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New application of sorafenib, regorafenib and analogues or derivatives thereof

A technology of regorafenib and its analogues, applied in the field of medicine, can solve the problems of high cost of bone marrow transplantation and lack of good therapeutic drugs, and achieve the effects of good clinical patient tolerance, light side effects, and low cost

Active Publication Date: 2020-11-03
THE SECOND XIANGYA HOSPITAL OF CENT SOUTH UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

This patented technology allows researchers to study different types of cancer like Polycythaemophilia Verruca (PV), Clinicists have found ways to make medicine better against certain forms of blood cell abnormalities such as PV monoclonal gammaglobulins. They also discovered how these chemicals could help reduce harm caused by other therapies used on older people who had developed this type of disease earlier.

Problems solved by technology

This patents describes various methods for identifying individuals likely to develop multiple forms of MPT associated pathologies like Polycline Leukaemesis Syndrome (PMWS)/Mycoblastic Langer Neurorvoked Disease (MCLND)). However, these techniques may result in delayed responses from certain time points during diagnosis leading to poor outcomes despite optimal chemotherapies. Therefore, new effective agents targeting specific molecular targets would provide better options for those affected by low-grade MPEs.

Method used

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  • New application of sorafenib, regorafenib and analogues or derivatives thereof
  • New application of sorafenib, regorafenib and analogues or derivatives thereof
  • New application of sorafenib, regorafenib and analogues or derivatives thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Embodiment 1, the establishment of two common drug-resistant cell models (HEL PE , HEL RE ).

[0046] 1. Materials and methods

[0047] 1. Cell line

[0048] HEL (Human erythroleukemia cell line) and drug-resistant HEL cells were cultured in RPMI medium (Gibco) containing 20% ​​heat-inactivated fetal bovine serum (Gibco) and 1% penicillin / streptomycin (Gibco).

[0049] HEL PE The model is the HEL-persistent model, which is constructed by treating HEL primitive cells with a high concentration of ruxolitinib that exceeds the IC50 concentration of the primitive cells by 100 times, and the concentration we use is 2.0 μM. The solution was changed every two days, and the cells that could not tolerate it died quickly, and the amplified cells were DTP (drug-tolerant-persisters), which were difficult to be killed by anti-tumor drugs. Stable drug-resistant cells were obtained after 4-6 weeks. Another resistance model is HEL RE That is, the HEL-resistant model, the construc...

Embodiment 2

[0058] Example 2, Sorafenib can inhibit the proliferation of two drug-resistant cell lines

[0059] The method is to use increasing concentrations of Sorafenib to treat drug-resistant cell lines, through CellTiter-Lumi TM Luminescence method is used to detect the proliferation of cells, the method is the same as in Example 1, and the results are shown in figure 2 .

[0060] The results show, figure 2 a reflects that in the ruxolitinib-resistant cell model HEL-persistent, the IC50 value of sorafenib is 2.80 μM, which is 1 / 9 of the ruxolitinib IC50 value of 25.5 μM, figure 2b reflects that in the ruxolitinib-resistant cell model HEL-resistant, the IC50 value of sorafenib is 3.56 μM, which is 1 / 7 of the ruxolitinib IC50 value of 24.9 μM. This shows that sorafenib can inhibit the proliferation of ruxolitinib-resistant cells, and this effect is enhanced with the increase of concentration.

Embodiment 3

[0061] Example 3, Sorafenib can promote the apoptosis of two drug-resistant cell lines

[0062] 1. Materials and methods

[0063] 1. Cell lines and inhibitors are the same as in Example 1.

[0064] 2. Apoptosis detection

[0065] In order to detect the pro-apoptotic effect of the inhibitor, the drug-resistant cell line was treated with increasing concentrations of Sorafenib for 24 hours (concentration: 0, 2.5, 5, 10 μM), and DMSO was supplemented to the same amount. Three parallel repeat groups were set up, and the apoptosis of cells was detected by flow cytometry after AnnexinV-PI staining.

[0066] Apoptotic rate calculation formula: Apoptotic rate = ratio of early apoptotic cells (AnnexinV+ / PI-) + ratio of late apoptotic cells and necrotic cells (AnnexinV+ / PI+).

[0067] 2. Results Analysis

[0068] image 3 In a, the drug concentration (average apoptosis rate) of ruxolitinib treatment group is: 0 μM (0.91%), 2.5 μM (0.920%), 5 μM (1.11%), 10 μM (0.740%); Sorafenib tre...

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Abstract

The invention belongs to the technical field of medicines, discloses an new application of sorafenib, and particularly relates to an application of the sorafenib to preparation of medicines for treating myeloproliferative neoplasmas. The myeloproliferative neoplasmas is myeloproliferative neoplasmas with polycythemia vera or drug resistance of ruxolitinib. The sorafenib is used for treating the polycythemia vera, a new treatment way is provided for patients suffering from the polycythemia vera, and more choices are provided for clinicians and patients. For a patient suffering from myeloproliferative neoplasmas with drug resistance of ruxolitinib, the sorafenib can provide continuous oral drug therapy for the patient, and bone marrow transplantation is avoided. The sorafenib can be chemically synthesized, and the cost is lower than that of a biological agent. And the sorafenib is approved by FDA and NMPA to appear on the market and is used for clinical treatment. The side reaction is less and lighter, the tolerance of clinical patients is good, and the burden of the patients is lighter.

Description

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Claims

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Application Information

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Owner THE SECOND XIANGYA HOSPITAL OF CENT SOUTH UNIV
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