23 results about "Apatinib" patented technology

The invention relates to application of a retinoic acid compound in preparation of a medicine for treating and / or preventing glioblastoma. Compared with the prior art, the retinoic acid compound (1uM, 5uM) group has the advantages that the tumor inhibition rate of a glioblastoma organ is higher than that of an apatinib (1uM, 5uM) group, and is higher than that of an apatinib (1uM, 5uM) group. The subcutaneous tumor inhibition rate of glioblastoma cells of a retinoic acid compound (0.5 mg / kg and 5mg / kg) group is higher than that of an apatinib (32.5 mg / kg) group, and is higher than that of the apatinib (32.5 mg / kg) group in tumor pathological blood vessel inhibition rate. Therefore, the medicine (retinoic acid compound) for treating and (or) preventing the glioblastoma has a remarkable treatment and (or) preventing effect on the glioblastoma.

The invention discloses an application of imatinib mesylate in preparation of a targeted therapeutic drug for gastric signet ring cell carcinoma. The imatinib mesylate has an obvious inhibition effect on the growth of six patients with the pathological type of gastric signet-ring cell carcinoma, the inhibition effect is more obvious along with the increase of the concentration, the concentration and dosage dependency relationship is shown, and the half inhibitory concentration (IC50) is obviously smaller than that of a positive control drug apatinib. The medicine can play a targeted therapeutic role on the gastric signet ring cell carcinoma, and is small in toxic and side effects, economical, practical and low in cost.

The present application relates to a kind of pharmaceutical composition for treating advanced gastric cancer, in particular, the pharmaceutical composition of pill soup stacking medicine method.The composition includes radix astragali, pungent turmeric, radix comphorae etc.Ingredients are mixed into decoction according to specific proportion, combined with Xi Huang pill and apatinib.The decoction has the effect of strengthening body resistance and consolidating foundation, while the pill is mainly used to attack and remove the metastasis into collaterals, and remove stasis and toxicant to eliminate mass.A series of clinical cases verify that the therapy shows significant efficacy on patients with advanced gastric cancer, and no serious adverse reactions are found.

This invention provides the application of apatinib in the preparation of antiviral drugs, specifically involving the application of the anticancer drug apatinib in inhibiting the replication of Hantanensis virus (HTNV) and Chikungunya virus (CHIKV). Apatinib can significantly inhibit HTNV replication and reduce viral titers at the cellular level. Experiments have shown that after treatment with apatinib, the expression levels of viral structural proteins, the nucleic acid levels of HTNV, and the viral titers in the cell culture supernatant were significantly reduced in HTNV-infected A549 cells, while the drug exhibited low cytotoxicity. Furthermore, apatinib can also inhibit CHIKV replication. This invention provides a novel anti-HTNV candidate drug and offers insights for the rapid development of antiviral drugs.

The present application belongs to the technical field of medicine, and particularly relates to a NAMPT inhibitor, a composition, a preparation method and use, a structural formula of which is: or R 1 H or Br; M is C or N, Y is C or N, Z is C or N; n=0, 1 or 2, or L is an amino group, a thiourea group, a urea group, R 2 H, CH3, CF3, OCH3, F or Cl; R is H, a methyl group, an ethyl group, an isopropyl group or a cyclopropyl group; X is F, Cl or Br; the compound of the present application is determined by an MTT method to have an effect of inhibiting proliferation of gastric cancer cells, has significant anti-gastric cancer activity, and has higher activity than that of apatinib at a cell level, and can be used for preparing an anti-gastric cancer drug.

The invention discloses an apatinib-immune synergistic nano-drug based on bacterial source vesicles as well as a preparation method and application of the apatinib-immune synergistic nano-drug. The nano-drug is Apatinib-MVs, and the nano-drug takes a membrane vesicle secreted by parabacteroides coumarini as a carrier to entrap an anti-angiogenesis drug apatinib; in-vitro anti-tumor experiment results show that the nano-drug can exert an efficient anti-tumor effect through a dual synergistic mechanism of inhibiting tumor angiogenesis and activating anti-tumor immune response at the same time.

The invention discloses an engineered bacterial vesicle co-loaded with apatinib and a PD-L1 antibody and a preparation method and application thereof.According to the engineered bacterial vesicle, an outer membrane vesicle derived from coprobacterium rodent serves as a carrier, a chemotherapeutic drug apatinib is loaded in the engineered bacterial vesicle, the surface of the engineered bacterial vesicle is modified with the PD-L1 antibody through chemical coupling, and the engineered bacterial vesicle is named as Apatinib-MVs alpha PD-L1; the engineered bacterial vesicle can synergistically deliver apatinib and a PD-L1 antibody to a breast cancer focus, so that synergistic interaction of chemotherapy and immunotherapy is realized; in-vitro experiments show that the engineered bacterial vesicles can significantly inhibit proliferation, migration and invasion of breast cancer cells; in-vivo experiments show that the compound can effectively inhibit tumor growth and remarkably increase infiltration of CD8 + T cells in a tumor microenvironment, and a new drug delivery platform is provided for combined treatment of breast cancer.

A method for predicting curative effect of glioblastoma and preparing related drugs belongs to the field of biological medicine, and characterizes N-glycome spectrums in a cerebrospinal fluid sample paired before and after treatment of a glioblastoma patient by using a hydrophilic interaction liquid chromatography combined fluorescence detection and mass spectrometry technology. After chromatographic and mass spectrometric data are analyzed by a computer, the treatment effect of glioblastoma, especially the treatment effect of apatinib, can be predicted or judged through changes of LacdiNAc, sialylation level and core fucosylation level, guidance is provided for a patient to select a treatment scheme, and the method can be used for preparing a medicine for treating glioblastoma.

The invention provides an apatinib-loaded engineered exosome as well as a preparation method and application thereof, belongs to the technical field of ophthalmic preparations, and aims to solve the problem of low bioavailability of current eye drops. The preparation method comprises the following steps: step 1, preparing APA-loaded PLGA nanoparticles; step 2, separating the HCE-EXs; step 3, preparing the Apa nano particles wrapped by the HCE-EXs; step 4, preparing a phospholipid polymer modified by arginine; and 5, mixing the HCE-EXs coated APa nanoparticles prepared in the step 3 with the arginine modified phospholipid polymer prepared in the step 4, incubating the mixture at 37 DEG C for 30 minutes, and removing free impurities through volume exclusion chromatography to obtain the engineered exosome. The engineered exosome can release nitric oxide (NO) to effectively solve oxidative stress after corneal alkali burn. Secondly, compared with traditional medicine eye drops, the engineered exosome can be retained in cornea for a long time to continuously release apatinib for treatment.

The application provides a slightly acid response type biomimetic nanovesicle and a preparation method and application thereof. The outer layer of the slightly acid response type biomimetic nanovesicle is composed of a PD-1 biological cell membrane, and apatinib is loaded into the slightly acid response type PEG-PAEs nanoparticle hydrophobic inner core. Apa-PPNP@mPD-1, as a new dosage form of combined administration of a small molecule inhibitor and a large molecule inhibitor, can precisely co-deliver apatinib and PD-1 protein to tumor tissues, release the drug in response to the slightly acid environment of the tumor, has a significant treatment effect of tumor growth regression and effective inhibition of lung metastasis, and also avoids toxic side effects on normal tissues, and has good biocompatibility.

The invention belongs to the technical field of biological medicine, and particularly relates to an apatinib-loaded engineered bacterial membrane vesicle and a preparation method and application thereof.The engineered bacterial membrane vesicle is prepared by mixing apatinib and a membrane vesicle derived from rodent bacillus in a PBS according to a specific mass ratio; incubating at 37 DEG C for 4 hours, removing free drugs by using a 100kDa ultrafiltration membrane, and concentrating; and washing with PBS to obtain a final product. Experimental results show that the engineered bacterial membrane vesicles can effectively inhibit malignant biological behaviors such as proliferation of breast cancer cells and significantly inhibit tumor growth in an animal model; mechanism research shows that the compound can effectively activate the anti-tumor immune response of the body; safety evaluation shows that the engineered bacterial membrane vesicle has no toxic or side effect; in conclusion, the engineered bacterial membrane vesicle provided by the invention has dual advantages of chemotherapy and immunotherapy, is good in safety, and has important application value in development of breast cancer treatment drugs.

The application discloses application of sunitinib malate in preparation of a targeted treatment drug for gastric signet ring cell carcinoma. Sunitinib malate has obvious inhibitory effect on growth of organoids from five patients with gastric signet ring cell carcinoma, and the inhibitory effect is more obvious with the increase of the concentration, and presents a concentration-dose dependent relationship, and a half maximal inhibitory concentration (IC50) is obviously smaller than that of a positive control drug, apatinib. The application can play a targeted treatment role on gastric signet ring cell carcinoma, has small toxic and side effects, is economical and practical, and is low in cost.

The invention discloses a parabacteroides coumarini vesicle nano preparation for PD-L1 targeted synergistic chemotherapy as well as preparation and application of the parabacteroides coumarini vesicle nano preparation. The nano preparation takes a parabacteroides coumarini-sourced membrane vesicle as a carrier, a chemical drug apatinib is loaded in the nano preparation, the surface of the nano preparation is modified with an anti-PD-L1 antibody through chemical coupling, and the nano preparation is named as Apatinib-MVsaPD-L1; according to the nano preparation, apatinib and a PD-L1 antibody can be synergistically delivered to a breast cancer focus, so that the synergistic interaction of chemotherapy and immune checkpoint blocking is realized; in-vitro experiments show that the nano preparation can significantly inhibit proliferation of breast cancer cells and induce apoptosis of the breast cancer cells; in-vivo experiments show that the compound can effectively inhibit tumor growth and remarkably increase infiltration of CD8 < + > T cells and TNF-alpha < + > CD8 < + > T cells in a tumor microenvironment, has no toxic or side effect, and provides a new safe and efficient drug delivery platform for combined treatment of breast cancer.

The invention belongs to the technical field of antitumor drug preparations, and relates to an antitumor drug apatinib mesylate tablet and a preparation method thereof. The apatinib mesylate tablet is composed of apatinib mesylate lipidosome and pharmaceutically acceptable auxiliary materials, apatinib mesylate is entrapped in a lipid material by using a lipidosome technology, and the apatinib mesylate tablet is prepared by optimizing a carrier material and a preparation process. The apatinib mesylate liposome and pharmaceutically acceptable auxiliary materials are prepared into tablets, and an acceleration test proves that compared with apatinib mesylate tablets sold in the market, the apatinib mesylate tablets have more excellent stability.

The invention relates to the technical field of medical data processing, and particularly discloses an apatinib medication monitoring information analysis system for an ovarian cancer patient. The system comprises a module for acquiring pharmacodynamic data of apatinib on an ovarian cancer patient, a module for detecting blood after the ovarian cancer patient uses apatinib, a proteome chip module, an apatinib medication evaluation module and an apatinib medication model verification module, the pharmacodynamic data acquisition module of apatinib for ovarian cancer patients can quickly complete screening of organism physiological change data of apatinib drugs in the first stage, the second stage and the third stage, and the blood detection module and the proteome chip module are combined after the ovarian cancer patients use apatinib. The quality of the apatinib medication evaluation model of the ovarian cancer patient can be visually shown, the established model is good in apatinib medication data applicability of the ovarian cancer first stage, and an analysis method and basis can be provided for apatinib medication data analysis of the ovarian cancer first stage patient.

The invention belongs to the technical field of medicine, and particularly relates to an NAMPT inhibitor, a composition, a preparation method and application, the structural formula is # imgabs0 # or # imgabs1 # R1 is H or Br; m is C or N, Y is C or N, and Z is C or N; n = 0, 1 or 2, or # imgabs2 is # imgabs3, # L is an amino group, a thiourea group or a ureido group, # imgabs4, # imgabs5, # R2 is H, CH3, CF3, OCH3, F or Cl; r is H, methyl, ethyl, isopropyl or cyclopropyl; x is F, Cl or Br; the compound has the effect of inhibiting gastric cancer cell proliferation through MTT method determination, has remarkable anti-gastric cancer activity, has higher activity than apatinib on the cellular level, and can be used for preparing anti-gastric cancer drugs.

The invention belongs to the field of medicine, and relates to injectable photo-thermal response type liposome hydrogel and a preparation method thereof, the injectable photo-thermal response type liposome hydrogel comprises injectable hydrogel, IR820 and drug-containing thermosensitive liposome, and the IR820 and the drug-containing thermosensitive liposome are co-loaded on the injectable hydrogel; the drug-containing thermosensitive liposome comprises a thermosensitive liposome Lip and a pharmaceutical composition co-loaded on the thermosensitive liposome Lip, the pharmaceutical composition is prepared from bufalin Bu and apatinib Ap. The injectable photo-thermal response type liposome hydrogel for treating colon cancer and the preparation method provided by the invention have the advantages of high precision, strong persistence and good stability.

The invention discloses a method for creating a vascular endothelial factor inhibitor adverse reaction prediction system. The method comprises the following steps: preselecting ten machine learning models as alternative prediction models; constructing a data set for training and testing the alternative prediction system; the data set is divided into a training set and a test set, the training set is used for training alternative prediction systems, the test set is used for testing the trained alternative prediction systems, AUC values are used for evaluating all the trained alternative prediction systems, and finally the AUC value of the random forest is the highest. And outputting the trained random forest as a prediction system for the adverse reaction of the vascular endothelial factor inhibitor. The random forest obtained by the invention supports risk prediction of three VEGFI drug use scenes of bevacizumab, apatinib and anlotinib, and has good generalization and high prediction accuracy and reliability.

The application discloses a kind of pharmaceutical composition, medicine and application for treating tumor, belong to combined medication technical field.The application provides a kind of pharmaceutical composition for treating tumor, antiangiogenic drug and HIF-1a inhibitor are combined with drug.The application proves that the hypoxic microenvironment of antiangiogenic therapy induced gastric cancer promotes the accumulation of intracellular HIF-1a, and HIF-1a reprograms the hypoxia tolerance of cell by enhancing glucose metabolism, so that gastric cancer cells maintain viability in hypoxic microenvironment.The application can produce synergistic complementary effect by the way of combined treatment of antiangiogenic drug apatinib and HIF-1a inhibitor CAY10585: aggravate intratumoral hypoxia of gastric cancer, block glucose metabolic reprogramming of gastric cancer cells, and then enhance anti-tumor effect, inhibit the progress of gastric cancer.

The present invention belongs to the technical field of pharmaceutical preparations, and provides an apatinib mesylate tablet and a preparation method thereof. The apatinib mesylate tablet prepared by the present invention effectively improves the dissolution of the tablet by adding powdered hydroxylated soybean lecithin and meglumine. The tablet preparation process is simple, and the tablet product quality is stable.

The application provides a kind of drug composition in the preparation for the application of the drug for the maintenance treatment of disease control ES-SCLC after first-line chemotherapy, belong to the biomedicine technical field.The drug composition is carimab and apatinib.The application finds that carimab is combined with apatinib as maintenance treatment, shows encouraging efficacy and acceptable safety in ES-SCLC patient who is not in progress after first-line chemotherapy, the median overall survival (OS) is 25.00 months, and the 12-month OS rate is 71.4%.This strategy of simultaneously targeting PD-1 and VEGFR2 provides a novel and reasonable solution for extending the disease control period in malignant tumors with limited treatment options after induction therapy, not only solves the key needs of ES-SCLC patients for more effective maintenance treatment, but also provides important insights into the biological principles of anti-angiogenic therapy combined with immunotherapy.

The invention provides a hydrogenation reduction preparation process of an apatinib intermediate, and relates to the technical field of pharmaceutical chemicals. According to the preparation process of the apatinib intermediate, 1-(4-nitrophenyl) cyclopentane-1-formonitrile and H2 are subjected to a hydrogenation catalytic reaction to prepare 1-(4-aminophenyl) cyclopentane formonitrile, and a used catalyst is a triphenylphosphine sulfide / raney nickel complex. The 1-(4-aminophenyl) cyclopentane formonitrile is prepared by efficiently and highly selectively catalyzing the hydrogenation of 1-(4-nitrophenyl) cyclopentane-1-formonitrile by taking a complex obtained by carrying out coordination complexation on triphenylphosphine sulfide and Raney nickel as a catalyst, and the reaction yield is high, the content of a byproduct is low, and the reaction conditions are mild. Meanwhile, the metal coordination catalyst reduces the consumption of nickel metal, greatly simplifies the process, saves the production cost, and has important industrial application value; the catalyst can be cyclically applied in a high-activity manner, and the catalyst does not need to be supplemented in the cyclically applied process.

Provided is a use of an anti-PD-1 antibody and apatinib in the preparation of a drug for treating acral melanoma, the regimen has a disease control rate of 72.2% for acral melanoma and an objective disease remission rate of 22.2%. Also provided is a use of an anti-PD-1 antibody, apatinib and temozolomide in the preparation of a drug for treating melanoma.