11 results about "Gefitinib" patented technology

The application discloses a fluorescence enhancement anchor agent based on a fluoroboron dipyrrin-tetrazine dye for inflation microscopy technology, and belongs to the technical field of biochemical analysis. The fluorophore of the fluorescence enhancement anchor agent is shown in formula (I), formula (II) or formula (III): the tetrazine group carried by the fluorescence enhancement anchor agent is removed from fluorescence quenching through a biological orthogonal reaction with a drug probe, and the drug probe is shown in formula (IV): the fluorescence enhancement anchor agent can covalently and non-covalently anchor small molecules in a hydrogel network based on a tetrazine biological orthogonal reaction, and realizes inflation microscopic fluorescence imaging of a double fluorescence enhancement mechanism. In addition, the drug probe selects a non-covalent drug, gefitinib, as a probe core, is modified with a BCN click handle, and successfully realizes in-situ fluorescence inflation microscopic imaging of an EGFR drug-target, thereby providing a new tool for research and clinical research on non-covalent drug target co-localization information of exosomes.

Disclosed are methods of treating cancer with a tri-agent therapy. The methods include a cancer treatment regimen with two or three different antineoplastic medications, including tamoxifen, gefitinib, and vinorelbine (TGV). The cancer treatment regimen can include sequential and / or concurrent administration of tamoxifen, gefitinib, and vinorelbine. The cancer treatment regimen can include sequential and / or concurrent administration of tamoxifen and gefitinib as adjuvants to a prescribed treatment. The cancer treatment regimen can be cyclical or can be a continuous metronomic treatment with metronomic dosing. The cancer treatment regimen can be cyclical and then can be followed by a continuous metronomic treatment with metronomic dosing.

This invention provides hepatocellular carcinoma-derived growth factor (HDGF) as a target for resistance to tyrosine kinase inhibitors and its related applications. This invention provides the application of HDGF as a target in screening and / or preparing drugs that can improve resistance to tyrosine kinase inhibitors in patients. This invention discovers that high expression of HDGF is one of the mechanisms of resistance to molecularly targeted drugs such as gefitinib and other tyrosine kinase inhibitors. Targeting HDGF can effectively improve resistance to gefitinib in NSCLC and enhance therapeutic efficacy.

This invention discloses the application of fruquintinib combined with PD-1 monoclonal antibody in maintenance therapy for HER-2 negative advanced gastric cancer / geoesophageal junction adenocarcinoma, belonging to the field of tumor treatment technology. This invention targets HER2-negative advanced gastric cancer or gastroesophageal junction adenocarcinoma, specifically patients who achieve disease control after 3 months of first-line induction therapy with PD-1 monoclonal antibody combined with oxaliplatin, followed by maintenance therapy with fruquintinib combined with PD-1 monoclonal antibody without chemotherapy. The maintenance therapy regimen provided by this invention improves patients' quality of life and prolongs overall survival while delaying disease progression, and has significant clinical implications.

The invention provides an SLC16A3 inhibitor based on ferroptosis regulation and application of the SLC16A3 inhibitor in lung adenocarcinoma, and relates to the technical field of biological treatment drugs. The SLC16A3 inhibitor is a drug MSC-4381, the drug MSC-4381 is an effective SLC16A3 inhibitor, the SLC16A3 inhibitor can be used for inhibiting lactic acid transporter SLC16A3, breaking the redox steady state of tumor cells, inducing ferroptosis and remarkably enhancing the curative effect of the drug gefitinib, and in an in-vivo and in-vitro model, cell proliferation, migration and invasion can be inhibited through SLC16A3 knock-down or pharmacological inhibition, so that the SLC16A3 inhibitor can be used for preventing and treating the tumor cells. The MSC-4381 and the gefitinib are combined to promote lipid peroxidation and iron ion accumulation, the tumor growth can be obviously delayed through drug combination of the MSC-4381 and the gefitinib, the effect can be partially reversed through the Ferrostatin-1, the ferroptosis-dependent mechanism of the MSC-4381 and the gefitinib is verified, and transcriptional regulation and control of the SLC16A3 by the HIF1A and influence on ferroptosis resistance are clear. The invention provides a feasible combined medication strategy, verifies the significant tumor inhibition effect of the HIF1A-SLC16A3 axis in cell and animal models, reveals the key effect of the HIF1A-SLC16A3 axis in lung adenocarcinoma drug resistance formation, and provides a new combined treatment strategy and a new molecular target.

The application discloses a composite nano-silicon ball drug delivery system and a preparation method and application thereof. The system takes mesoporous silica nanoparticles as a carrier, loads gefitinib, and is coated with a PD-L1 antibody modified platelet membrane on the surface. The application prepares a composite multifunctional mesoporous silica nanoparticle which loads gefitinib and is coated with a PD-L1 antibody modified platelet membrane on the surface, so that the composite multifunctional mesoporous silica nanoparticle can be directed to reach a tumor surgery blood vessel damage site, kill residual tumor cells, reduce matrix hardness in the microenvironment, enhance the permeability and toxicity of immune cells, the two effects are interdependent and mutually enhanced, and the application overcomes the invalidity of colorectal tumor immunotherapy and prolongs the survival period of patients.

The invention discloses a macrocyclic cytochalasin derivative as well as a preparation method and application thereof. The macrocyclic cytochalasin derivative comprises the macrocyclic cytochalasin derivative disclosed by the invention, and the macrocyclic cytochalasin derivative can obviously inhibit the proliferation of non-small cell lung cancer (H1975), and the inhibitory activity of part of compounds obviously exceeds that of positive control gefitinib. Wherein the efficacy of the compound 8 is equivalent to that of cis-platinum in H1975 cells, the efficacy of the compound 8 is better in HCC827 cells, and the toxicity of the compound 8 to normal cells is lower than that of the cis-platinum.

Provided are an shRNA for reversing EGFR-TKI drug resistance in non-small cell lung cancer and use thereof, belonging to the fields of molecular biology and biomedicine. By using the designed shRNA, the expression of the KLHL22 gene is targeted and inhibited, and the nucleotide sequence of the shRNA is set forth in SEQ ID No. 1-SEQ ID No. 2. It is found by means of in vivo experiments that targeted inhibition of KLHL22 expression can effectively reverse the drug resistance of NSCLC cells to EGFR-TKI. In in vitro cell experiments, inhibition of KLHL22 expression significantly improves the sensitivity of drug-resistant NSCLC cells to gefitinib, thereby restoring the anti-tumor effect of the drug. This innovative strategy provides a new direction for overcoming EGFR-TKI drug resistance, and has important clinical application prospects.

The invention discloses a polypeptide for inhibiting lung adenocarcinoma metastasis and application thereof, belongs to the technical field of biology, and aims to solve the problems that lung adenocarcinoma cells in the prior art have very strong invasion and migration ability, and non-small cell lung cancer patients with high expression of NSUN2 easily generate drug resistance to gefitinib drugs. The amino acid sequence of the polypeptide for inhibiting lung adenocarcinoma metastasis is as shown in a general formula X-RHTQIRPTMFPPY; x at the N terminal in the general formula represents a modification group, and Y at the tail represents a cell-penetrating peptide; the invention is suitable for preparing a therapeutic reagent for lung cancer, and can achieve the effect of inhibiting the methylation modification of NSUN2 so as to inhibit the metastasis of lung adenocarcinoma.

The application belongs to the technical field of pharmaceutical chemistry, and relates to a gefitinib pharmaceutical co-crystal and a preparation method thereof. The application specifically provides a co-crystal formed by gefitinib and malonic acid in a molar ratio of 1:2. The gefitinib pharmaceutical co-crystal provided by the application has high solubility and good solubility, is helpful to improve the bioavailability, and has important value for optimization and development of gefitinib preparations.

Disclosed are a composition comprising a TLR4 / MD2 pathway inhibitor and an EGFR inhibitor, a pharmaceutical composition comprising the composition, and the use of the composition / pharmaceutical composition in cancer treatment. The TLR4 / MD2 pathway inhibitor and the EGFR inhibitor can synergistically kill a variety of cancers, including cutaneous melanomas, and have a significant inhibitory effect on the growth of cancer cells without affecting bodyweight of mice. Moreover, compared with separate administration of the individual components, the composition according to the present disclosure can delay the occurrence of drug resistance in tumor-bearing mice and significantly inhibit the growth of Gefitinib-resistant cancer cells (e.g., non-small cell lung cancer tumors). Therefore, the composition according to the present disclosure can be used for preparing safe and effective anti-tumor medicament.