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Pharmaceutical application of mTOR inhibitor and pharmaceutical composition of mTOR inhibitor

A technology of inhibitors and compositions, applied in the direction of drug combinations, pharmaceutical formulations, antineoplastic drugs, etc., can solve problems such as relationships that have not been reported, and achieve the best drug effect

Inactive Publication Date: 2022-06-21
德琪(浙江)医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the function of its mutations in tumorigenesis and the relationship with drug efficacy have not been reported yet.

Method used

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  • Pharmaceutical application of mTOR inhibitor and pharmaceutical composition of mTOR inhibitor
  • Pharmaceutical application of mTOR inhibitor and pharmaceutical composition of mTOR inhibitor
  • Pharmaceutical application of mTOR inhibitor and pharmaceutical composition of mTOR inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1A

[0071] Example 1 Inhibitory effect of ATG-008 on various lung cancer cells

[0072] The inventors have tested the tumor suppressive effect of ATG-008 in various lung cancer cell lines, and found that ATG-008 can effectively inhibit the proliferation, self-renewal and self-renewal of MUC5B gene-mutated lung cancer cells compared with MUC5B wild-type cells. Invasion ability. The plan is as follows:

[0073] experiment method:

[0074] 1. Cell Culture

[0075] Cells were recovered and cultured in their respective medium.

[0076] 2. Cell plating (Day 1):

[0077] 2.1 Harvest cells in logarithmic growth phase and count cells using a cell counter. Cell viability was detected by trypan blue exclusion method to ensure that the viability of each cell line was above 80%.

[0078] 2.2 Dilute and adjust the cell concentration with culture medium, add 90 μL of cell suspension to the 96-well cell plate (including the cell control T0 on the day of drug treatment), so that the cell den...

Embodiment 2

[0115] Example 2 ATG-008 significantly inhibits tumors with MUC5B gene mutation

[0116] ATG-008 significantly inhibited the growth of tumors carrying MUC5B gene mutation in a mouse heterotopic tumor model, and the drug efficacy was better than that of the MUC5B wild-type tumor model.

[0117] 1. The experimental design is shown in Table 2 below:

[0118] Table 2 Mode of administration

[0119]

[0120] 2. Cell culture and transfer

[0121] Experimental animals: BALB / c Nude mice, female, were purchased from Jiangsu Jicui Yaokang Biotechnology Co., Ltd., production license number: SCXK (Su) 2018-0008. Breeding environment: SPF grade.

[0122] Environmental conditions of the experimental animal breeding room: the experimental animals are kept in an independent ventilation box with constant temperature and humidity, the temperature of the breeding room is 20-26 ℃, the humidity is 40-70%, the ventilation is 10-20 times / hour, and the light and dark alternating time of day and...

Embodiment 3

[0144] Example 3 Frequency analysis of MUC5B gene mutation in various tumors

[0145] Using the TCGA database analysis, it was demonstrated that MUC5B occurs at a high frequency in multiple tumor types, such as Figure 8 shown. From high to low are melanoma, endometrial cancer, colorectal cancer, esophageal adenocarcinoma, cervical cancer, non-small cell lung cancer, B-cell lymphoma, head and neck cancer, bile duct cancer, bladder and urinary tract cancer, stomach cancer, esophagus Squamous cell carcinoma, liver cancer, sarcoma, breast cancer, glioma and kidney cancer, etc.

[0146] These data indicate that the mTOR inhibitor ATG-008 of the present application can be used for the precise treatment of various tumors related to MUC5B gene mutation, thereby further improving the clinical treatment effect.

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Abstract

The invention provides pharmaceutical application of an mTOR inhibitor and a pharmaceutical composition of the mTOR inhibitor, namely application of the mTOR inhibitor in preparation of a medicine for preventing and / or treating tumors with MUC5B gene mutation. And a pharmaceutical composition for preventing and / or treating tumors with MUC5B gene mutation, which contains an effective amount of mTOR inhibitor for prevention and / or treatment and a reagent for detecting MUC5B gene mutation. The inventor finds that compared with a MUC5B wild type tumor cell line, the tumor cell line with MUC5B gene mutation is highly sensitive to an mTOR C1 / 2 inhibitor Onatassertib (ATG-008), and the ATG-008 shows an excellent drug effect in a mouse ectopic transplantation tumor model with MUC5B gene mutation.

Description

technical field [0001] The present invention relates to the field of medicines for preventing and / or treating tumors. Specifically, the present invention relates to the use of mTOR inhibitors in the preparation of medicaments for preventing and / or treating tumors, especially tumors with MUC5B gene mutation, and the use of mTOR inhibitors for preventing and / or treating tumors, especially It is a pharmaceutical composition for tumors with MUC5B gene mutation. Background technique [0002] The phosphoinositide 3-kinase (PI3K) / protein kinase B (proteinkinase B, PKB or AKT) signaling pathway is associated with tumorigenesis. The mammalian target of rapamycin (mTOR), as an important serine-threonine protein kinase downstream of PI3K / Akt, regulates the proliferation, survival, invasion and metastasis of tumor cells by activating ribosomal kinases. During tumorigenesis, the AKT / mTOR pathway is often highly activated. Various mTOR inhibitors, such as rapamycin, everolimus, and the...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K45/00A61K31/4985A61P35/00
CPCA61K45/00A61K31/4985A61P35/00
Inventor 侯冰单波梅建明谢辉王爱华
Owner 德琪(浙江)医药科技有限公司
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