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Itraconazole applied to treatment of malignant tumor or salt thereof and composition thereof

A technology for itraconazole and malignant tumors, applied in the field of tumor treatment, can solve the problem of not finding the use of itraconazole for tumors, and achieve the effect of slowing down the growth rate of tumors and reducing the size of tumors

Inactive Publication Date: 2013-04-17
万礼 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] After that, pharmaceutical workers including the applicant did in-depth research on the conventional dose of itraconazole, but did not find other tumor uses of itraconazole

Method used

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  • Itraconazole applied to treatment of malignant tumor or salt thereof and composition thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Embodiment 1 in vivo anti-liver cancer test

[0022] 1. Animals

[0023] Fifty-two SPF grade Kunming mice inoculated with liver cancer H22, aged 5-6 weeks and weighing 18-22 grams, were purchased from Harlan Company in the Netherlands.

[0024] Test drug: inject itraconazole (produced by SIGMA Company of the United States), and dissolve itraconazole in dimethyl sulfoxide (produced by SIGMA Company of the United States) to make a solution.

[0025] 2. Grouping

[0026] Randomly divided into itraconazole high-dose group (15mg / kg), itraconazole low-dose group (30mg / kg), itraconazole combination (20mg / kg itraconazole+10mg / kg bortezomib ) group and 4 groups of model control group, half male and half male, fed in separate cages.

[0027] 3. Detection indicators

[0028] The general condition of the animals was observed daily. On the next day after drug withdrawal, blood was collected from the orbit to prepare serum for detection of ALT, AST, TP and ALB. The mice were ki...

Embodiment 2

[0030] Example 2 In vivo anti-lung cancer test

[0031] 1. Animal C57B / 6 mouse, female, 18-22g; tumor line Lewis lung cancer cells

[0032] 2. Method

[0033] Lewis lung cancer cells were ground into a cell homogenate with physiological saline, and the cell number was adjusted to 5×106 / ml, and 0.2ml / only was inoculated subcutaneously in the armpit of the right forelimb of 30 C57BL / 6 mice, and grouped after the tumor grew about 0.5g Administration: control group: paclitaxel (10ml / kg); test group 1: itraconazole (30mg / kg); test group 2: itraconazole composition (20mg / kg itraconazole + 10mg / kg boron Tezomib) group. There were 10 mice in each group, and each group was administered once a day for 8 consecutive days. From the day of administration, the tumor diameter was measured every 1 d. The mice were sacrificed the next day after the treatment, the tumors were peeled off, weighed, and the tumor inhibition rate was calculated according to the formula.

[0034] Tumor inhibiti...

Embodiment 3

[0037] Example 3 Anti-gastric cancer test in vivo

[0038] 1 Reagent Goat anti-human CD34 antibody and VEGF antibody.

[0039] 2 Animal model Healthy male NOD SCID mice, aged 6-7 weeks, weighing 20-25g. The human gastric cancer cell line SGC7901 passaged subcutaneously in nude mice was sacrificed during transplantation, the skin was disinfected, the tumor was removed, and immersed in 0.9% sodium chloride solution. The gastric cancer orthotopic transplantation model was established by orthotopic transplantation of human gastric cancer tissue into NOD SCID mice. After the animal was anesthetized, the gastric wall was exposed, and the gastric serosa layer was injured with scissors in the middle of the greater curvature of the stomach, and the human gastric cancer tissue block (about 150 mg) was sewn on At the injured site, the abdominal wall and skin were sutured.

[0040] After the model was established, the mice were divided into itraconazole group (n=20), itraconazole compos...

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Abstract

The invention relates to itraconazole applied to treatment of gastric cancer, lung cancer and liver cancer, and a composition of the itraconazole. The daily dose of the itraconazole is 0.1-5000mg, and the itraconazole has good curative effect when the daily dose is 200mg. The itraconazole and the composition of the itraconazole disclosed by the invention have the beneficial effects that by subcutaneous injection of the itraconazole solution or the composition, the survival time of high and low-dose groups of SPF-grade Konmin mice that have liver cancer H22 can be prolonged. The itraconazole or the composition of the itraconazole has obvious inbibitional effect on Lewis lung cancer of mice in comparison with the control group according to the influence on subcutaneous tumor of the Lewis lung caner, the growth rate (P(0.01) of the tumor can be slowed down; the size (P(0.01) of the tumor is reduced; and the tumor control rate is respectively 43.0% and 45.6% after the treatment is ended. The itraconazole or the composition of the itraconazole influences positive staining of the human gastric cancer tissue VEGF (Vascular Endothelial Growth Factor) in cell cytoplasm, and the VEGF positive expression of a 0.9% sodium chloride solution group is obviously higher than that of the itraconazole group (P(0.05).

Description

technical field [0001] The invention belongs to the field of tumor treatment, in particular to itraconazole and its composition used in the treatment of gastric cancer, lung cancer and liver cancer. Background technique [0002] Itraconazole is a synthetic azole broad-spectrum antifungal drug, used for systemic infections caused by deep fungi, and can also be used for candidiasis and aspergillosis. [0003] Chemical name: cis-4-[4-[4-[4-[[2-(2,4-dichlorophenyl)-2-(1H-1,2,4-triazolyl-1-methanol base) [0004] The structural formula is: [0005] [0006] Itraconazole belongs to triazole broad-spectrum antifungal drugs, and its dosage forms include intravenous preparations, oral capsules and oral liquids. Previously, the applicant accidentally discovered the use of itraconazole for treating multiple myeloma, and applied for Chinese patent CN2011100299861 in 2011. [0007] Afterwards, pharmaceutical workers including the applicant conducted in-depth research on the conven...

Claims

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Application Information

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IPC IPC(8): C07D405/14A61K38/05A61K31/496A61P35/00
Inventor 万礼杨烨
Owner 万礼
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