51 results about "Temozolomid" patented technology

The invention relates to an injectable parenteral medicinal preparation of temozolomide and a preparation method thereof. The medicinal preparation comprises (1) temozolomide or pharmaceutically acceptable salt thereof, (2) at least one stabilizer, and (3) at least one aqueous diluent, wherein the stabilizer is selected from L-alanine, L-glycine, L-cysteine, L-cysteine hydrochloride anhydride, L-cysteine hydrochloride monohydrate, acetyl cysteine, S-carboxymethyl-L-cysteine, L-ethyl cysteine hydrochloride, L-methyl cysteine hydrochloride, vitamin C or a mixture thereof. The invention further relates to lyophilized power containing the medicinal preparation and products thereof.

Provided herein are compounds and methods for the treatment of brain cancer in a mammal, wherein the method comprises the administration to the mammal a compound that stabilizes tubulin dimers or microtubles at G2-M interface during mitosis but is not a substrate for MDR protein. In particular, the present application relates to the use of an orally effective abeo-taxane, alone or in combination with temozolomide or bevacizumab, for the treatment of brain cancer.

The present invention relates to combination therapy for cancer with a WT1 peptide vaccine and temozolomide.

The use of dianhydrogalactitol provides a novel therapeutic modality for the treatment of non-small-cell lung carcinoma (NSCLC) and ovarian cancer, as well as other types of malignancy, including brain metastases of NSCLC. Dianhydrogalactitol acts as an alkylating agent on DNA that creates N7 methylation. Dianhydrogalactitol is effective in suppressing the growth of cancer stem cells and is activeagainst tumors that are refractory to temozolomide, cisplatin, and tyrosine kinase inhibitors; the drug acts independently of the MGMT repair mechanism. Dianhydrogalactitol can be used together withother anti-neoplastic agents and can possess additive or super-additive effects.

The invention discloses a drug-tolerant glioblastoma cell line of primary temozolomide and bevacizumab, a construction method and application of the cell line. The construction method comprises the following steps: obtaining tissue specimens of patients with drug-resistant glioblastoma cell of primary temozolomide and bevacizumab through clinical screening, primarily culturing tumor cells through an enzyme digestion method, and continuously extending generation to 50 generations to obtain a strain of drug-tolerant glioblastoma cell line of primary temozolomide and bevacizumab; the microbial preservation number of the drug-tolerant glioblastoma cell line of primary temozolomide and bevacizumab is CGMCC No.8205. The glioblastoma cell line, disclosed by the invention, is stable in characteristics, stably heritable and high in tolerance to temozolomide and bevacizumab; the cell generation cycle lasts about 48 hours; the glioblastoma cell line has strong invasiveness and tumorigenicity. The glioblastoma cell line constructed by the construction method has important application prospect in aspects of screening medicines for treating glioblastoma and researching nosogenesis of the glioblastoma, and the like.

The invention belongs to the technical field of biomedicine, and particularly relates to a glioma malignant progress and survival prognosis detection molecular marker, a temozolomide drug resistance detection target and application. An m6A methylation reader HNRNPC which is highly expressed in glioma tissue and closely related to the tumor occurrence and development process is screened out by a bioinformatics method, further analysis finds that the expression level of the m6A methylation reader HNRNPC is closely related to the survival rate and prognosis of patients, and through clinical masstumor tissue sample verification, the m6A methylation reader HNRNPC can be used as a molecular marker and an independent survival prognosis factor for glioma malignant progress. Meanwhile, it is foundthat knockout of the HNRNPC can increase medicine sensitivity of glioma cells to temozolomide. A new diagnosis, treatment and prognosis predicting target is provided for glioma treatment, and a new molecular target can be provided for improving temozolomide drug resistance.

The invention discloses an application of IncRNA LNC_004208 and detection reagent thereof in preparing a glioma prognosis reagent. Through research on and utilization of IncRNA sequencing, the invention finds that IncRNA LNC_004208 has ultrahigh expression in a temozolomide-resisted glioma cell line; through telephone follow-up for 104 glioma patients, detailed inquiry for their first onset time,level, treatment condition, relapse situation, other diseases, other drugs, relapse time, death time, and the like, and registration for survival time and state, a result shows that average survival time and progression free survival of high expression patients are obviously shorter than those of low expression or no expression patients and are related to reactivity of temozolomide; thus, LNC_004208 is a molecular marker related to glioma prognosis; IncRNA LNC_004208 is high in expression; prognosis of patients is poor.

The invention discloses a compound or a pharmaceutically acceptable salt thereof. The compound includes a moiety derived from temozolomide and a moiety derived from elemene, and the moiety derived from temozolomide and the moiety derived from elemene are directly covalently linked or covalently linked via a linker. The invention also discloses a composition comprising the above compound, and a method of treating cancers.

The invention discloses a temozolomide magnetic temperature-sensitive liposome and relates to the field of nanomedicine. Firstly, a solid precursor liposome is prepared from a small molecular drug temozolomide (TMZ) and a liposome with a phase transition temperature, and then hydration is carried out by using an ultra-small ferroferric oxide magnetic nanoparticle (Fe3O4 MNPs) suspension to form atemozolomide magnetic temperature-sensitive liposome (TMZ / Fe-TSL). The drug delivery mode of the form combines magnetofluid thermal therapy, chemotherapy and temperature-controlled drug release, so that the plasma half-life period of the temozolomide is prolonged, the curative effect of the temozolomide is enhanced, and the drug toxicity can be reduced. A temozolomide magnetic temperature-sensitive liposome drug delivery system disclosed by the invention provides a wide transformation and application prospect for magnetofluid thermal therapy combined with chemotherapy, and also provides a newscheme for treatment and research of brain glioma.

The invention relates to applications of temozolomide or a pharmaceutical composition containing the temozolomide in preparation of medicines for treating cervical cancer, colorectal cancer, and other diseases. The composition comprises the temozolomide and a pharmaceutically acceptable carrier thereof. The preparation formula is a suppository preferably. The invention also relates to a formula of the suppository and a preparing method of the suppository.

The invention relates to an interference plasmid for knocking down expression of COPS5 protein in a glioblastoma cell line, application of the interference plasmid as a drug for solving the drug resistance problem of temozolomide in treatment, and application of a combined drug formed by the interference plasmid for knocking down expression of the COPS5 protein and temozolomide as a glioblastoma chemotherapeutics. The interference plasmids knock down expression of COPS5 protein and regulate the ferroptosis process of glioblastoma cells, specifically, the expression of ferroptosis promoting protein is increased, and the expression of ferroptosis inhibiting protein is reduced.

The invention discloses a combined medication mode for synergistically treating human brain glioma, and belongs to the technical field of pharmacology. Through the combined use of two tumor cell inhibiting drugs, i.e. Perphenazine and temozolomide are combined to treat human brain glioma cells, a model is established to quantify a combined effect. By selecting different concentrations of a stem cell inhibitor perphenazine and a human brain glioma chemotherapeutic drug temozolomide, the proliferation of U87 cells and U251 cells is inhibited by combined administration, the combination index (CI) value obtained by model quantification after the two drugs are combined for use reaches 0.3299 + / -0.002, and a strong synergistic effect is achieved; through colony formation experiment detection, the cell clone formation rate of a drug combination group is obviously lower than that of a control group and a single drug administration group, and a novel and creative drug administration mode can provide a novel drug administration strategy for treating human brain glioma.

Temozolomide nano-prodrug micelles comprise a hydrophilic shell and a hydrophobic core, the hydrophilic shell is polyoxazoline or polyethylene glycol, and the hydrophobic core is polytemozolomide. Its preparation method is: react polyoxazoline or polyethylene glycol with 4-cyano-4-pentanoic acid through esterification, and use the obtained product as a macromolecular RAFT reagent under the catalysis of azobisisobutyronitrile to react with Temozolomide-methyl methacrylate reacts to obtain an amphiphilic block polymer. The amphiphilic block polymer of the present invention can prolong the half-life of temozolomide. The two kinds of amphiphilic block polymer nanomicelles belong to the drug prodrug of temozolomide. At the same time, the micelle core can carry other anticancer drugs to achieve different Combination therapy of drugs. After the polyoxazoline-polytemozolomide micelles enter the tumor cells, they are cleaved in the acidic environment of the cancer cells, and the encapsulated drugs are quickly released, thereby producing a highly effective therapeutic effect, which solves the problem of slow release of the drug carrier drug and easy to produce anti-inflammatory effects. Medicinal issues.

The present invention is in the field of drug delivery, and specifically, cationic liposome-based drug delivery. In embodiments, this invention provides methods of making ligand-targeted (e.g., antibody- or antibody fragment-targeted) liposomes useful for the delivery of liposomes to tumors, including brain tumors. In embodiments, the liposomes deliver temozolomide across the blood-brain barrier for treatment of primary or metastatic brain tumors. Additional cancers that can be treated with the liposomes include neuroendocrine tumors, melanoma, prostate, head and neck, ovarian, lung, liver, kidney, breast, urogenital, gastric, colorectal, cervical, vaginal, angiosarcoma, liposarcoma, rhabdomyosarcoma, choriocarcinoma, pancreatic, retinoblastoma and other types of cancer. In another embodiment the liposomes deliver melphalan for the treatment of multiple myeloma, other tumors of the blood or other solid tumors. In still other embodiments the liposomes can deliver other drugs such as pemetrexed or irinotecan for treatment of cancer or drugs including atropine for treatment of organophosphate poisoning.

The invention discloses application of tubeimoside combined with temozolomide in preparation of a medicine for treating or inhibiting glioblastoma. Under the condition that the temozolomide is adopted to treat glioblastoma, the glioblastoma with temozolomide resistance can be generated, the sensitivity of the glioblastoma with temozolomide resistance to temozolomide can be enhanced by combining tubeimoside with temozolomide for treatment, so that the drug resistance of the glioblastoma to temozolomide is weakened; and the compound has small adverse reaction on non-tumor cells, and has great value in preparation of drugs for treating or inhibiting glioblastoma.

Disclosed is a use of E2F6 as a target capable of increasing the sensitivity of temozolomide. Temozolomide is used for treating glioblastoma. E2F6 inhibitor and temozolomide treatment can increase the curability of glioblastoma. The invention provides scientific evidence for the pathogenesis and clinical treatment of glioblastoma from the clinical patient sample level, cell function level and molecular level.

The new use of gemfibrozil relates to the field of glioma treatment. Application of the gemfibrozil of the present invention in improving the therapeutic effect of temozolomide on glioma. The application of the gemfibrozil of the present invention in enhancing the killing effect of temozolomide on glioma cells. A pharmaceutical composition for preventing and / or treating glioma of the present invention, the pharmaceutical composition contains gemfibrozil and temozolomide. It has been proved by experiments that gemfibrozil can improve the therapeutic effect of temozolomide on glioma, has synergistic effect of temozolomide on killing glioma cells, and can enhance the killing effect of temozolomide on glioma cells. The preparation of gemfibrozil and temozolomide into a drug for preventing and / or treating glioma can improve the therapeutic effect of temozolomide on glioma. The application of gemfibrozil in the preparation of drugs for the prevention and / or treatment of glioma opens up a new application of gemfibrozil, and provides a new therapy and treatment plan for the treatment of the chronic disease of glioma.

The present invention relates to temozolomide resistant glioblastoma cells lines. Further, the present invention relates to a method for identifying, screening and characterizing temozolomide resistant cells derived from glioblastoma cells lines in patients diagnosed with glioblastoma and undergoing treatment with temozolomide and / or in patients on the part to recovery to avoid or treat relapse. The issue of temozolomide resistance at the level of diagnosis and treatment of glioblastoma is undertaken by the present invention to be solved by the present invention.

The invention belongs to the field of medicine, and particularly relates to application of a drug combination of vitamin K1 and temozolomide in preparation of a medicine for treating bile duct cancer. The application of the drug combination of the vitamin K1 and the temozolomide in preparation of the medicine for treating the cholangiocarcinoma is provided for the first time, the vitamin K1 and the temozolomide have an obvious synergistic effect, so curative effect is effectively improved; the curative effect of the drug combination is more obvious compared with a single component, and killing performance on tumor cells is improved; dosage is effectively reduced, so toxic and side effects are reduced; and the drug combination can save cost, relieve the economic burden of patients, provide a new way for the prevention and treatment of bile duct cancer, and have wide application prospects in the field of medicine and pharmacology.

The invention relates to an auxiliary pharmaceutical composition for chemoradiotherapy of newly-diagnosed glioblastoma, which is used for postoperative synchronous chemoradiotherapy of the newly-diagnosed glioblastoma, is taken during chemotherapy, and comprises a combination of two independent reagents, namely temozolomide and apatinib mesylate. by using the auxiliary pharmaceutical composition, the treatment effect of newly diagnosed glioblastoma is improved, and a new strategy and thought are provided for treatment of glioma.

The present invention provides, inter alia, methods for treating or ameliorating the effects of a cancer in a subject, e.g., glioblastoma (GBM) in a subject that is resistant to temozolomide (TMZ), methods for delaying the emergence of TMZ resistance and / or increasing the TMZ sensitivity in a subject, and methods for reducing tumor aggressiveness in a subject. Also provided are pharmaceutical compositions and kits to implement such methods.

Provided herein are compounds and methods for the treatment of brain cancer in a mammal, wherein the method comprises the administration to the mammal a compound that stabilizes tubulin dimers or microtubles at G2-M interface during mitosis but is not a substrate for MDR protein. In particular, the present application relates to the use of an orally effective abeo-taxane, alone or in combination with temozolomide or bevacizumab, for the treatment of brain cancer.