37 results about "Chemosensitizer" patented technology

This invention generally relates to use of 8-fluoro-2{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indol-6-one represented by formula 1 as a chemosensitizer that enhances the efficacy of cytotoxic drugs or radiotherapy.

This invention provides pharmaceutical combinations of 8-fluoro-2{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indol-6-one, or a pharmaceutically acceptable salt thereof and at least one additional therapeutic agent, kits containing such combinations and methods of using such combinations to treat subjects suffering from diseases such as cancer.

The invention discloses an adriamycin nano drug delivery system as well as a preparation method and application thereof. The drug delivery system comprises the following components in percentage by weight: 0.02%-1.5% of active ingredient containing adriamycin, 1%-20% of solid lipid, 0.1%-20% of liquid lipid, 0.5%-20% of emulsifier and 0.1%-5% of isoosmotic adjusting agent, wherein the solid lipid and the liquid lipid form nanoparticles to cover the active ingredient containing the adriamycin. The preparation method comprises the following steps: (1), uniformly dispersing the active ingredient containing the adriamycin, the solid lipid, the liquid lipid and fat-soluble emulsifier in an organic solvent, evaporating the organic solvent to obtain an oil phase; (2), uniformly dispersing other emulsifiers and the isoosmotic adjusting agent in water to obtain a water phase; (3), adding the water phase into the oil phase for emulsifying drop by drop; (4), homogenizing under high pressure; (5), cooling and degerming. The adriamycin nano drug delivery system disclosed by the invention can be used for realizing co-transporting of the adriamycin and a chemosensitizer, so that the killability of the adriamycin on liver cancer cells is strengthened.

The invention relates to indole alkaloid formalardeemin shown in a chemical structural formula ((-)-5-N-formalardeemin), pharmaceutically acceptable salts of the same, and application of the indole alkaloid formalardeemin serving as an anti-tumor medicament in curing malignant tumors of human beings. The indole alkaloid formalardeemin serving as an anti-tumor medicament can not only inhibit the growth of malignant tumors directly, but also can be used as a chemosensitizer when used together with other anti-tumor medicaments such as doxorubicine, vincristine and the like to achieve the effect of effectively killing tumor cells by reversing the multi-drug resistance of the tumor cells. More significantly, compared with the indole alkaloid formalardeemin serving as a tumor cell growth inhibitor directly, the indole alkaloid formalardeemin serving as the chemosensitizer has a better effect, so the indole alkaloid formalardeemin has important clinical application prospect.

The present invention provides nucleobase oligomers and oligomer complexes that inhibit expression of an IAP polypeptide, and methods for using them to induce apoptosis in a cell. The nucleobase oligomers and oligomer complexes of the present invention may also be used to form pharmaceutical compositions. The invention also features methods for enhancing apoptosis in a cell by administering a nucleobase oligomer or oligomer complex of the invention in combination with a chemotherapeutic or chemosensitizing agent.

The invention discloses a preparation method and application of a polycarbonate drug-loaded nano chemosensitizer based on nitric oxide. The sensitizer is prepared by self-assembling a polycarbonate block copolymer containing a nitric oxide donor and a small molecule chemotherapeutic drug. The polycarbonate drug-loaded nano chemosensitizer based on nitric oxide has the advantages of good water solubility, small toxic and side effects, good stability in a normal physiological environment and the like, and effectively solves the problems of poor water solubility, large toxic and side effects and the like of indissolvable chemotherapeutic drugs such as adriamycin, mitoxantrone and the like in clinical use. The polycarbonate drug-loaded nano chemosensitizer based on nitric oxide also has the features that the drug-loading capacity is high, the tumor targeting property is remarkable, the tumor microenvironment can be regulated and controlled, the ideal chemotherapy sensitization effect is achieved, and tumor recurrence is reduced.

The present invention relates to novel TMPK inhibitor and their methods of use. In particular, it relates to novel TMPK inhibitor of Formula (I) and therapeutics that decrease the cellular dTTP level to suppress the growth and inhibit DNA repair in tumor cells and acts as a novel chemosensitizer, which are useful in methods for treating or preventing cancers.

This invention encompasses an expeditious method and compositions that have been found to show selective cytotoxicity against several different cancer cell lines. for treating a wide variety cancer neoplasms that have tumor microenvironments by administering a stand-alone anti-tumor chemotherapeutic composition or administered as an adjunct with chemotherapy and/or radiotherapy with enhanced tumor site affinity that preferentially elevates the pH at the tumor site to suppress and eliminates the acidic tumor microenvironment, administered as chemosensitizing and/or radiosensitizers enhancing the tumor, suppression, remission and inhibit tumor metastisis. The invention encompasses controlling mechanisms of intracellular and extracellular ionic physiology through the administration of alkali salts for pH modulating and for restoring and enhancing ionic physiology. The compositions are useful in effective treatment of cancers, particularly malignant melanomas and squamous cell carcinomas (SCCs), thereby inhibiting angiogenesis, reducing metastatic proliferation, supressing tumor generated induced acidotic pain.

A liposome including a lipid bilayer, an elastin-like polypeptide (ELP) conjugated to a hydrophobic moiety; a chemosensitizer; and an anticancer agent, a pharmaceutical composition including the same, and a method of delivering a chemosensitizer and an anticancer agent to a target site of a subject by using the liposome.

The invention discloses an application of cryptotanshinone in preparation of a chemosensitizer for acute lymphocytic leukemia, and application of combination of cryptotanshinone and anticancer drugs in preparation of drugs for treating and/or preventing acute lymphocytic leukemia, drug resistance reversal drugs and/or drugs for preventing relapse after pre-treatment. According to research discovery of the present invention, when cryptotanshinone and anticancer drugs are combined for use, cryptotanshinone and anticancer drugs are compounded to greatly increase the sensitivity of leukemia cellsto anticancer drugs, and the proliferation inhibition effect of multiple anticancer drugs on acute lymphocytic leukemia cells is improved in an explosive manner, so that the usage amount of each drugis far lower than that of the current clinical drug, and the explosive synergistic interaction effect is realized. Therefore, cryptotanshinone is used as an effective chemosensitizer for acute lymphocytic leukemia, and has important research significance and wide application prospect in the aspects of treating acute lymphocytic leukemia and solving the problem of drug resistance of acute lymphocytic leukemia.

The present invention provides a novel xanthone derivative compound or a pharmaceutically acceptable salt thereof. The compound is useful as a chemosensitizer that reduces anticancer drug resistance.

The invention relates to the field of medicines, and discloses novel application of gossypol. The gossypol can be used for effectively inhibiting the activity of NF-kappa B, AP-1 and HIF-1 alpha which are induced by reduction-oxidation of APE1 (apurinic/apyrimidinic endonuclease-1) and combined with DNA (deoxyribonucleic acid), and also remarkably inhibiting the DNA damage repairing function of APE1, so that the invention provides the application of gossypol in preparing an APE1 reduction-oxidation inhibitor or a DNA damage repairing function inhibitor of APE1. Furthermore, gossypol can be used for improving the sensitivity of tumor cells to etoposide chemotherapy, and can also reverse drug resistance of the tumor cells to chemotherapeutic medicines caused by high expression of APE1 in the tumor cells, so that the invention also provides application of gossypol in preparing adjuvants or chemosensitizer for treating cancers.

Methods of detecting novel therapeutically active compositions based on their ability to modulate the glycolipid metabolism and overcome multidrug resistance are described. These methods are particularly useful in screening for novel chemotherapeutic agents for the treatment of cancer, as well as chemosensitizers that are capable of enhancing the cytotoxicity of such chemotherapeutic agents. A combination of one or more of these compositions can be used in the treatment of a various cancers.

The invention belongs to the field of medicines, relates to application of solasodine in preparing an antitumor drug and particularly relates to application of solasodine in preparing a drug-resistant reversal agent of an antitumor drug. The solasodine is a natural product which has effect of reversing multidrug resistance of tumor cells, and can be used as a reversal agent for multidrug resistance of tumors. The solasodine further has effects of increasing sensitivity of tumor multidrug-resistant cells on the anti-tumor drug and can be used as a chemosensitizer. The invention further provides a method for inhibiting tumor multidrug-resistant cell multiplication by a pharmaceutical composition that combines the anti-tumor drug and solasodine. According to the invention, a small molecule compound solasodine can be used as a novel antitumor drug or an auxiliary ingredient thereof to be developed, and is obvious in tumor inhibiting effect, green and environment-friendly, so that a new way and means is provided for treating and curing tumors.

The invention belongs to the technical field of medicine preparation, and particularly relates to a new application of nobiletin and a nobiletin composition. The nobiletin is applied to preparation of drugs for reducing P-gp expression in synovial tissues of arthritis. Combined use of nobiletin and methotrexate can reduce cartilage and bone injuries and improve swelling and arthritis injury. On the other hand, nobiletin can reverse P-gp expression in patients with arthritis injury, thereby reducing outflow of the methotrexate and maintaining effect of the methotrexate. The nobiletin and the methotrexate have an obvious synergistic effect. The growth inhibition and apoptosis of RA-FLS/methotrexate cells can be recovered through the joint treatment of the nobiletin and the methotrexate at noncytotoxic concentration of nobiletin. The nobiletin can be used as a potential chemical sensitizer to overcome drug resistance in RA.

This invention includes a fluorophore-tagged antimalarial represented by the following structural formula (1) or a salt thereof. This invention relates to the synthesis of fluorophore-tagged antimalarials and describes the synthesis of a fluorophore-tagged antimalarial. These fluorophore-tagged antimalarials can be used to image live cells to determine the location of the antimalarial in the cell, identify drug resistance and growth related pathways in Plasmodium isolates, identify new drug targets and chemo-sensitizers to reverse drug resistance.

The present invention relates to a ubiquitin-specific peptidase 24 inhibitor, a medicinal composition including the same and a method of delaying or reversing multidrug resistance in cancers using the same. The USP24 inhibitor, which includes a shUSP24 RNA and/or a carbonyl substituted phenyl compound, can serve as a chemosensitizing agent for inhibiting the drug pump out, cancer sternness and genomic instability of cancer cells, thereby being applied to a medicinal composition and a method for delaying or reversing multidrug resistance in cancers.