority Applications(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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