Novel medicine use of lopinavir in alleviating toxicity of irinotecan

A technology of irinotecan and application, which is applied in the direction of medical preparations containing active ingredients, pharmaceutical formulas, drug combinations, etc., and can solve the problems of increasing the physique of tumor patients

Inactive Publication Date: 2017-12-29
BINZHOU MEDICAL COLLEGE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Clinically, the anti-HIV protease inhibitor (protease inhibitor) lopinavir is suitable for use in combination with other antiretroviral drugs to treat human immunodeficiency virus-1 (HIV-1) infection in adults and children over 2 years old, but Anti-HIV protease inhibitor lopinavir alone or the combination of lopinavir and ritonavir and antineoplastic drug irinotecan or its active metabolite 7-ethyl-10 hydroxycamptothecin (SN-38 ) combined use, prevent or treat to reduce the toxic reaction of irinotecan or SN-38, reduce the diarrhea caused by irinotecan or SN-38, reduce the decrease in diet due to intestinal dysfunction caused by diarrhea, and increase the physical fitness of tumor patients , improving the dose of irinotecan or SN-38 used by tumor patients and prolonging the time of using irinotecan or SN-38 in tumor patients has not been reported

Method used

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Examples

Experimental program
Comparison scheme
Effect test

experiment example 1

[0006] Experimental example 1 The effect of anti-HIV protease inhibitor lopinavir on the toxicity caused by irinotecan administration

[0007] 1.1 Drugs and reagents

[0008] Lopinavir (purity 99.5%, purchased from Shanghai Hanxiang Biotechnology Co., Ltd.)

[0009] Ritonavir (purity 99.4%, purchased from Shanghai Hanxiang Biotechnology Co., Ltd.)

[0010] Irinotecan hydrochloride (purity 99.5%, purchased from Shanghai Hanxiang Biotechnology Co., Ltd.)

[0011] Experimental animals: SPF grade C57 mice, male, weighing 20g-22g, provided by the Experimental Animal Center of Beijing Weitong Lihua Experimental Animal Technology Co., Ltd., the animal qualification certificate number is: SCXK (Beijing) 2012-0001.

[0012] 1.2 Experimental methods and results

[0013] 1.2.1 Preparation, grouping and administration of toxicity model mice caused by continuous administration of irinotecan

[0014] 70 male mice, weighing 20-22g, were taken and divided into 7 groups, namely normal grou...

experiment example 2

[0023] Experimental example 2 Effect of anti-HIV protease inhibitor lopinavir on survival of tumor-bearing nude mice treated with irinotecan

[0024] 2.1 Drugs and reagents

[0025] Lopinavir (purity 99.5%, purchased from Shanghai Hanxiang Biotechnology Co., Ltd.)

[0026] Ritonavir (purity 99.4%, purchased from Shanghai Hanxiang Biotechnology Co., Ltd.)

[0027] Irinotecan hydrochloride (purity 99.5%, purchased from Shanghai Hanxiang Biotechnology Co., Ltd.)

[0028] Experimental animals: BALB / c nude mice SPF grade, male, weighing 20g-22g, provided by the Experimental Animal Center of Beijing Weitong Lihua Experimental Animal Technology Co., Ltd., the animal qualification certificate number is: SCXK (Beijing) 2012-0001.

[0029] 2.2 Experimental methods and results

[0030] 2.2.1 Grouping and administration of tumor-bearing nude mice with continuous administration of irinotecan

[0031] 70 tumor-bearing nude mice, weighing 20-22g, were taken and divided into 7 groups, nam...

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PUM

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Abstract

The present invention provides anti-HIV protease inhibitor lopinavir alone or the combination of lopinavir and ritonavir in the prevention or / and treatment of delayed diarrhea caused by an antineoplastic drug, diarrhea caused intestinal Use in drugs for dysfunction, wherein the antineoplastic drug refers to irinotecan or its active metabolite 7-ethyl-10-hydroxycamptothecin (SN-38). In the present invention, lopinavir has clear pharmacological effects, can effectively alleviate delayed diarrhea, and protect intestinal function.

Description

technical field [0001] The invention belongs to the field of chemical medicine, and specifically relates to anti-HIV protease inhibitor lopinavir used alone or a combination of lopinavir and ritonavir combined with antitumor drug irinotecan to reduce the toxic reaction of irinotecan , increase the physique of tumor patients, that is, increase the dosage of irinotecan tolerated by tumor patients, and prolong the time of using irinotecan for tumor patients. Background technique [0002] Irinotecan is clinically used for the treatment of advanced colorectal cancer, combined with 5-fluorouracil and leucovorin (LV) to treat patients with advanced colorectal cancer who have not received chemotherapy before; as a single drug, to treat patients who have failed treatment with 5-fluorouracil-containing chemotherapy regimens . Irinotecan Hydrochloride 180mg / m 2 Intravenous infusion for 30-90 minutes, the first day; LV 400mg / m 2 It should be administered immediately after irinotecan ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/513A61K31/4745A61P35/00A61P1/12
CPCA61K31/513A61K31/4745
Inventor 蒋王林张广华张雪李德芳
Owner BINZHOU MEDICAL COLLEGE
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