56 results about "Brain metastasis" patented technology

The present disclosure relates generally to methods for treating or preventing central nervous system (CNS) metastases with a KRAS inhibitor, and more specifically to treating CNS metastases with a pyridopyrimidine derivative.

The invention discloses an application of pegylated irinotecan in preparation of a medicine for preventing and / or treating triple-negative breast cancer brain metastasis diseases, which is shown by in-vivo imaging observation and lifetime observation of high, medium and low dose groups of pegylated irinotecan with a specific structure. The high-dose group, the medium-dose group and the low-dose group all have a definite anti-tumor effect, bioluminescence signal values are inhibited to different degrees, the lifetime is prolonged, and the lifetime of the high-dose group and the lifetime of the medium-dose group are remarkably longer than that of the NKTR-102 group.

The invention provides application of an arsenene nano preparation and / or beta-elemene in preparation of a product for treating brain tumors, and belongs to the technical field of biology. The arsenene nano preparation and / or beta-elemene are / is applied to brain glioma and lung cancer brain metastatic tumor model mice, so that tumor cells can be effectively killed, tumor metastasis can be inhibited, in-vivo immune response can be activated, maturation of dendritic cells can be promoted, NK cells and CD8 + T cells can be effectively activated, and the secretion amount of tumor suppression cell factors can be increased. Meanwhile, the beta-elemene effectively reduces cardiotoxicity caused by accumulation of the arsenene nano preparation in vivo.

The invention belongs to the field of biological medicines, and discloses an (R)-3-(1-([1, 1 '-biphenyl]-2-yl) ethyoxyl) pyridine-2-amine derivative as well as a synthesis method and application thereof. A compound with a structure as shown in a general formula I of the derivative or pharmaceutically acceptable salt, hydrate, solvate, polymorphic substance, tautomer, stereoisomer, isotope derivative or prodrug thereof has higher ROS1 or ALK protein kinase inhibitory activity; the compound has high anti-proliferative activity on human non-small cell lung cancer and solid tumors such as brain metastatic tumors, glioblastoma and breast cancer, and can be used for preparing drugs for treatment and / or prevention and / or delay and / or adjuvant treatment and / or treatment of tyrosine protein kinase, especially diseases mediated by ROS1 and ALK kinase and mutant kinase thereof.

The application belongs to the technical field of biology and particularly relates to application and a kit of CoL10A1. CoL10A1 is highly expressed in BC tissues and lowly expressed in normal tissues, CoL10A1 is highly expressed at mRNA and protein levels in BCBM tissues, therefore, application of a reagent for detecting CoL10A1 expression in preparation of a breast cancer brain metastasis diagnosis product is proposed, and the diagnosis product can also be used for diagnosing breast cancer.

The invention discloses treatment of EGFR mutation positive non-small cell lung cancer brain metastasis by administering an effective dose of an EGFR inhibitor. The EGFR inhibitor is N-(2-((2-(dimethylamine) ethyl) (methyl) amine)-4-methoxy-5-((4-(1-deuterated methyl-1H-indol-3-yl) pyrimidine-N '-2-yl) amine) phenyl) acrylamide mesylate.

The application discloses application of tenapanol in preparation of a medicine for inhibiting tumor brain metastasis. The application targets neutrophils which are recruited in brain metastasis foci and promote tumor growth, screens out an inhibitor tenapanol for a neutrophil chemotactic receptor FPR2, inhibits the neutrophil recruitment to the brain and the subsequent promotion of tumor cell clonal growth by inhibiting the combination of the receptor and SAA1 which is specifically up-regulated in metastatic tumor cells, and thus the therapeutic effect of inhibiting the progression of intracranial lesions is achieved.

The invention discloses a substituted 2-amino-9-(3, 3-difluoropiperidine-4-yl)-7, 9-dihydro-8H-purine-8-ketone compound with a structural formula as shown in formula (I): (I) The substituted 2-amino-9-(3, 3-difluoropiperidine-4-yl)-7, 9-dihydro-8H-purine-8-ketone compound disclosed by the invention as well as a derivative and pharmaceutically acceptable salt thereof, and a preparation method of the substituted 2-amino-9-(3, 3-difluoropiperidine-4-yl)-7, 9-dihydro-8H-purine-8-ketone compound. The compound can be used as a protein kinase inhibitor drug to play a role, especially can inhibit protein expression induced by DNA-PK, and can be used for treating or preventing diseases related to abnormal protein kinase activity. The compound can be used for treating cancer, such as cancer, cancer accompanied with brain metastasis, cancer accompanied with meningeal metastasis, glioma, glioblastoma, diffuse endogenous bridge glioma (DIPG) and the like, and can be independently applied or combined with other treatment modes (such as radiation therapy or chemotherapy).

Described herein are methods of treating a MTAP-null lung cancer in a patient comprising administering to the patient a PRMT5 inhibitor and an anti-PD1 antibody, optionally in combination with carboplatin and either paclitaxel or pemetrexed. Further described herein are methods of treating a MTAP-null cancer in a patient also suffering from brain metastases comprising administering to the patient a PRMT5 inhibitor.

To provide methods for treating cancer.SOLUTION: Provided is a drug for inhibiting tumor growth or causing tumor regression in a subject with estrogen receptor alpha-positive breast cancer brain metastasis, the subject having one or more estrogen receptor alpha mutations selected from the group consisting of Y537S, Y537C, Y537N, D538G, and S463P. The drug comprises, as an active ingredient, a therapeutically effective amount of RAD1901 having a given structure, or a salt or solvate thereof, which is used in combination with palbociclib.SELECTED DRAWING: None

The present disclosure provides compositions and methods comprising amrannekast, or a pharmaceutically acceptable salt thereof, for the treatment and prevention of brain metastases. The present disclosure provides treatment and / or prevention of brain metastases in a subject suffering from ER + breast cancer within such compositions and methods.

The invention belongs to the technical field of biological medicine, and particularly relates to application of CST6 as a lung cancer brain metastasis early diagnosis marker. The core of the invention is to confirm that CST6 is used as a marker for early diagnosis and prediction of brain metastasis of lung cancer for the first time. In experimental verification, the CST6 protein expression quantity of the lung cancer cell strain H1975-BrM with high brain metastasis potential is remarkably higher than that of a common cell strain, an animal model further shows that overexpression of CST6 can promote formation of brain metastasis, and knock-down expression can inhibit metastasis capacity; clinical sample analysis shows that the serum CST6 concentration of brain metastasis patients is far higher than that of non-metastasis patients and healthy people, and the diagnostic value of CST6 is supported. In the aspect of diagnosis efficiency, the area under the ROC curve of the serum CST6 reaches 0.848, and high accuracy is shown. On the whole, the clinical blank is filled, and a reliable tool is provided for non-invasive lung cancer brain metastasis risk management.

The present disclosure provides methods for treating or inhibiting the growth of a tumor, wherein the method includes selecting a patient with lung cancer and brain metastasis in need thereof and administering to the patient a therapeutically effective amount of a programmed death 1 (PD-1) inhibitor (e.g., cemiplimab or a bioequivalent thereof). In certain embodiments, the lung cancer is non-small cell lung cancer (NSCLC) and PD-L1 is expressed in ≥50% of tumor cells. In certain embodiments, the methods lead to improvements in functioning and quality of life.

This invention discloses a wasp venom peptide-M nanocomposite, its preparation method, and its applications, belonging to the field of medicinal chemistry. Using indocyanine green as a morphology mediator, this invention prepares an ultra-small particle size dendritic tetrasulfide by reacting it with triethylamine, hexadecyltrimethylammonium bromide, tetraethyl orthosilicate, and bis[3-(triethoxysilyl)propyl]tetrasulfide in water. Wasp venom peptide-M is then loaded onto this nanocomposite to obtain the wasp venom peptide-M nanocomposite. In vitro experiments have confirmed that this composite can significantly kill 4T1 breast cancer cells. Furthermore, thanks to its ultra-small particle size, it also exhibits good targeting and enrichment, significant anti-tumor efficacy, and excellent safety in a breast cancer brain metastasis model, providing a novel and efficient nanomedicine delivery system for brain tumor treatment and the development of related therapeutic drugs.

This invention belongs to the field of pharmaceutical formulation technology, specifically disclosing a gastrodin transdermal patch and its preparation method. The patch consists of a backing layer, a drug-containing matrix layer, and an anti-adhesive layer, using gastrodin as the active ingredient. It employs HP-β-CD inclusion technology, combined with an HPMC and PVP polymer backbone and an oleic acid-menthol composite transdermal enhancement system. The preparation utilizes solvent casting and low-temperature vacuum drying processes, which are mild and controllable. This invention effectively solves the problems of difficult transdermal absorption, easy recrystallization, and low bioavailability of gastrodin. The resulting patch has excellent adhesion, no skin irritation, high transdermal penetration, and good skin biocompatibility. It can efficiently cross the blood-brain barrier, regulate the neuroinflammatory microenvironment in the brain, significantly inhibit the colonization and progression of non-small cell lung cancer brain metastases, and strongly reverse tumor-related anxiety and depression-like mood disorders. It provides a novel drug delivery regimen with great clinical translational potential for the non-invasive synergistic treatment of brain tumors and their associated mood disorders.

The present invention relates to the treatment of cancer with metastases in the central nervous system (CNS), in particular in the brain, using the HER2 tyrosine kinase inhibitor zongertinib. Accordingly, compounds for use, methods of prevention and / or treatment and uses related to said treatment are herewith provided.

The utility model relates to the technical field of tumor cell metastasis models, in particular to a breast cancer circulating tumor cell remote metastasis model which comprises a base and a fixing rod, the fixing rod is fixedly connected to the base, the fixing rod is fixedly connected with a brain metastasis model, a placing component is installed on the brain metastasis model, and the placing component is fixedly connected with the brain metastasis model. The placing part comprises an inclined plate, a fixed plate, a movable plate, a pressed plate, a straight spring and a collecting box, the inclined plate is fixedly connected in the brain metastasis model, the clamping plate clamps small balls with different colors through the matching effect of the extrusion rod, the movable plate, the collecting box and other parts, the small balls can be taken out by pulling the clamping plate, and the small balls can be conveniently taken out. And residual water is left in the collecting box, so that the small balls can be quickly taken out, meanwhile, no water drips on the outer surface of the model, the situation that the transparency of the model is affected by water marks generated on the outer surface of the model due to water dripping is avoided, and the transparency of the organ model and the cleanliness of a placement environment are guaranteed.

The present application relates to the field of medicine, and provided thereby is a quinoline derivative used for treating small cell lung cancer. The 1-[[[4-(4-fluoro-2-methyl-1H-indol-5-yl)oxy-6-methoxyquinolin-7-yl]oxy]methyl]cyclopropylamine or a pharmaceutically acceptable salt thereof as provided by the present application may be used for the treatment of small cell lung cancer, especially for patients suffering from refractory relapsed small cell lung cancer, which may significantly prolong the survival time thereof; in addition, the therapeutic effect on brain metastatic small cell lung cancer is also very significant.

The epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) osimertinib has significantly prolonged progression-free survival (PFS) in EGFR-mutant lung cancer patients, including those with brain metastases. However, osimertinib-treated patients often develop lethal metastatic relapse, often to the brain. The genetic repression of S100A9, ALDH1A1, or RA receptors (RAR) in cancer cells, or treatment with a pan-RAR antagonist, dramatically reduces brain metastasis. S100A9 expression in cancer cells correlates with poor PFS in osimertinib-treated patients, and is identified as a novel, therapeutically targetable S100A9-ALDH1A1-RA axis. A combination of osimertinib and AGN-194310, for example, treats such cancer while avoiding metastatic relapse.

This invention relates to the field of biomedical technology, providing the application of a combination of diagnostic biomarkers for lung adenocarcinoma brain metastases based on BNIP3, CD74, and LYZ. Specifically, it relates to the application of this combination of diagnostic biomarkers in the preparation of reagents for predicting the prognosis of lung adenocarcinoma brain metastases. These reagents predict the prognosis of lung adenocarcinoma brain metastases by detecting the expression levels of BNIP3, CD74, and LYZ in the brain metastatic tissues of patients with lung adenocarcinoma brain metastases. This invention, based on a combination of diagnostic biomarkers for lung adenocarcinoma brain metastases based on BNIP3, CD74, and LYZ, can accurately assess the progression and risk level of a patient's disease in predicting prognosis and risk stratification of lung adenocarcinoma brain metastases. This provides precise reference for subsequent individualized treatment plans and rehabilitation programs, thus optimizing patient management.

The invention relates to the technical field of biology, in particular to a construction method of a novel lung cancer brain transfer model. The method comprises the following steps: carrying out induction culture on stem cells to obtain an embryoid organ, and carrying out differentiation culture on the embryoid organ to obtain a midbrain ventral organ; the method comprises the following steps: shearing and digesting small cell lung cancer (SCLC) tissue blocks to obtain SCLC cells, and carrying out suspension culture to obtain small cell lung cancer (SCLC) organs; and placing the midbrain ventral organ and the small cell lung cancer organ in the same culture container, and carrying out co-culture to obtain the novel lung cancer brain transfer model. Compared with a human-derived tumor tissue xenograft technology with a low success rate, the novel lung cancer brain transfer model provided by the embodiment of the invention has high fusion efficiency and batch stability, and interference of other heterologous animal components can be reduced. In addition, the organoid fusion model established by using the technology of the invention is easier to observe, deliver drugs and sample.

The invention relates to the field of pathologies affecting the central nervous system, particularly severe cerebral pathologies, especially those restricted by the presence of the blood-brain barrier (BBB): gliomas, brain metastases, neurodegenerative diseases (e.g., Alzheimer's, Parkinson's, or ALS), genetic diseases (Huntington's, myopathies, Leigh syndrome, Rett syndrome), but also to the field of cancers, musculoskeletal and immunological disorders, vascular diseases (thrombosis) in numerous organs (e.g., liver, kidney, or muscle) and in combination with numerous therapeutic approaches (e.g., chemotherapy, immunotherapy, targeted therapy, or gene therapy). The invention relates to a microbubble comprising a fluorinated polymer or copolymer and a fluorinated gas, its use, and intermediate polymer or copolymer compounds. Abbreviated figure: 0

This invention provides a nucleic acid aptamer that targets and binds to the IGF2BP2 protein and its application, belonging to the field of pharmaceutical technology. This invention is the first to design a highly specific nucleic acid aptamer targeting the RNA recognition protein IGF2BP2, obtaining a nucleic acid aptamer that can target and specifically bind to the IGF2BP2 protein (see SEQ ID No. 1-2). This nucleic acid aptamer can effectively inhibit the activity of tumor cells, tumor stem cells, and breast cancer brain metastases, breast cancer lung metastases, breast cancer liver metastases, breast cancer kidney metastases, and breast cancer bone metastases, providing a new drug component for the treatment of malignant and refractory tumors (especially glioblastoma and distant metastatic breast cancer). Furthermore, it was discovered that modification with N6-methyldeoxyadenosine monophosphate can further enhance the specificity of the nucleic acid aptamer and strengthen its efficacy in inhibiting tumor cell activity.

The present disclosure is directed to a method that involves selecting a subject having a primary tumor and obtaining, from the selected subject, a sample containing exosomes derived from primary tumor cells. The exosomes are isolated from the sample and expression levels of cell migration-inducing and hyaluronan-binding protein (CEMIP) are detected in the isolated exosomes.

The present invention relates to a method for predicting survival of non-small cell lung cancer patients with brain metastasis. More specifically, it proposes a method that is useful for predicting the survival of the patients by comparing TMTrg of the patients with cut off value for predicting long term survival.

The application belongs to the technical field of pharmaceutical preparations, and specifically discloses an acetyl gastrodin transdermal patch and a preparation method thereof. The transdermal patch takes acetyl gastrodin as an effective component, is encapsulated in cubic phase liposomes composed of glycerol monostearate, cholesterol and Pluronic F127, is dispersed in a complex matrix of hydroxypropyl methyl cellulose and ethyl cellulose, and is matched with a complex transdermal enhancer of glyceryl caprylate / caprate and ethanol. In the preparation, the liposome material is first melted to load the drug, and then drug-loaded cubic phase liposomes are formed through ice water bath ultrasonic treatment. Then, the drug-loaded cubic phase liposomes are mixed with the polymer matrix and excipients, are defoamed, are coated, and are dried in two steps to be shaped. The cubic phase liposomes are used to significantly improve the drug penetration rate and stability, realize 24-hour smooth drug release, efficiently penetrate the skin and the blood-brain barrier, significantly inhibit non-small cell lung cancer brain metastases, improve tumor secondary anxiety and depression, have excellent skin compatibility, and provide a new non-invasive synergistic treatment scheme for brain tumors and concurrent emotional disorders.

The invention provides a fourth-generation EGFR (epidermal growth factor receptor) inhibitor as well as a preparation method and pharmaceutical application thereof, and particularly, the fourth-generation EGFR inhibitor has a structure as shown in a formula I. Definitions of X, W, Q, T and Ar are as described in any embodiment of the invention. The compound disclosed by the invention is a fourth-generation EGFR (Epidermal Growth Factor Receptor) inhibitor, and can be used for effectively aiming at drug resistance mutation, such as C797S mutation, occurring after third-generation EGFR-TKI treatment. The compound has good blood-brain barrier penetrability and can effectively treat brain metastatic tumor. The compounds have good curative effects on different EGFR mutation sites in cell activity experiments, are expected to have good curative effects in various EGFR mutant cancers, and provide powerful support on targeted drugs for cancer treatment.

The present application discloses a treatment of EGFR mutation-positive non-small cell lung cancer with brain metastasis by administering an effective dose of an EGFR inhibitor. The EGFR inhibitor is N-(2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxy-5-((4-(1-deuteriomethyl-1H-indol-3-yl)pyrimidin-N'-2-yl)amino)phenyl)acrylamide methanesulfonate.

The invention provides an identification method and system for multi-omics analysis of lung cancer brain metastasis driving genes. The method comprises the following steps: data quality control: acquiring single-cell RNA sequencing data from a public data source, carrying out initial cell screening after standardization processing, removing low-quality data and ensuring the reliability of the data; a batch effect removing algorithm is adopted, technical deviation between batches is eliminated, and data consistency is ensured; the cells are grouped, the cells are divided into different subgroups through dimensionality reduction and clustering analysis, and the heterogeneity and diversity of the cells in the tumor microenvironment are revealed; inferring copy number variation, and inferring genome instability and possible canceration characteristics of the cells by analyzing the copy number variation in the single cell data; performing quasi-time sequence analysis, reconstructing a cell development or transformation process by utilizing the quasi-time sequence analysis, and exploring the change of cell fate in the brain metastasis process of the lung cancer; function enrichment analysis: carrying out function annotation on different cell subgroups, and identifying key pathways and molecular markers related to brain metastasis of lung cancer; and drug sensitivity analysis before and after radiotherapy: analyzing the sensitivity difference of different cell subgroups to drugs before and after radiotherapy, and providing a basis for an individualized treatment scheme.

The invention provides a combined medicine (such as a set preparation or a compound preparation) for treating advanced non-small cell lung cancer patients or advanced non-small cell lung cancer patients with brain metastasis, and the combined medicine contains ubenimex and afatinib which are far lower than the conventional dosage in low dosage. The treatment effect is equal to or better than that of afatinib with a conventional dosage, and basically no side effect exists; the use of low doses of ubenimex and afatinib for the manufacture of the above combination medicament for the treatment of the above patient; and a method of treating the cancer comprising administering the combination drug to the patient.