52 results about "Egfr mutation" patented technology

The invention relates to an application of alvitinib in preparation of an NLRP3 inflammasome inhibitor. The alvetinib is used for preparing a medicament for treating infectious shock, a medicament for treating acute liver injury and a medicament for treating peritonitis. A new choice is provided for prevention or treatment of NLRP3 inflammasome related diseases, the problem of treatment of EGFR mutation lung cancer patients combined with NLRP3 inflammasome related diseases (infectious shock / acute liver injury / acute peritonitis) is solved, tumor progression and inflammatory response are inhibited at the same time through the Aviitinib (third-generation EGFR-TKI), and the NLRP3 inflammasome related diseases are treated through the Aviitinib (third-generation EGFR-TKI). It is suggested that the medicine is preferentially selected by the patients, and the medicine with higher treatment potential is provided for treatment of infectious shock medicines, acute liver injury medicines and acute peritonitis.

The invention provides a primer probe set for digital PCR detection of non-small cell lung cancer EGFR mutation and application thereof, and relates to the technical field of digital PCR detection, the primer probe set comprises a primer pair and a probe for specific detection of EGFR gene exon 19 deletion mutation (19del) and exon 21 L858R point mutation, and the 19del mutation probe comprises a plurality of sequences to cover common subtypes. The primer probe group can be combined with a microfluidic digital PCR platform for use, a sample is divided into tens of thousands of microdroplets for amplification, and FAM, HEX, ROX and CY5 fluorescence channel signals are detected to realize absolute quantification. The system provided by the invention has high sensitivity and excellent linearity and precision, is particularly suitable for detecting extremely-low-frequency EGFR mutation in body fluid such as plasma, and has important application value in individualized diagnosis and treatment, curative effect monitoring and drug resistance evaluation of non-small cell lung cancer.

The invention discloses a method for constructing an osimertinib curative effect prediction model based on an elastic score and T790M mutation, and relates to the technical field of biological medicines, and the method is technically characterized in that the osimertinib curative effect prediction model based on the elastic score and the T790M mutation is constructed; the interaction mechanism between the radiomics characteristics and the EGFR mutation state is explored, so that a more accurate decision basis is provided for personalized clinical treatment, and the treatment effect is improved.

The invention relates to a compound for inhibiting EGFR (epidermal growth factor receptor) mutant cancer and a pharmaceutical application thereof. The present disclosure provides a compound of a specific chemical structure, or a pharmaceutically acceptable salt thereof, having an activity of inhibiting and / or degrading a mutant EGFR protein. The present disclosure also provides compositions comprising such compounds, or pharmaceutically acceptable salts thereof. The present disclosure provides a pharmaceutical use of a compound according to the present disclosure, a salt thereof, and a composition comprising the compound according to the present disclosure, a salt thereof, for the treatment or prevention of cancer with EGFR mutation, particularly lung cancer. The disclosure also provides methods for treating or preventing EGFR mutant cancer, particularly lung cancer, comprising administering to a subject in need thereof an effective amount of a compound according to the invention, a salt thereof, or a composition comprising a compound according to the invention, a salt thereof.

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 invention is applicable to the technical field of disease detection, and particularly relates to an EGFR mutation abundance detection system based on dual-threshold dynamic analysis, the system comprises: a sample processing unit, which is used for separating tissue DNA, is internally provided with a micro-fluidic chip, and is used for quantitatively extracting nucleic acid; the PCR amplification unit is used for amplifying EGFR (epidermal growth factor receptor) sensitive mutation through multiple fluorescent PCR; the signal acquisition unit is used for capturing fluorescence signal intensity through a high-precision photoelectric sensor; the core processing unit is used for executing a dual-threshold abundance grading algorithm through the embedded chip; and the output terminal is used for displaying the abundance level and treatment suggestions through a touch screen. Fluorescence signals are captured through the high-precision photoelectric sensor, the EGFR abundance can be accurately recognized, a basis is provided for achieving an accurate medication scheme for an EGFR sensitive mutation NSCLC patient according to the EGFR abundance, and the detection precision is improved.

This invention provides a DNA origami-based nanoscale ruler and its application. The nanoscale ruler includes a substrate structure, fluorescent indicator chains, and spacing indicator chains. The substrate structure is a three-layer rectangular structure constructed using DNA origami technology to maintain the basic configuration of the nanoscale ruler. Several fluorescent indicator chains are distributed on the first surface of the substrate structure according to a predetermined rule. These fluorescent indicator chains emit fluorescent signals through their fluorescent groups under specific excitation light. Two spacing indicator chains are disposed on the first surface of the substrate structure, forming a predetermined distance between them. These spacing indicator chains are used to target and bind to receptor proteins on the cell membrane via ligand proteins. One technical advantage of this invention is its rational design, which not only enables rapid and accurate determination of the presence of EGFR mutations in tissue samples but also effectively shortens the time required to determine the presence of EGFR mutations.

The application belongs to the field of diagnosis and treatment, and particularly relates to a lung cancer EGFR mutation non-invasive prediction model based on unsupervised decoupling and gate fusion. A multi-modal fusion model is constructed based on enhanced CT images and clinical data of non-small cell lung cancer patients. The application adopts a mask image modeling task, and autonomously learns morphological and texture primitive features of tumors from three-dimensional enhanced CT images without EGFR mutation labels. The application overcomes the dependence on a large amount of labeled data, enables the model to learn visual representations with high discriminability and generalization ability from unlabeled data, and significantly improves feature expression capability. A multi-modal fusion architecture based on a gate mechanism is designed, which can dynamically adjust the contribution weights of deep features, imaging features and clinical information in different samples. Personalized feature fusion for different cases is realized, the limitations of traditional static fusion methods are overcome, and complementary information between multi-source heterogeneous data is fully mined.

The application discloses a heterocyclic EGFR mutation inhibitor in the field of pharmaceutical chemistry, which is a heterocyclic compound shown in general formula I or a stereoisomer or optical isomer thereof or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, p, X, Y, Z, W, Cy1 and Cy2 are as defined in the claims. The main effect of the heterocyclic EGFR mutation inhibitor is to exert an antitumor effect by inhibiting a mutant EGFR.

The application belongs to the field of biomedicine, and particularly relates to application of fibroblasts in disease treatment; and specifically discloses application of ANXA6 gene in preparation of a diagnostic preparation for treating EGFR mutation-mediated diseases, wherein when overexpression of the ANXA6 gene in CAF cells is detected, the EGFR mutation-mediated diseases cannot be treated by using EGFR targeted drugs; further, the EGFR targeted drugs are epidermal growth factor receptor tyrosine kinase inhibitors (EGFR-TKIs).

The invention belongs to the technical field of gene engineering and cell engineering, particularly relates to an osimertinib-resistant human lung adenocarcinoma cell line BCH-LUNK1 fused with EGFR (epidermal growth factor receptor) mutation and TPM3-NTRK1 gene, and further discloses a construction method and application of the osimertinib-resistant human lung adenocarcinoma cell line BCH-LUNK1. The human lung adenocarcinoma cell line BCH-LUNK1 disclosed by the invention is a human lung adenocarcinoma cell line with EGFR (Epidermal Growth Factor Receptor) mutation and TPM3-NTRK1 gene fusion, and is preserved in the China General Microbiological Culture Collection Center (CGMCC), and the preservation number is CGMCC No.46021. According to the invention, a stable human lung adenocarcinoma cell line is successfully established, and the cell line has EGFR19 exon mutation and TPM3-NTRK1 gene fusion at the same time, and is a good model for researching EGFR targeted therapy drug resistance mechanism, and screening and drug resistance mechanism research of NTRK targeted inhibitors.

This invention belongs to the field of tumor biology and drug screening technology, specifically disclosing a human EGFR mutation-driven mouse primary lung cancer cell line, its construction method, and its applications. The cell line, ZST-1, is a human EGFR (L858R / T790M) mutation-driven lung cancer cell line derived from mouse primary lung cancer. It is stable, capable of subcutaneous tumor formation in C57BL / 6 mice, and simultaneously expresses Luciferase and tdTomato reporter genes. Its construction method includes obtaining transgenic mice, virus-induced tumor formation, continuous in vivo passage in nude mice, and in vitro culture and screening steps. This cell line can be applied to in vitro screening and efficacy evaluation of human EGFR mutation-targeting drugs, research on EGFR-TKI resistance mechanisms, tumor bioluminescence imaging and fluorescence tracing, and in vivo tumorigenesis and efficacy experiments in an immune-intact C57BL / 6 background.

The present application provides a method of treating a cancer in a subject in need thereof, where it has been determined that the cancer in the subject comprises one or more atypical epidermal growth factor receptor (EGFR) mutations, comprising administering to the subject (R)-N-(2-(4-(4-cyclopropylpiperazin-1-yl) piperidin-1-yl)-5-((6-(3-(3, 4, 5, 6-tetramethyl-3-piperidin-1-yl)-5-(4-(4-cyclopropylpiperazin-1-yl) piperidin-1-yl)-5-(4-(4-cyclopropylpiperazin-1-yl) piperidin-1-yl)-5-( The present invention relates to a pharmaceutically acceptable salt of 4-(4-(4-(4-(4-(4-(4-(4-(4-(4-(4-(4-(4-(4-(4-(4-(4-(4-(4-(4-(4-(4-(4-(4-(4-(

Disclosed herein are plinabulin and its use for treating a cancer or tumor characterized by expression of a mutant form of an epidermal growth factor receptor (EGFR) protein, comprising administering plinabulin to a subject in need thereof.

The invention relates to an application of osimertinib combined with chidamide in treatment of osimertinib drug-resistant lung cancer, and particularly relates to the following aspects: (1) osimertinib is an epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI), and shows a remarkable curative effect in treatment of non-small cell lung cancer (NSCLC) patients carrying specific EGFR mutation; (2) chidamide is a novel oral HDACi, can induce cell apoptosis, cell cycle arrest and cell growth inhibition, and shows good tolerance and antitumor activity in various cancer types; and (3) chidamide is taken as an epigenetic regulating agent and can be in synergistic effect with osimertinib, so that the capability of killing lung cancer cells is enhanced. The invention belongs to the technical field of medicines, and particularly provides application of osimertinib combined with chidamide in treatment of osimertinib drug-resistant lung cancer.

To provide a new generation of receptor tyrosine kinase inhibitors that spare wild-type EGFR, penetrate the blood-brain barrier, and show specific activity against exon 20 insertions and / or drug-resistance mutations.SOLUTION: Disclosed are amino-substituted heteroaromatic compounds, for example 4-amino-quinazolines, pharmaceutically acceptable salts of the compounds, and pharmaceutical compositions thereof. Also disclosed are methods of treating or preventing cancer using the amino-substituted heteroaromatic compounds, pharmaceutically acceptable salts of the compounds, and pharmaceutical compositions thereof.SELECTED DRAWING: None

This invention relates to a system, kit, and application for the one-pot detection of miRNA and DNA mutations based on CRISPR-Cas12a and aptamers, belonging to the field of biomedical technology. The system for the one-pot detection of miRNA and DNA mutations based on CRISPR-Cas12a and aptamers includes: Cas12a protein, crRNA-R targeting miRNA, aptamer P1, aptamer P2, a linker, AO, and crRNA-D targeting DNA mutations. This invention combines CRISPR / Cas12a with a aptamer-based detection strategy to develop a label-free, direct detection system compatible with smartphones. This system can simultaneously detect EGFR mutations and miRNA-21 expression levels.

The present disclosure provides compounds of specific chemical structures or pharmaceutically acceptable salts thereof, which have the activity of inhibiting and / or degrading mutant EGFR proteins. The present disclosure also provides compositions comprising such compounds or pharmaceutically acceptable salts thereof. The present disclosure provides the use of the compounds, salts thereof and compositions comprising the compounds, salts thereof according to the present disclosure for the treatment or prevention of cancers with EGFR mutations, especially lung cancer, as medicaments. The present disclosure also provides a method for the treatment or prevention of EGFR mutant cancers, especially lung cancer, which method comprises administering to a subject in need of treatment an effective amount of a compound, a salt thereof according to the present invention or a composition comprising the compound, a salt thereof according to the present invention.

The present invention provides a delivery system for targeted inhibition of epidermal growth factor receptor (EGFR), comprising RNA capable of inhibiting EGFR gene expression; the RNA capable of inhibiting EGFR gene expression comprises a promoter element and at least one of an siRNA capable of inhibiting EGFR gene expression and an encoding siRNA. Compared to existing technologies, the present invention has the following advantages: the delivery system is based on synthetic biology elements, utilizing mammalian organs as natural bioreactors. The targeting element and the RNA capable of inhibiting EGFR gene expression are self-assembled within the mammalian body into a composite structure capable of targeted treatment of EGFR mutation-related diseases, which is then secreted into the circulatory system. Furthermore, under the action of the targeting element, the composite structure transports the RNA to tumor cells awaiting treatment, exerting its therapeutic effect, resulting in excellent therapeutic efficacy and high efficiency.

This invention discloses a bivalent ligand molecule targeting EGFR and its applications, belonging to the field of drug development technology. Its general structural formula is: [Formula omitted for brevity], where L is a linking group, and M1 and M2 are EGFR protein ligands. This invention forms a bivalent EGFR ligand molecule by covalently linking two EGFR ligands through a linking group. This bivalent ligand molecule can induce additional protein-protein interactions between EGFR monomers, which greatly enhances the binding strength and stability of the drug to EGFR, thereby overcoming the drug resistance problem of traditional EGFR inhibitors and providing a new treatment strategy for cancer patients carrying EGFR mutations and other patients with other diseases.

The present invention relates to a biomarker and an information provision method, for predicting whether or not a mutation is present in an epidermal growth factor receptor (EGFR) by utilizing single-cell multi-omics analysis in a non-small cell lung cancer (NSCLC) patient, and predicting responsiveness to immune checkpoint inhibitor (ICI) therapy. The present invention provides, as an information provision method for predicting responsiveness to ICI therapy in an NSCLC patient, the information provision method comprising the steps of: analyzing a sub-population composition ratio of CD8-positive T cells by performing single-cell multi-omics analysis of a lung sample of a patient; and measuring the frequency of dysfunctional CD8 T cells (CD8_Td) and the frequency of naive-like cells (CD8_Tn) among the CD8-positive T cells, wherein, when the frequency of CD8_Td decreases and the frequency of CD8_Tn increases in EGFR mutation-positive patients, it is predicted that responsiveness to ICI therapy is low.

The present invention relates to use of an EGFR inhibitor in the preparation of a medicament for treating an EGFR mutation co-occurring with a deleterious mutation and a method for treating the described disease. Specifically, disclosed is use of a compound of formula I or a pharmaceutically acceptable salt thereof in the preparation of a medicament for treating a disease related to an EGFR mutation co-occurring with a deleterious mutation in a subject. The medicament, when administered to a subject with a disease related to an EGFR mutation co-occurring with a deleterious mutation, provides one or more of the following improvements: improved progression-free survival (PFS) or improved overall survival (OS).

The present invention relates to treatment of subjects having EGFR exon 20 insertion and other uncommon EGFR mutations.

The invention relates to the technical field of biological medicine, in particular to application of siRNA of targeted RAC1B in preparation of medicine for treating lung cancer. The siRNA of the targeted RAC1B provided by the invention can avoid the effect on healthy tissues due to the targeted RAC1A; the obvious anti-tumor effect on the lung adenocarcinoma is shown in cell lines, organoids and patient-derived xenotransplantation tumor models, and a new target spot and a new medicine are provided for treating the lung adenocarcinoma; a combined anti-tumor effect on EGFR mutation positive lung adenocarcinoma is shown in organoid and patient-derived xenotransplantation tumor models, and a new treatment strategy is provided for EGFR mutation lung adenocarcinoma.

The invention relates to an EGFR mutation inhibitor and application thereof. Particularly, the invention relates to an EGFR mutation inhibitor with a structure shown in a formula (I), a pharmaceutical composition of the EGFR mutation inhibitor, application of the EGFR mutation inhibitor as the EGFR mutation inhibitor and application of the EGFR mutation inhibitor in preparation of drugs for treating cancers, tumors or metastatic diseases which are at least partially related to EGFR Del19 mutation, EGFR L858R mutation, EGFR L858R / C797S double mutation, EGFR Del19 / C797S double mutation, L858R / T790M / C797S three mutation and Del19 / T790M / C797S three mutation, the invention particularly relates to application in preparation of drugs for treating hyperproliferative diseases and cell death disorder inducing diseases. Wherein the definition of each substituent in the formula (I) is the same as the definition in the specification.

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 discloses a Chinese and western medicine composition and a preparation method and application thereof, and belongs to the technical field of anti-lung cancer targeted drugs, the traditional Chinese medicine composition and EGFR-TKI cooperate to treat EGFR mutation advanced non-small cell lung cancer, the lifetime of a patient is prolonged, the treatment effective rate is increased, the life quality is improved, and the side effect of the targeted drugs is relieved. Compared with EGFR-TKI single medicine treatment, the traditional Chinese medicine composition is combined with EGFR-TKI, proliferation of HCC827 lung cancer cells is remarkably enhanced and inhibited, cell apoptosis is promoted, cycle division of cells is interfered, the traditional Chinese medicine and western medicine composition provided by the invention has the advantages that by regulating and controlling tumor cell energy metabolism and regulating and controlling expression of metabolism-related proteins LDHA, HK2, GLUT1 and HIF-1alpha, the effect of inhibiting HCC827 lung cancer cells is achieved, and the curative effect of the HCC827 lung cancer cells is improved. Therefore, effective control of the advanced non-small cell lung cancer is realized.

The present invention relates to treatment of subjects having EGFR exon 20 insertion and other uncommon EGFR mutations.