38 results about "Trametinib" patented technology

The invention belongs to the technical field of medicine, and discloses application of trametinib in preparation of a drug for treating Parkinson's disease, wherein trametinib is used for preparing the drug to delay the degeneration of dopaminergic neuron. The obtained product can effectively delay the degenerative death of dopaminergic neuron, to treat Parkinson's disease fundamentally; the drug can be taken orally without injection to achieve the treatment effect, has excellent curative effect for Parkinson's disease caused by a variety of reasons, and has important significance for the treatment and curing of Parkinson's disease.

The invention provides a method of blocking transmission of a Plasmodium parasite and a method of treating or preventing malaria comprising administering to an animal an effective amount of a first compound of formula I: wherein A, B, R¹, R², R¹⁰, and R¹¹ are described herein, either alone or in combination with a second compound selected from elesclomol, NSC 174938, NVP-AUY922, Maduramicin, Narasin, Alvespimycin, Omacetaxine, Thiram, Zinc pyrithione, Phanquinone, Bortezomib, Salinomycin sodium, Monensin sodium, Dipyrithione, Dicyclopentamethylene-thiuram disulfide, YM155, Withaferin A, Adriamycin, Romidepsin, AZD-1 152-HQPA, CAY10581, Plicamycin, CUDC-101, Auranofin, Trametinib, GSK-458, Afatinib, and Panobinostat.

The invention relates to applications of trametinib to preparation of a drug for treating pulmonary inflammatory diseases and promotion of Tfh cell differentiation. The chemical formula is C26H23FIN5O4. The applications include an application of trametinib to promotion for Tfh cell differentiation and an application of trametinib to preparation of the drug for treating the pulmonary inflammatory diseases. The trametinib has beneficial effects as follows: cytokine storm caused by activation of T cells and mononuclear macrophages can be better inhibited, and meanwhile, Tfh differentiation, B cell maturation mediation and antibody production are promoted; and as abroad-spectrum immune regulation drug, the trametinib has an effect of promoting antibody production in the aspects of other viralpneumonia, virus infection or seedling inoculation.

The invention discloses a medicine for treating lung cancer. The medicine is composed of NG25 and trametinib at a mass ratio of 4 to 1; and the lung cancer is a lung cancer in which the function of CLU genes is absent or down-regulated. Further, the lung cancer is a lung cancer in which the function of the CLU genes is absent or down-regulated and is driven by KRASG 12D oncogenes. In vitro experiments show that CLU knock-down lung cancer cells are more sensitive to NG25, compared with controls, the NG25 can significantly inhibit the growth of the lung cancer cells, and while after the cells are treated by combining with the Trametinib, it is found that the inhibition on the lung cancer cells is even more significant. Similarly, in animal models, a TAK1 inhibitor NG25 can inhibit the growthof CLU knock-down cell transplantation tumors and CLU knock-out orthotopic lung cancer, the treatment combined with the Trametinib can significantly shrink the tumor, and the purpose of treating thetype of the lung cancer is achieved.

The present disclosure relates to pharmaceutical combinations comprising a cyclin dependent kinase 4/6 (CDK4/6) inhibitor compound, (b) a mitogen activated protein kinase (MEK) inhibitor compound, andoptionally (c) an alpha-isoform specific phosphatidylinositol 3-kinase (PI3K) inhibitor compound, for the treatment or prevention of cancer, as well as related pharmaceutical compositions, uses, andmethods of treatment or prevention of cancer.

The invention discloses a trametinib microemulsion and application thereof. The microemulsion is prepared from trametinib, methyl salicylate, vitamin E, caprylic capric triglyceride, diethylene glycol monoethyl ether and polyoxyethylated castor oil EL. Compared with a trametinib water suspension, the trametinib microemulsion disclosed by the invention has the advantages that the retention volume is high; Compared with oral trametinib suspension, the trametinib microemulsion has more remarkable tumor inhibition efficacy, so that the trametinib micro-emulsion can effectively inhibit the melanoma and has more remarkable curative effect and advantages in the aspect of treating the melanoma. In addition, adopted instruments and equipment are simple and convenient, the preparation process is efficient, simple and controllable, and the method is suitable for industrial production.

Inventors have shown that targeting DDR1 and DDR2 collagen receptors by Imatinib resensitizes melanoma tumors to BRAFV600E to targeted therapy and normalizes the fibrotic stromal reaction. These findings provide the rationale to combine Imatinib (or other DDR inhibitors) and MAPK-targeting agents to disrupt the influence of the matrix microenvironment in order to delay or prevent the emergence of therapy-resistant cells. They have shown that inhibition of DDR1 and DDR2 kinase activities by Imatinib suppressed the protection of melanoma cells against Vemurafenib (BRAFi) and Trametinib (MEKi) co-drugging and led to cell cycle arrest and cell death. Similar biochemical cell cycle and apoptotic events were promoted in presence of Nilotinib. They validated this anti-tumor activity of Imatinib combined with Vemurafenib in a pre-clinical xenograft model of melanoma and showed that targeting DDR1/2 signaling delays tumor relapse. Accordingly, the present invention relates to a method for treating melanoma in a subject in need thereof comprising a step of administering said subject with a therapeutically effective amount of: i) an inhibitor of BRAF, ii) an inhibitor of MEK, and iii) an inhibitor of DDR1/2.

The invention belongs to the technical field of medicine application, and discloses an application of trametinib in preparing a medicine for reversing multi-medicine resistance of tumors. Trametinib can be used for significantly reversing the multi-medicine resistance of the tumors mediated by membrane transport protein to ensure that the sensitivity of P-glycoprotein high expression cells to anti-cancer medicines can be restored. According to the medicine for reversing the multi-medicine resistance of the tumors, disclosed by the invention, trametinib and the anti-cancer medicines can be combined to ensure that the effects of treating and controlling resistant tumors can be achieved by restoring the sensitivity of resistant cells to the anti-cancer medicines.

The invention belongs to the technical field of induced differentiation of stem cells, in particular to an inducer for neural differentiation of mesenchymal stem cells. The inducer for neural differentiation of the mesenchymal stem cells is prepared from the following components by a mass concentration ratio, 2-8 mg/L of acetaminophen, 4-6 mg/L of insulin, 2-6 mg/L of glucagon-like peptide-1 (GLP-1), 200-400 [mu]g/L of trametinib, 20-100 [mu]g/L of forskolin, 2-10 [mu]g/L of keratinocyte growth factor (KGF) and 2-10 [mu]g/L of bone morphogenetic protein-4 (BMP-4). The inducer has high induction efficiency, few induction steps and short induction time; nerve cells obtained by induction have high activity, have no rejection and no ethical problem after being transplanted, and are high in safety.

A method of reducing the severity of radiation induced fibrosis (RIF) by administering to a patient at least a first dose of an MeK inhibitor such as trametinib between 0.01 mg to 2.0 mg, and after said radiation procedure, administering to said patient a further dose of the MeK inhibitor between 0.01 mg and 2.0 mg after the radiation procedure.

The present invention relates to administration methods and dosage regimens for treatment of neurodegenerative diseases using trametinib and markers. The administration methods and dosage regimens induce neural regeneration and changes in gene expression.

The present invention relates to a pharmaceutical combination comprising (a) a Raf inhibitor as defined herein, or a pharmaceutically acceptable salt thereof and (b) a MEK inhibitor, particularly trametinib, particularly for use in the treatment of a proliferative disease. This invention also relates to uses of such combination for preparation of a medicament for the treatment of a proliferative disease; methods of treating a proliferative disease in a subject in need thereof comprising administering to said subject a jointly therapeutically effective amount of said combination; use of such combination for the treatment of proliferative disease; pharmaceutical compositions comprising such combination and commercial packages thereto.

The invention relates to application of trametinib in preparation of an anti-arenavirus antiviral preparation, and belongs to the technical field of medicine application. The invention particularly relates to application of trametinib in preparation of an antiviral preparation for inhibiting or killing arenavirus. The new application of trametinib is provided, the application range of trametinib is expanded, and particularly, trametinib can be used for preparing the antiviral preparation of the arenavirus and killing or inhibiting the arenavirus, and then can be used for treating arenavirus infection and diseases caused by the arenavirus infection.