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New medical application of Elvitegravir for alleviating irinotecan toxicity

A technology of irinotecan and other uses, which is applied in the field of anti-HIV integrase inhibitors, and can solve the problems of increasing tumor patients

Inactive Publication Date: 2017-10-24
BINZHOU MEDICAL COLLEGE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Detegravir (dolutegravir, ) is an integrase inhibitor approved by the US FDA. The dose is 50mg, once a day. It can rapidly inhibit HIV replication. Or treatment-naïve HIV-1 adults and children aged 12 and over with a body weight of at least 40 kg, but detegevir and the antineoplastic drug irinotecan or its active metabolite 7-ethyl-10-hydroxycamptothecin (SN- 38) Combined use, prevention or treatment to reduce the toxicity 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 risk of cancer patients Physical fitness, 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 Effect of anti-HIV protease inhibitor Detegravir on toxicity caused by irinotecan administration

[0007] 1.1 Drugs and reagents

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

[0009] Irinotecan hydrochloride (purity 99.5%, purchased from Shanghai Hanxiang Biotechnology Co., Ltd.)

[0010] 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.

[0011] 1.2 Experimental methods and results

[0012] 1.2.1 Preparation, grouping and administration of toxicity model mice caused by continuous administration of irinotecan

[0013] 60 male mice, weighing 20-22g, were divided into 6 groups, namely normal group, irinotecan group, irinotecan + detegravir 5mg / kg group, irinotecan + detegravir 25mg / kg group, irinotecan...

experiment example 2

[0022] Experimental Example 2 Effect of Anti-HIV Protease Inhibitor Detegravir on the Survival Period of Tumor-bearing Nude Mice Taking Irinotecan

[0023] 2.1 Drugs and reagents

[0024] Detegravir ethanolate (purity 99.5%, purchased from Shanghai Hanxiang Biotechnology Co., Ltd.)

[0025] Ritonavir (purity 99.4%, purchased from Shanghai Hanxiang Biotechnology Co., Ltd.)

[0026] Irinotecan hydrochloride (purity 99.5%, purchased from Shanghai Hanxiang Biotechnology Co., Ltd.)

[0027] 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.

[0028] 2.2 Experimental methods and results

[0029] 2.2.1 Grouping and administration of tumor-bearing nude mice with continuous administration of irinotecan

[0030] 60 tumor-bearing nude mice, weighing 20-22g, were divided into 6 gro...

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PUM

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Abstract

The present invention provides the use of anti-HIV integrase inhibitor Detegravir in the prevention or / and treatment of delayed diarrhea caused by an anti-tumor drug, and the use of a drug for intestinal dysfunction caused by diarrhea, wherein the anti- Oncology drug refers to irinotecan or its active metabolite 7‑ethyl‑10‑hydroxycamptothecin (SN‑38). In the present invention, detegevir has clear pharmacological effects, can effectively relieve delayed diarrhea, and protect intestinal function.

Description

technical field [0001] The invention belongs to the field of chemical medicine, and specifically relates to the combined use of an anti-HIV integrase inhibitor detegravir and an antitumor drug irinotecan to reduce the toxic reaction of irinotecan and increase the physique of tumor patients, that is, to improve the tolerance of tumor patients to irinotecan. The dosage of rinotecan can 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 hydrochloride in...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/5365A61K31/4745A61P1/12A61P1/00A61P35/00
CPCA61K31/5365A61K31/4745
Inventor 蒋王林张广华张雪李德芳
Owner BINZHOU MEDICAL COLLEGE