Novel application of Apatinib for preparing medicine for treating acute myelogenous leukemia

An apatinib, acute myeloid technology, applied in the field of drug application, can solve problems such as no relevant reports, and achieve the effects of good safety, good biocompatibility, and no toxic side effects

Inactive Publication Date: 2019-10-01
THE FIRST AFFILIATED HOSPITAL OF XIAMEN UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The results of current II / III clinical trials show that apatinib is effective against a variety of solid tumors such as gastric cancer (Li J, QinS, Xu J, et al. Randomized, double-blind, placebo-controlled phase iii trial of apatinib in patients with chemo-therapy refractory advanced or metastaticadenocarcinoma of the stomach or gastroesophageal junction[J].Am J ClinOncol,2016,34(13):1448-1454) and breast cancer (Hu X, Zhang J, Xu B, et al.Multicenterphase II study of apatinib, a novel VEGFR inhibitor in heavily preservedpatients with metastatic triple-negative breast cancer[J].Int J Cancer,2014,135(8):1961-1969), etc. have significant killing effect, but there is no information about its application in acute myeloid leukemia see related reports

Method used

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  • Novel application of Apatinib for preparing medicine for treating acute myelogenous leukemia
  • Novel application of Apatinib for preparing medicine for treating acute myelogenous leukemia
  • Novel application of Apatinib for preparing medicine for treating acute myelogenous leukemia

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] Evaluation of the Inhibitory Effect of Apatinib on the Proliferation of AML Cell Lines

[0050] The operation method is: take the quantity as 2×10 4 AML cell lines in the logarithmic growth phase (including HL60, K562, Kasumi-1, Kg1a, Molm13, MV411, NB4, Thp1 and U937 cell lines) were inoculated in 96-well plates, and the control group and different concentrations of Apatinib groups (0, 2.5, 5, 10, 20, 40 μM), after each group was treated for 48h and 72h, respectively, the proliferation of AML cells in different groups was detected with the CCK8 kit (the specific operation steps were carried out according to the kit instructions).

[0051] The result is as figure 1 As shown, wherein (a) is the result of Apatinib acting for 48h, and (b) is the result of Apatinib acting for 72h. Depend on figure 1 It can be seen that: Apatinib can significantly inhibit the proliferation of various AML cell lines, especially Molm13 cells and MV411 cells; moreover, the inhibitory effect ...

Embodiment 2

[0056] Evaluation of Apatinib Inducing Apoptosis in AML Cell Lines

[0057] The operation method is: take the quantity as 2×10 5 AML cell lines in the logarithmic growth phase (including HL60, K562, Kasumi-1, Kg1a, Molm13, MV411, NB4, Thp1 and U937 cell lines) were inoculated in 24-well plates, and the control group and different concentrations of Apatinib groups (0, 10, 20, 30, 40 μM), each group was treated for 48h and 72h respectively, and Annexin V / PI kit was used to detect the apoptosis of AML cells in different groups (the specific operation steps were carried out according to the kit instructions).

[0058] The result is as figure 2 Shown, wherein (a) is the result of Apatinib acting for 48h, (b) is the result of Apatinib acting for 72h. Depend on figure 2 It can be seen that: Apatinib can significantly induce apoptosis of various AML cell lines, especially for Molm13 cells and MV411 cells; moreover, Apatinib has a significant concentration-dependent effect on indu...

Embodiment 3

[0060] Evaluation of the effect of apatinib on AML cells and normal bone marrow mononuclear cells from primary cell level

[0061] The operation method is as follows: collect 57 cases of bone marrow samples from patients with newly diagnosed or refractory recurrent AML and 11 cases of bone marrow samples (BMMCs) from hematopoietic stem cell transplantation donors, and extract mononuclear cells with lymphocyte separation medium. After treating primary AML cells and normal BMMCs cells with different concentrations of Apatinib (0, 10, 20, 30, 40 μM) for 48 hours, the apoptosis ratio of primary AML cells and normal BMMCs was detected by Annexin V / PI double staining method.

[0062] The result is as image 3 Shown, wherein (a) is the apoptosis result of primary AML cells, (b) is the apoptosis result of normal BMMCs cells. Depend on image 3 It can be seen that the addition of Apatinib can significantly increase the apoptosis rate of primary AML cells, and the apoptosis rate gradu...

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PUM

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Abstract

The invention relates to novel application of Apatinib or pharmaceutically acceptable salts, ester and solvent compounds thereof for preparing a medicine for treating acute myelogenous leukemia. The Apatinib restrains acute myelogenous leukemia cell amplification and induces apoptosis of cells by activating the mitochondrion-mediated endogenesis apoptosis way and lowering the VEGFR2 phosphorylation level and the PLCgama/PKC/S6 signal channel of the downstream thereof, and finally the effect of treating acute myelogenous leukemia is obtained; Apatinib or pharmaceutically acceptable salts, esterand solvent compounds thereof have no toxic or side effect on normal marrow mononuclear cells, the safety is good, the theoretical basis is provided for researching the treatment strategy for acute myelogenous leukemia, and an embedded point is supplied to preparation of the medicine for treating the acute myelogenous leukemia.

Description

technical field [0001] The invention relates to the field of drug application, in particular to the new application of apatinib in the preparation of drugs for treating acute myeloid leukemia. Background technique [0002] Acute myeloid leukemia (AML) is one of the most common types of leukemia in adults, with a median age of onset of 67 years old. Symptoms, such as anemia, bleeding, infection and infiltration of tissues and organs. After decades of research by a large number of researchers, it is generally believed that AML is a malignant clonal proliferative disease originating from hematopoietic stem / progenitor cells (hematopoietic stem / progenitor cells). It is a combination of chemotherapy and allogeneic hematopoietic stem cell transplantation (Short NJ, Rytting ME, Cortes JE, Acute myeloidleukaemia. [J]. Lancet 2018 08 18; 392(10147)). [0003] In recent years, with the improvement of the dose of multi-drug combination chemotherapy, the progress of hematopoietic stem ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/444A61P35/02
CPCA61K31/444A61P35/02
Inventor 徐兵邓漫漫李志峰查洁赵海军方志鸿
Owner THE FIRST AFFILIATED HOSPITAL OF XIAMEN UNIV
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