The drug composition of erlotinib

A technology of ibrutinib and composition, applied in the field of pharmaceutical composition of antitumor drug ibrutinib and CYP3A enzyme inhibitor

Inactive Publication Date: 2017-03-08
BEIJING MEIBEITA DRUG RES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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  • The drug composition of erlotinib
  • The drug composition of erlotinib
  • The drug composition of erlotinib

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Example 1 The inhibitory effect of the composition of ibrutinib and ritonavir on target cells and non-target cells

[0022] The composition of different ratios of ibrutinib and ritonavir was tested by MTT method on Pfeiffer cells, purchased from Shanghai Enzyme Research Biotechnology Co., Ltd.), and non-target cells HepG2 cells and HEK293 cells (purchased from Shanghai Enzyme Research Biotechnology Co., Ltd.) inhibition.

[0023] Culture the cells to be tested, and prepare a concentration of about 2.5×10 4 cells / mL of cell suspension, seeded in 96-well culture plate, 100.0uL / well, placed at 37°C, 5% CO 2 Incubate in an incubator for 24 hours; add different concentrations of test substances to the 96-well plate of cultured tumor cells, and continue to culture for 72 hours; discard the culture medium, add 100.0 μL of 0.05% MTT application solution to each well, and incubate for 4 hours Discard the culture medium, add 100 μL DMSO to each well, shake for 5 minutes to diss...

Embodiment 2

[0032] Example 2 The inhibitory effect of the composition of ibrutinib and ketoconazole on target cells and non-target cells

[0033] Referring to the method of Example 1, the inhibitory effect of the composition of ibrutinib and ketoconazole in different ratios on Pfeiffer cells, HepG2 cells and HEK293 cells was tested. The results are shown in Table 2.

[0034] Table 2 Ibrutinib and ketoconazole composition anti-tumor activity evaluation results

[0035]

[0036] It can be seen from Table 2 that the addition of different proportions of ketoconazole does not affect the inhibitory effect of ibrutinib on target cell lymphoma B lymphocytes; but the addition of a high proportion of ketoconazole increases the effect on non-target cells HepG2 cells ( liver-derived) and HEK293 cells (nephrogenic), especially HepG2 cells have significant toxicity, suggesting that the composition containing a high proportion of ketoconazole may have stronger liver toxicity.

Embodiment 3

[0037] Example 3 Inhibition of the Composition of Ibrutinib and Cobicistat on Target Cells and Non-Target Cells

[0038] Referring to the method of Example 1, the inhibitory effect of the composition of ibrutinib and cobicistat in different ratios on Pfeiffer cells, HepG2 cells and HEK293 cells was tested. The results are shown in Table 3.

[0039] Table 3 Evaluation results of the antitumor activity of the combination of ibrutinib and cobicistat

[0040]

[0041] It can be seen from Table 3 that the addition of different proportions of cobicistat does not affect the inhibitory effect of ibrutinib on target cell lymphoma B lymphocytes; but the addition of a high proportion of cobicistat increases the effect on non-target cells HepG2 cells ( liver-derived) and HEK293 cells (kidney-derived), suggesting that the composition containing a high proportion of cobicistat may have certain liver and kidney toxicity.

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Abstract

The invention relates to a pharmaceutical composition for an antineoplastic agent erlotinib and a CYP3A enzyme inhibitor, wherein the CYP3A enzyme inhibitor is ritonavir, ketoconazole or terrestroside. The weight ratio of erlitinib and ritonavir is 1: 0.5 to 1:20, and the weight ratio of erlitinib and ketoconazole is 1: 2 to 1:40, and the weight ratio of erlotinib and comparable is 1: 1 to 1 : 30. The drug composition provides a pharmaceutical composition comprising an effective therapeutic amount of erlitinib, a non-toxic pharmaceutically acceptable salt, cytochrome CYP3A inhibitor and a non-toxic pharmaceutically acceptable salt thereof as a Bruton Tyrosine Kinase Inhibitors in the preparation of antineoplastic agents, wherein the daily dose of erlotinib is 0.2-2.0 mg / kg per person.

Description

[0001] Technical field: [0002] The present invention relates to the pharmaceutical composition of antineoplastic drug ibrutinib and CYP3A enzyme inhibitor; wherein the CYP3A enzyme inhibitor is ritonavir, ketoconazole or cobicistat; the combination of ibrutinib and ritonavir The weight ratio is 1:0.5 to 1:20, the weight ratio of ibrutinib and ketoconazole is 1:2 to 1:40, and the weight ratio of ibrutinib and cobicistat is 1:1 to 1:30 . [0003] technical background: [0004] Ibrutinib (Ibrutinib) selectively inhibits Bruton's tyrosine kinase (BTK), effectively prevents tumor migration from B cells to lymphoid tissues adapted to the tumor growth environment, and exerts targeted anti-tumor effects; Lymphoma (Mantle Cell Lymphoma), chronic lymphocytic leukemia (chronic lymphocytic leukemia, CLL) and B-cell non-Hodgkin lymphoma (B-cell non-Hodgkin lymphoma, B-NHL) have a good curative effect. [0005] Ibrutinib is primarily metabolized by cytochrome P450CYP3A4 enzymes. Unknown...

Claims

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Application Information

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IPC IPC(8): A61K45/06A61K31/519A61K31/427A61K31/496A61K31/5377A61P35/00
CPCA61K31/427A61K31/496A61K31/519A61K31/5377
Inventor 王建明杨家俊王进京
Owner BEIJING MEIBEITA DRUG RES
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