Medicine composition of tyrosine kinase inhibitor and histone deacetylase inhibitor

A technology of tyrosine kinase and deacetylase, which is applied in the field of drugs for the treatment of tumors, can solve the problems of poor drug resistance, insufficient tumor curative effect, and large clinical drug doses, and achieve the effect of delaying drug resistance and reducing drug resistance

Inactive Publication Date: 2013-05-08
毛幼桦 +1
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  • Abstract
  • Description
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Problems solved by technology

[0007] In order to overcome the problems of insufficient curative effect, poor drug resistance, and large clinical dosage of tyrosine kinase inhibitors when t

Method used

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  • Medicine composition of tyrosine kinase inhibitor and histone deacetylase inhibitor
  • Medicine composition of tyrosine kinase inhibitor and histone deacetylase inhibitor
  • Medicine composition of tyrosine kinase inhibitor and histone deacetylase inhibitor

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Embodiment Construction

[0023] According to the technical scheme of the present invention, this embodiment provides a drug combination of a tyrosine kinase inhibitor and a histone deacetylase inhibitor, the tyrosine kinase inhibitor is selected from imatinib, histone The sirtuin inhibitor is hemisodium valproate, and the combination of the two according to the mass ratio of 0.5:1~1:4 is only a further description of the present invention, not a specific combination of tyrosine kinase inhibitors and specific combinations. Concomitant use of protein deacetylase inhibitors is limited.

[0024] The dose of valproate adopts a low cytotoxic dose, and the clinically relevant dose is 100-1000 mg / d; the dose of imatinib adopts a clinical dose, and the clinically relevant dose is 50-800 mg / d. d, and used in combination with valproate.

[0025] The tyrosine kinase inhibitors include, but are not limited to, imatinib, dasatinib, nilotinib, gefitinib, etc.; the histone deacetylase inhibitors include, but are not...

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Abstract

The invention discloses a medicine composition of a tyrosine kinase inhibitor and a histone deacetylase inhibitor. The prepared medicine composition comprises a tyrosine kinase inhibitor and a histone deacetylase inhibitor according to a mass ratio of (0.5:1)-(1:4). The tyrosine kinase inhibitor is selected from imatinib, dasatinib, nilotinib, gefitinib and the like; and the histone deacetylase inhibitor is selected from short-chain fatty acid such as butyric acids and valproic acids, hydroxamic acids such as trichostatin A, cyclic tetrapeptides and benzamides. Compared with the tyrosine kinase inhibitor of treating tumors by one target, the medicine composition has the advantages of strong treatment effect, high medicine tolerance, and small clinical medicine dosage, and is applied clinically by using a medicine preparation form.

Description

technical field [0001] The invention relates to the technical field of drugs for treating tumors, in particular to a pharmaceutical composition of a tyrosine kinase inhibitor and a histone deacetylase inhibitor. Background technique [0002] Tyrosine kinase inhibitors (TKIs) are a class of compounds that inhibit the activity of tyrosine kinases. Tyrosine kinase is a kind of kinase that catalyzes the transfer of γ-phosphate on ATP to protein tyrosine residues. It can catalyze the phosphorylation of protein tyrosine residues on various substrates, and plays an important role in cell growth, proliferation and differentiation. effect. Most of the protein tyrosine kinases discovered so far belong to the oncogene products of oncogenic RNA viruses, and can also be produced by proto-oncogenes in vertebrates. [0003] Tyrosine kinase inhibitors can be used as competitive inhibitors of the binding of adenosine triphosphate (ATP) to tyrosine kinases, and can also be used as analogs o...

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Application Information

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IPC IPC(8): A61K45/06A61K31/506A61K31/5377A61P35/00
Inventor 林蓉张继业张建丰杨广德毛幼桦熊俊峰
Owner 毛幼桦
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