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Application of regorafenib and lapatinib in preparation of antitumor combination drug

A lapatinib and anti-tumor technology, which is applied in the field of anti-tumor drug preparation, can solve the problems such as the lack of combined use of regoratinib and lapatinib, and achieve the effects of superimposed curative effects, reduced dosage, and cost savings

Inactive Publication Date: 2016-02-24
JINAN UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] At present, there is no relevant literature report on the combined use of rigatinib and lapatinib

Method used

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  • Application of regorafenib and lapatinib in preparation of antitumor combination drug
  • Application of regorafenib and lapatinib in preparation of antitumor combination drug
  • Application of regorafenib and lapatinib in preparation of antitumor combination drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Example 1MTT method to detect the sensitivity of different tumor cells to rigatinib or lapatinib

[0037] Human colorectal cancer cells HCT116, SW620, HT29 and HCT8 were inoculated into 96-well plates with 5000-9000 cells per well. After the cells adhered to the wall, different concentrations of regoratinib or lapatinib were added respectively. of PBS solution. After culturing for 72 h, add 10 μL of MTT with a concentration of 5 mg / mL to each well and culture for another 4 h, then discard the culture solution and add 100 μL of DMSO to each well, and read the absorbance value of each well at 490 nm with a microplate reader. The half inhibitory concentration (IC50) was calculated by Bliss method. For specific results, see figure 1 .

[0038] From figure 1 It can be seen that the IC50 values ​​of rigatinib and lapatinib on different tumor cells are in a relatively small range, and the IC50 values ​​of rigatinib on different tumor cells are in the range of 15-25 μM , w...

Embodiment 2

[0039] Example 2 Effects of rigatinib or lapatinib alone and in combination on the survival rate of different tumor cells

[0040] Human colorectal cancer cells HCT116 and SW620 were inoculated into 96-well plates with 5000-9000 cells per well. After the cells adhered to the wall, PBS solutions with different ratios of rigatinib and lapatinib were added. . After culturing for 72 h, add 10 μL of MTT with a concentration of 5 mg / mL to each well and culture for another 4 h, then discard the culture solution and add 100 μL of DMSO to each well, and read the absorbance value of each well at 490 nm with a microplate reader. CompuSyn software was used for synergy comprehensive factor (Combinationindex, CI) analysis. see results figure 2 and Table 1, figure 2 It shows the cell viability of HCT116 and SW620 after combined treatment with different drug concentrations.

[0041]The CI value represents a composite index when the drug is combined, and the CI value is less than, equal ...

Embodiment 3

[0044] Example 3 Effects of rigatinib and lapatinib on the cell cycle of HCT116 and SW620 cells after separate and combined use

[0045] The cell cycle arrest of colorectal cancer cells HCT116 and SW620 induced by rigatinib and lapatinib alone and in combination was detected by flow cytometry. HCT116 and SW620 cells were divided into 3 × 10 per well 5 Cells were inoculated into 6-well plates at a density of 1000000000000000000000000000000000000000000000000000000000000000000000000000000000000000000000000000000000000000000 plate, after the cells adhered to the wall, the HCT116 and SW620 cells were divided into four experimental groups, and the following solutions were added respectively: the first group was the control group without treatment; Gritinib alone treatment group (3 μM, 10 μM, 30 μM three gradients); the third group was lapatinib single treatment group (3 μM, 10 μM, 30 μM three gradients); the fourth group was regatitinib Ni and lapatinib combined treatment group (co...

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Abstract

The invention belongs to the technical field of preparation of antitumor drugs and particularly relates to application of regorafenib and lapatinib in the preparation of an antitumor combination drug. The combination drug of regorafenib and lapatinib is significant in causing tumor cell cycle arresting, thus arresting tumor cells in the stage G0 / G1 and inhibiting the development of colon cancer; the ability to kill tumor cells can be effectively improved, and tumor cell apoptosis can be greatly promoted. The regorafenib and lapatinib are significant in synergistic action, effectively improving the curative effect, and has more significant effect than the single effect of a single component or double components, thus improving the ability to kill tumor cells; usage of the regorafenib and lapatinib is effectively reduced, thus reducing toxic or side effect. The combined use of the regorafenib and lapatinib can also save the cost and relieve the economic burden of a patient, a new way to control tumors is provided, and this drug has a promising application prospect in the field of medicine.

Description

technical field [0001] The invention belongs to the technical field of preparation of anti-tumor drugs, and in particular relates to the application of regoratinib and lapatinib in the preparation of combined anti-tumor drugs. Background technique [0002] With the development of tumor molecular biology, tumor chemotherapy has entered the era of molecular targeted therapy, and a new generation of anti-tumor drugs targeting molecular targets will become another major direction of tumor treatment by virtue of their specificity and targeting. Multi-target inhibitors are superior to single-target inhibitors in treatment, and multi-target combined blockade of signal transduction is a new development direction for tumor therapy and drug development. [0003] Combined drug therapy is one of the hot spots in the field of tumor chemotherapy in recent years. A large number of clinical and experimental studies have proved that combined drug therapy has special effects in the prevention...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/517A61P35/00A61K31/44
Inventor 石智张文姬陈耀魏梦宁邱建阁蒋起韦覃武明杨阳郑迪威
Owner JINAN UNIVERSITY
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