40 results about "Cytarabine" patented technology

Provided is a combination therapy for an antitumor agent that exhibits a high antitumor effect using a pyridone carboxylic acid derivative.　An antitumor agent characterized by being administered in combination with other antitumor agents, and comprising, as an active ingredient, a compound represented by the formula (1) (in the formula, the wavy line represents the steric configuration being the R configuration or the S configuration) or a salt thereof, wherein the other antitumor agents are one or more types selected from cytarabine, venetoclax, azacitidine, gilteritinib, birabresib, vorinostat, GSK126, MK-8776, AZD7762, rabusertib, dabrafenib, vemurafenib, olaparib, adavosertib, alisertib, decitabine, midostaurin, and AZD5991.

The invention provides an application of a traditional Chinese medicine monomer rhamnatin or a solvate, hydrate or salt thereof in preparation of a medicine for treating or relieving leukemia. The antitumor activity of rhamnatin is discussed from multiple aspects such as in-vitro and in-vivo levels. Experiments show that the traditional Chinese medicine monomer rhamnatin can inhibit proliferation of leukemia cell strains, induce cell apoptosis and enhance the leukemia inhibition effect of cytarabine; in vivo, rhamnatin can inhibit the growth of leukemia subcutaneous transplantation tumors and prolong the lifetime of tumor-bearing mice. Further experiments reveal that rhamnatin realizes a biological mechanism of inhibiting leukemia proliferation and promoting apoptosis by regulating a PI3K-AKT signal channel, and shows that rhamnatin has a certain prospect in treatment of leukemia.

The invention belongs to the field of medicine, and discloses application of lactobacillus paracasei in preparation of medicine for repairing intestinal barrier function and treating AML (acute myeloid leukemia). Generally, gastrointestinal mucosal barriers, immune systems and nutrient absorption of AML patients receiving induced chemotherapy are severely damaged, and the factors severely destroy intestinal microbial balance, so that the progress of the disease course is promoted, and the occurrence rate of complications is increased. The invention finds that the lactobacillus paracasei has a remarkable effect in preparing the medicine for repairing the intestinal barrier function and treating AML (acute myeloid leukemia), and particularly, the lactobacillus paracasei can repair the intestinal barrier function and enhance the curative effect of cytarabine.

The invention discloses a combined pharmaceutical composition for preventing, relieving or treating acute myelogenous leukemia and application, and relates to the technical field of biomedicine. The invention provides a combined pharmaceutical composition for preventing, relieving or treating acute myelogenous leukemia. The combined pharmaceutical composition comprises vincristine and cytarabine or pharmaceutically acceptable salts and solvates of the vincristine and the cytarabine. According to the vincristine and cytarabine combined pharmaceutical composition, the apoptosis level of acute myelogenous leukemia cells can be remarkably improved, and compared with single-drug treatment, the vincristine and cytarabine combined pharmaceutical composition has higher anti-tumor efficacy; vincristine interferes or blocks a cell senescence state induced by cytarabine through a microtubule destruction effect, so that the problem of drug insensitivity caused by cell senescence is solved, and drug resistance caused by cell senescence is effectively reversed.

The present invention provides an application of cytarabine combined with an immune checkpoint inhibitor in the treatment of glioma. Experiments have proved that cytarabine combined with an immune checkpoint inhibitor has a synergistic effect in the treatment of glioma. Cytarabine combined with an immune checkpoint inhibitor can enhance the anti-tumor effect of cytarabine and significantly prolong the survival of mice, providing a new strategy for the treatment of glioma.

Provided are methods for treating hematologic malignancy, especially AML-MRC, MDS and / or MM. Specifically, provided are methods for treating AML-MRC and MDS with a compound of formula (I) or a pharmaceutically acceptable salt thereof, optionally in combination with at least one additional anti-cancer agent such as 5-azacitidine or cytarabine, and treating MM with a compound of formula (I) or a pharmaceutically acceptable salt thereof, optionally in combination with at least one additional anti-cancer agent such as pomalidomide, thalidomide, lenalidomide, and / or dexamethasone.

Chemotherapy resistance is the major therapeutic barrier in acute myeloid leukemia (AML). To address this issue, the inventors generated a syngeneic mouse model of AML, which we evolved to develop resistance to a front-line chemotherapy regimen. The inventors identified SRRM1 as a critical vulnerability of chemoresistant leukemic cells and identified that PAK1 and CLK kinases are regulators of SRRM1 in chemoresistant AML cells. Human and murine chemoresistant cells were found to be markedly more sensitive to inhibitors of PAKs (FRAX597) and CLKs (TG003 and ML 167) compared to their naive counterparts, an effect which was even further enhanced by treatment with cytarabine and daunorubicin. Simultaneous suppression of Clk1 and Pak1 or Clk-4 and Pak1 using validated shRNAs and combinations of FRAX597 and TG003, or FRAX597 and ML 167 synergized to reduce the growth and the colony-forming capacity of chemoresistant AML cells and sensitized them to chemotherapy. The combined treatment improved overall mouse survival and reduced disease burden in the chemoresistant AML mouse models. Moreover, AML patient cells that were primarily refractory or from a post chemotherapy relapse (n=21 ) exhibited a higher ex vivo sensitivity to the FRAX597 + TG003 combination in comparison with chemosensitive patients at diagnosis (n=28). Finally, combined PAK1 and CLK inhibition more effectively reduced disease progression in animals transplanted with the relapse sample than in those engrafted with the sample taken at diagnosis. Thus, the present invention relates to combination of PAK1 inhibitors and CLK inhibitors for preventing resistance to chemotherapy in patients suffering from acute myeloid leukemia.

Compounds of the formula Iwherein X is a bond or —CH2, and pharmaceutically acceptable salts thereof are useful in the parenteral treatment of leukemia, myelodysplastic syndrome or lymphoma, especially in patients presenting with cytarabine resistance and / or over 60 years of age.

The invention discloses a cytarabine syndrome risk prediction model, a training method thereof and a system adopting the same. The model training method comprises the following steps: constructing an artificial intelligence model; wherein the input of the artificial intelligence model comprises the weight and the heating duration of the to-be-evaluated object; the output of the artificial intelligence model is the risk probability that the to-be-evaluated object belongs to the cytarabine syndrome fever; large sample data are adopted to train the artificial intelligence model, cases with fever of the cytarabine syndrome are positive samples, and other fever cases are negative samples. According to the present invention, the identification standard of the cytarabine syndrome fever and the infected fever is established, and the risk probability of the cytarabine syndrome of the object to be evaluated can be evaluated by analyzing the difference of the two detection results in the laboratory, such that the unreasonable use of the antibacterial agent is reduced, the medical cost is reduced, and the drug resistance risk of the antibacterial agent is reduced.

The present invention relates to the use of cytarabine, a mitochondrial metabolism inhibitor and an agent that downregulates the expression or activity of CDA in the treatment of cancer.

The application relates to a pharmaceutical cocrystal of cytarabine and 5-fluorouracil and a preparation method thereof, and relates to the technical field of pharmaceutical cocrystals. The pharmaceutical cocrystal is composed of one cytarabine molecule and one 5-fluorouracil molecule as a basic structural unit, and has a chemical formula of [C9H 13 N3O5.C4H3N2O2F]; the pharmaceutical cocrystal belongs to an orthorhombic system and has a space group of P212121. The pharmaceutical cocrystal prepared by a solvent evaporation method and a cooling method improves the permeability of cytarabine, appropriately reduces the solubility of cytarabine, and significantly improves the antitumor activity of cytarabine; through the complementary advantages of the properties and the pharmacodynamic effects of two components, the synergistic antitumor effects of cytarabine and 5-fluorouracil are realized, and a new idea is provided for developing synergistic antitumor pharmaceutical cocrystals. The pharmaceutical cocrystal can keep the skeleton structure of the crystal unchanged after long-term placement at room temperature, the preparation method is simple and easy to implement, the cost is low, and the pharmaceutical cocrystal is convenient for large-scale production.

The invention relates to application of mitoxantrone liposome in preparation of a medicine for treating acute myelogenous leukemia (AML) in combination with cytarabine, or in further combination with other medicines, such as homoharringtonine or vinca. A method of treating AML, the method comprising administering to a patient with AML a pharmaceutical composition comprising a liposome of mitoxantrone and cytarabine, the pharmaceutical composition may further comprise homoharringtonine or vinca.

The invention belongs to the technical field of cytarabine, and particularly relates to a preparation method of cytarabine. Cytidine reacts in the presence of a condensation reagent and alkali to form cyclo-cytidine, cyclo-cytidine reacts with chloroacetic acid acyl chloride to form a compound C, and the compound C reacts in the presence of ammonia water to form cytarabine or a pharmaceutically acceptable salt thereof. According to the method, a high-toxicity dehydrating agent and complex synthesis steps are not used, and a high-purity cytarabine finished product can be directly obtained.

The invention belongs to the technical field of veterinary drugs, and particularly relates to novel application of monomeric compounds, in particular to application of nucleotide analogues in preparation of drugs for preventing and / or treating diseases caused by bovine nodular skin disease viruses. Iodine glycoside, non-auridine, cytarabine and vidarabine are all monomeric compounds and belong to nucleotide analogues. It is found for the first time that iodoglycoside, non-aurine glycoside, cytarabine and vidarabine can inhibit bovine nodular skin disease virus replication in a safe concentration range in a dose-dependent mode. The iodoglycoside, the non-aurine glycoside, the cytarabine and the vidarabine have low cytotoxicity, can efficiently inhibit the bovine nodular dermatosis virus, and have a good application prospect in the aspect of preventing or treating the bovine nodular dermatosis.

The invention provides an oral administration composition combining a cytarabine amino-acid ester medicine and chidaridine, and belongs to the field of medicines. The invention provides a cytarabine amino-acid ester composition. The cytarabine amino-acid ester composition comprises cytarabine amino-acid ester or salt of the cytarabine amino-acid ester and chidaridine. In one aspect, the pharmaceutical composition of the present invention relates to a method for increasing the oral bioavailability of cytarabine by increasing the permeability of the small intestine. The compound has a more excellent effect of inhibiting the activity of cytidine deaminase, and the metabolism of cytarabine is reduced. The specific proportion effect of the pharmaceutical composition disclosed by the invention is superior to the effect of the combination of the non-cytarabine amino-acid ester prodrug and the chidaridine.

The application provides an application of a TRIM44 expression inhibitor in preparation of a cytarabine-resistant leukemia drug, and belongs to the technical field of bioengineering.The application provides the application of the TRIM44 expression inhibitor in preparation of the cytarabine-resistant leukemia drug.In the application, a key gene TRIM44 affecting AML drug resistance is identified by analyzing a single cell transcriptome data set, the expression of the TRIM44 can be lowered by using sinomenine, the function of regulatory T cells (T-reg cells) is inhibited, the sensitivity of AML cells to a chemotherapy drug is enhanced, a good synergistic treatment effect with cytarabine is shown, the cytarabine resistance of leukemia is reversed, and a new target site and a molecular marker are provided for predicting and improving the treatment effect of patients in clinic.

Novel cytotoxic fluoropyrimidine polymers for treating cancer (e.g., colorectal cancer (CRC)) in a subject (e.g., a subject having cancer) are nucleic acid molecules including 5-fluoro-2′deoxyuridine monophosphate (FdUMP)[10] having a polyethylene glycol (PEG) spacer appended to the 5′ terminus and a cytarabine (AraC) nucleotide appended to 3′termius. These novel cytotoxic fluoropyrimidine polymers may be used in compositions, kits and methods for treating advanced and high-risk cancers, including CRC.

The invention relates to compositions and methods for treating patients with hematological proliferative disorders who are ineligible for treatment with standard intensive chemotherapy, using low intensity treatment with CPX-351, a liposomal composition of daunorubicin and cytarabine.

This invention belongs to the field of biopharmaceuticals and specifically discloses the preparation and application of a compound formulation of Hedyotis diffusa (5-30 parts), Scutellaria barbata (3-10 parts), Houttuynia cordata (3-6 parts), Ganoderma lucidum (2-4 parts), and astaxanthin for adjuvant tumor treatment. This compound is prepared by gradient decoction, nanoemulsification, and synergistic combination of ingredients, including Hedyotis diffusa (5-30 parts), Scutellaria barbata (3-10 parts), Houttuynia cordata (3-6 parts), Ganoderma lucidum (2-4 parts), and astaxanthin (0.5-1 parts). The combination of gradient temperature-controlled decoction and nanoemulsification (particle size 50-200 nm) significantly improves the bioavailability of heat-sensitive components (such as astaxanthin), allowing for the design of various dosage forms (tablets, capsules, and pills) to meet diverse clinical needs. Animal models have demonstrated that this compound enhances the efficacy of cytarabine and cisplatin while reducing chemotherapy toxicity (resumption of ALT / AST levels to normal). This invention combines multi-target anti-tumor and immunomodulatory properties with dosage form stability, providing an innovative solution for adjuvant tumor treatment.

This invention relates to the use of cytarabine, mitochondrial metabolism inhibitors, and agents that downregulate the expression or activity of CDA in the treatment of cancer.

The invention discloses an application of curcumin in improving puberty male reproductive capacity damage caused by chemotherapeutic drugs. Aiming at the problems of testicular germ cell quantity reduction, oxidative stress injury, long-term fertility damage and the like caused by cytosine arabinoside chemotherapy, curcumin is applied while or before the cytosine arabinoside is applied. The application is realized through combined administration or a pharmaceutical composition containing curcumin and cytarabine. Experiments show that the scheme can effectively relieve testicular tissue form damage, reduce germ cell apoptosis and antagonize oxidative stress, and significantly improve the sperm quality of adult individuals. The invention provides a new potential strategy for synchronously protecting the reproductive function of a clinical child tumor patient during chemotherapy.

The invention relates to compositions and methods for treating patients with hematological proliferative disorders who are ineligible for treatment with standard intensive chemotherapy, using low intensity treatment with CPX-351, a liposomal composition of daunorubicin and cytarabine.

The utility model relates to dissolving equipment for cytarabine and daunorubicin compound lipidosome, which belongs to the technical field of medicine processing equipment and comprises a base, a connecting frame is mounted at the top of the base, a dissolving bin is mounted on one side, close to the center of the base, of the connecting frame, and a leakage bin is fixedly connected to the bottom of the dissolving bin. A dissolving tank is mounted in the dissolving bin, and a heater is mounted on the inner wall of the dissolving bin; a stirring mechanism for increasing the dissolving speed is mounted in the dissolving tank. The lipid dissolving device has the beneficial effects that through the arrangement of the stirring mechanism, the arc-shaped stirring paddle can be driven to rotate through the rotating motor and the rotating shaft, and lipid in the dissolving tank is stirred through the arc-shaped stirring paddle, so that the dissolving speed is increased, and meanwhile, one side of the arc-shaped stirring paddle is attached to the inner wall of the dissolving tank, so that the lipid dissolving effect is improved. The leakage holes can be prevented from being blocked by lipid, and it is ensured that dissolved liquid is smoothly discharged out of the dissolving tank.

The invention discloses a tumor composite vaccine for treating tumors by combining PD-1 with pyrimidine antimetabolic drugs and a preparation method of the tumor composite vaccine, and belongs to the technical field of biological medicines. The preparation method comprises the following steps: mixing and dissolving soybean lecithin, DSPE-PEG2000, cholesterol, alphaPD-1, an inactivated bacterial liquid and a solvent, and performing reduced pressure evaporation to obtain a mixed solution containing a film; mixing the mixed solution containing the thin film with a pyrimidine anti-metabolism drug, and sequentially performing ultrasonic treatment and extrusion to obtain a pretreatment solution; after the pretreatment liquid is subjected to dialysis treatment, deionized water is added to fix the volume to 10 mL, then a freeze-drying protective additive is added for mixing, and the tumor composite vaccine is obtained through freeze-drying. According to the invention, inactivated bacterial liquid, pyrimidine antimetabolic drug cytarabine for inhibiting cell synthesis and alphaPD-1 for relieving immunosuppressive effect and activating T cell function are mixed and freeze-dried, so that the tumor composite vaccine with good anti-tumor effect is obtained.

The utility model relates to an emulsifying and mixing device for cytarabine and daunorubicin compound lipidosome, which belongs to the technical field of mixing devices and comprises a support frame, a support plate is fixedly connected to the inner wall of the support frame, a mixing tank is fixedly connected to the inside of the support plate, a sealing cover is connected to the upper end face of the mixing tank in an attached manner, and the sealing cover is fixedly connected to the upper end face of the mixing tank. A driving shaft is rotationally connected to the center of the interior of the sealing cover, and a stirring rod is fixedly connected to the outer wall of the driving shaft. The cytarabine and daunorubicin mixing tank has the beneficial effects that the turning plate rotates in the vertical direction at the bottom of the mixing tank, so that the material accumulation at the bottom of the mixing tank can be broken, the deposition and layering of the material at the bottom are effectively prevented, the uniform distribution of cytarabine and daunorubicin in the mixing process is ensured, and the mixing effect and the product quality are improved; and the material at the bottom can be turned upwards to be fully mixed with the material at the upper layer, so that the mixing process is accelerated, the mixing is more uniform, and the mixing efficiency is improved.

The invention provides application of the cytarabine combined immune checkpoint inhibitor in glioma treatment, experiments prove that the cytarabine combined immune checkpoint inhibitor has a synergistic effect on glioma treatment, and the anti-tumor effect of the cytarabine can be enhanced by the cytarabine combined immune checkpoint inhibitor; the lifetime of the mouse is obviously prolonged, and a new strategy is provided for treating glioma.

The present invention provides the use of a traditional Chinese medicine monomer, rhamnosine, or a solvate, hydrate, or salt thereof, in the preparation of a drug for treating or alleviating leukemia. The present invention explores the anti-tumor activity of rhamnosine from multiple levels, including in vitro and in vivo levels. Experiments have shown that the traditional Chinese medicine monomer, rhamnosine, can inhibit the proliferation of leukemia cell lines, induce cell apoptosis, and enhance the effect of cytarabine in inhibiting leukemia; in vivo, rhamnosine can inhibit the growth of leukemia subcutaneous transplanted tumors and prolong the survival of tumor-bearing mice. Further experiments revealed the biological mechanism by which rhamnosine inhibits leukemia proliferation and promotes apoptosis by regulating the PI3K‑AKT signaling pathway, indicating that it has certain prospects in the treatment of leukemia.

The invention discloses application of brutinib and a combined pharmaceutical composition thereof in treatment of leukemia, and the leukemia comprises acute myelogenous leukemia, chronic myelogenous leukemia, T acute lymphoblastic leukemia and B acute lymphoblastic leukemia. The invention creatively finds that the brutinib has a remarkable synergistic effect on treatment of the leukemia when being combined with the vinca, the cytarabine or the daunorubicin for use, and a brand new drug combination scheme provided by the invention provides a more effective drug combination choice for treatment of the leukemia, and is expected to improve the treatment effect of patients with the leukemia.

The invention belongs to the field of medicines, and discloses application of an LMP1 expression inhibitor in regulation and control of MCM3 protein. The inventor finds that the LMP1 protein is related to drug resistance of NKTCL cells to drugs synthesized by targeted DNA through research. The LMP1 interacts with a key protein MCM3 synthesized by DNA of a host, other signal channels, related to cell cycle regulation and DNA repair, of the host are influenced through the LMP1-MCM3 type, and overexpression of the LMP1 promotes survival of tumor cells and inhibits cell apoptosis, so that the effect of a chemotherapeutic drug is reduced; knockdown of the LMP1 can significantly enhance the sensitivity of cells to drugs. The function of MCM3 can be reduced by inhibiting the expression or function of LMP1. The interaction between EBV and host cells can be broken, and the curative effect of chemotherapeutic drugs such as cytarabine which are widely used clinically is improved. In addition, the strategy can also be used for preventing reactivation of EBV and reducing the occurrence risk of virus-related tumors.