156 results about "Carboplatin" patented technology

The present invention provides a medicinal composition having an excellent antitumor activity. That is, it provides a medicinal composition comprising a sulfonamide compound, a sulfonate compound or a salt of them, which is represented by the following formula: (wherein ring A represents an aromatic ring which may have a substituent group; ring B represents a 6-membered unsaturated hydrocarbon ring which may have a substituent group etc.; ring C represents a 5-membered hetero-ring containing one or two nitrogen atoms, and the ring C may have a substituent group; W represents a single bond or -CH=CH-; X represents -NH- etc.; and Y represents a carbon atom or a nitrogen atom; and Z represents -NH- etc.), particularly N-(3-chloro-1H-indol-7-yl)-4-sulfamoylbenzenesulfonamide or a salt thereof, combined with at least one substance selected from (1) irinotecan hydrochloride trihydrate; (2) mitomycin C; (3) 5-fluorouracil; (4) cisplatin; (5) gemcitabine hydrochloride; (6) doxorubicin; (7) taxol; (8) carboplatin; (9) oxaliplatin; (10) capecitabine; and (11) a salt of the above-mentioned (1) to (10).

The present invention provides methods and compositions for treating non-small-cell lung cancer (NSCLC) by administering a) a composition comprising nanoparticles that comprise paclitaxel and an albumin and b) a platinum-based agent (e.g., carboplatin). The present application also provides methods of treating prostate cancer by administering to the individual a) an effective amount of a composition comprising nanoparticles comprising docetaxel and an albumin; and b) an effective amount of a steroid.

The present invention provides methods and compositions for treating non-small-cell lung cancer (NSCLC) by administering a) a composition comprising nanoparticles that comprise paclitaxel and an albumin and b) a platinum-based agent (e.g., carboplatin). The present application also provides methods of treating prostate cancer by administering to the individual a) an effective amount of a composition comprising nanoparticles comprising docetaxel and an albumin; and b) an effective amount of a steroid.

The present invention provides phosphaplatins, stable isolated monomeric phosphate complexes of platinum (II) and (IV), and methods of use thereof for treating cancers, including cisplatin- and carboplatin-resistant cancers. Unlike cisplatin, these complexes do not readily undergo hydrolysis and are quite soluble and stable in aqueous solutions. Moreover, these complexes—unlike cisplatin, carboplatin, and related platinum-based anti-cancer agents—do not bind DNA. Rather, data suggests that phosphaplatins trigger overexpression of fas and fas-related transcription factors and some proapoptotic genes such as Bak and Bax. Nevertheless, the complexes exhibit tremendous cytotoxicity towards cancer cells. Thus, the present invention provides novel platinum anticancer agents that have a different molecular target than those in the art.

The present invention provides methods and compositions for treating non-small-cell lung cancer (NSCLC) by administering a) a composition comprising nanoparticles that comprise paclitaxel and an albumin and b) a platinum-based agent (e.g., carboplatin), wherein the individual has diabetes, has four or more metastatic sites, and / or is at least about 70 years old.

The invention relates to a nano micelle of a biodegradable macromolecular-bonding Pt(IV) anti-cancer medicament and a preparation method thereof. The structural formula of the anti-cancer medicament is defined in the specification, wherein the biodegradable macromolecule is tri-block copolymer, namely polyethylene glycol-b-polyester-b-polylysine; and tetravalency platinum coordination compound Pt(IV) is connected with a side amino on the block of polylysine on a macromolecular carrier through alpha, omega-polyethylene glycol. The carrier is non-toxic and is water-soluble, thus being convenient for reacting with the platinum(IV) coordination compound in water phase; a nano micelle form can be formed through self assembly; a platinum(IV) coordination compound is reduced to platinum(II), namely, cis-platinum, Carboplatin or Oxaliplatin, and the anti-cancer effect is known; the synthesis of the nano micelle is easy; the reduction potential of platinum(IV) is low, so that the platinum(IV) can be rapidly reduced to platinum(II) in cancer cells to take treatment effect; and the platinum(IV) is connected to the side chain of the macromolecule rather than the end of a chain, a macromolecular chain can be connected with multiple platinum(IV)s, and the content of platinum can be as high as 10-20%.

The invention discloses a medicinal composition for treating non-small cell lung cancer. The medicinal composition comprises a target medicament, a chemotherapeutic medicament and a traditional Chinese medicament, wherein the target medicament is one or more of bortezomib, imatinib, gefitinib and sunitinib; the chemotherapeutic medicament is one or more of 5-fluorouracil, carboplatin, epirubicin, adriamycin and fludarabine; and the traditional Chinese medicament is one or more of salvia miltiorrhiza, astragalus membranaceus, sappanwood, Chinese pulsatilla root and portulaca oleracea. The medicinal composition has a remarkable synergetic treatment effect when being used for treating the non-small cell lung cancer, and can be used for remarkably strengthening the cancer-inhibition effect compared with treatment of a single medicament, so that the medicament dosage can be reduced, and the toxic and side effects of chemotherapeutic medicaments can be reduced.

The present disclosure relates to the field of oncology, more particularly to the field of melanoma. Provided are methods of treating melanoma, particularly advanced cutaneous melanoma, with a combination of pharmaceutical agents comprising MDM4-specific antagonists (such as an inhibitor of the MDM4-p53 interaction or a molecule that decreases MDM4 protein stability) or MDM4-MDM2 dual inhibitors (i.e., molecules that disrupt the interactions between p53 and MDM2 and p53 and MDM4) and one or more chemotherapeutic agents such as for example alkylating agents (i.e., Dacarbazine (DITC) or melphalan), alkylating-like agents (i.e., cisplatin or carboplatin) or mitotic inhibitors (taxanes docetaxel or paclitaxel) and PI3K-AKT, B-RAF and MEK inhibitors. Further provided are pharmaceutical formulations of MDM4-specific antagonists (be it an inhibitor of the MDM4-p53 interaction or a molecule that decreases MDM4 protein stability) or MDM4-MDM2 dual inhibitors (i.e., molecules that disrupt the interactions between p53 and MDM2 and p53 and MDM4) and a pharmaceutical formulation of one or more chemotherapeutic agents such as for example alkylating agents (i.e., Dacarbazine (DITC) or melphalan), alkylating-like agents (i.e., cisplatin or carboplatin) or mitotic inhibitors (taxanes docetaxel or paclitaxel) and B-RAF and MEK inhibitors.

The present invention provides a medicinal composition having an excellent antitumor activity. That is, it provides a medicinal composition comprising a sulfonamide compound, a sulfonate compound or a salt of them, which is represented by the following formula: (wherein ring A represents an aromatic ring which may have a substituent group; ring B represents a 6-membered unsaturated hydrocarbon ring which may have a substituent group etc.; ring C represents a 5-membered hetero-ring containing one or two nitrogen atoms, and the ring C may have a substituent group; W represents a single bond or -CH=CH-; X represents -NH- etc.; and Y represents a carbon atom or a nitrogen atom; and Z represents -NH- etc.), particularly N-(3-chloro-1H-indol-7-yl)-4-sulfamoylbenzenesulfonamide or a salt thereof, combined with at least one substance selected from (1) irinotecan hydrochloride trihydrate; (2) mitomycin C; (3) 5-fluorouracil; (4) cisplatin; (5) gemcitabine hydrochloride; (6) doxorubicin; (7) taxol; (8) carboplatin; (9) oxaliplatin; (10) capecitabine; and (11) a salt of the above-mentioned (1) to (10).

The present disclosure relates to the field of oncology, more particularly to the field of melanoma. Provided are methods of treating melanoma, particularly advanced cutaneous melanoma, with a combination of pharmaceutical agents comprising MDM4-specific antagonists (such as an inhibitor of the MDM4-p53 interaction or a molecule that decreases MDM4 protein stability) or MDM4-MDM2 dual inhibitors (i.e., molecules that disrupt the interactions between p53 and MDM2 and p53 and MDM4) and one or more chemotherapeutic agents such as for example alkylating agents (i.e., Dacarbazine (DITC) or melphalan), alkylating-like agents (i.e., cisplatin or carboplatin) or mitotic inhibitors (taxanes docetaxel or paclitaxel) and PI3K-AKT, B-RAF and MEK inhibitors. Further provided are pharmaceutical formulations of MDM4-specific antagonists (be it an inhibitor of the MDM4-p53 interaction or a molecule that decreases MDM4 protein stability) or MDM4-MDM2 dual inhibitors (i.e., molecules that disrupt the interactions between p53 and MDM2 and p53 and MDM4) and a pharmaceutical formulation of one or more chemotherapeutic agents such as for example alkylating agents (i.e., Dacarbazine (DITC) or melphalan), alkylating-like agents (i.e., cisplatin or carboplatin) or mitotic inhibitors (taxanes docetaxel or paclitaxel) and B-RAF and MEK inhibitors.

Methods of treating cancer comprising administering a fibroblast growth factor receptor 1 (FGFR1) extracellular domain (ECD) and / or an FGFR1 ECD fusion molecule in combination with at least one additional therapeutic agent selected from docetaxel, paclitaxel, vincristine, carboplatin, cisplatin, oxaliplatin, doxorubicin, 5-fluorouracil (5-FU), leucovorin, pemetrexed, and bevacizumab are provided. Dosage packs comprising an FGFR1 ECD and / or an FGFR1 ECD fusion molecule and / or at least one additional therapeutic agent selected from docetaxel, paclitaxel, vincristine, carboplatin, cisplatin, oxaliplatin, doxorubicin, 5-fluorouracil (5-FU), leucovorin, pemetrexed, and bevacizumab are also provided. In some embodiments, a dosage pack comprises instructions for administering FGFR1 ECD and / or FGFR1 ECD fusion molecule with at least one additional therapeutic agent.

The invention relates to a composite developing thermosensitive gel embolizing agent as well as a preparation method and application thereof. The preparation method comprises the following steps: firstly, preparing a mixed aqueous solution of an anticancer active substance, a thermosensitive material and a developing agent into composite developing thermosensitive gel; secondly, forming a composite developing thermosensitive gel embolizing agent by the composite developing thermosensitive gel and a coagulant on the scene, wherein the thermosensitive material is hydroxyl C1-4 alkyl cellulose, Pluronic, alginate or a mixture of the substances; the anticancer active substance is arsenic trioxide, docetaxel, cisplatin, carboplatin, nedaplatin, oxaliplatin, lobaplatin, miriplatin, siRNA or a mixture of the substances; the developing agent is a water-soluble developing agent of iodixanol, ioversol or iohexol and the like. The preparation method disclosed by the invention is simple and convenient, is suitable for industrial large-scale production, is particularly suitable for preparing an embolizing agent which is biodegradable and good in biocompatibility and is used for hemorrhagic diseases, and is especially suitable for preparing the composite developing thermosensitive gel embolizing agent for treating liver cancer, kidney cancer, lung cancer, prostate cancer, uterine myoma or splenic tumor and the like.

The invention provides a quadrivalent-platinum glycosyl complex for treating tumors and a preparation method thereof. The synthesized compound has good anti-tumor activity better than that of cisplatin and oxaliplatin, and has better stability than that of bivalent platinums such as cisplatin, carboplatin and oxaliplatin. In addition, since the quadrivalent platinum with galactosylated modification has better targeting for tumor cells, the high selectivity to the tumor cells is improved. Furthermore, the compound provided by the invention has the advantages that the problems of poor solubility and more troublesome clinical compatibility of the original bivalent-platinum anti-tumor medicine are solved, and both fat solubility and water solubility are better. The quadrivalent-platinum glycosyl derivative not only can improve the in-vivo availability and enhance the curative effect, but also can reduce the toxic and side effects of the original bivalent-platinum medicine on the kidney and the like.

The present invention provides phosphaplatins, stable isolated monomeric phosphate complexes of platinum (II) and (IV), and methods of use thereof for treating cancers, including cisplatin- and carboplatin-resistant cancers. Unlike cisplatin, these complexes do not readily undergo hydrolysis and are quite soluble and stable in aqueous solutions. Moreover, these complexes-unlike cisplatin, carboplatin, and related platinum-based anti-cancer agents-do not bind DNA. Rather, data suggests that phosphaplatins trigger overexpression of fas and fas-related transcription factors and some proapoptotic genes such as Bak and Bax. Nevertheless, the complexes exhibit tremendous cytotoxicity towards cancer cells. Thus, the present invention provides novel platinum anticancer agents that have a different molecular target than those in the art.

This invention relates a method of treating hyperproliferative diseases. More particularly, the present invention relates to a method of treating hyperproliferative diseases, such as cancer, comprising the step of administering to a mammal in need of such treatment, either simultaneously or sequentially, (i) a therapeutically effective amount of a taxane derivative, a platinium coordination complex selected from the group consisting of carboplatin, tetraplatin, and topotecan, a nucleoside analog selected from the group consisting of gemcitabine hydrochloride and 5-FU, an anthracycline, a topoisomerase selected from the group consisting of etoposide, teniposide, amsacrine, topotecan, and Camptosar®, an aromatase inhibitor; and (ii) a therapeutically effective amount of an isothiazole derivative. The combinations of the present invention may optionally include an anti-hypertensive agent. This invention also relates to pharmaceutical compositions useful in the treatment of hyperproliferative diseases in mammals, containing such combinations. The present invention also relates to kits having a first compartment with a compound of formula 1 and a second compartment containing a taxane derivative, a platinum coordination complex, a nucleoside analog, an anthracycline, a topoisomerase inhibitor, or an aromatase inhibitor and a third compartment containing an anti-hypertensive agent.

The invention relates to a method for preparing an antitumor drug of carboplatin H12C6O4N2Pt, which comprises that: a reagent of cis-diiododiammineplatinum(II) is added with water, stirred uniformly, heated in water bath to 50 to 60 DEG C, kept away from sunshine, added with mercury(I) 1,1-cyclobutyldicarboxylate(Hg2CBDCA) slowly for reaction for 8 to 10 hours; and the products of the reaction are filtered, and c a illiterate is concentrated under reduced pressure and thus solid carboplatin is obtained. The molar ratio of Pt (NH3)2I2 to Hg2CBDCA is 1:1. The method for preparing the carboplain is short in preparation process, avoids introducing an impurities containing Ag+, allows for easy removal of HgI due to small solubility product and achieves high target product yield up to more than 80 percent. (CBDCA is used to replace 1,1-cyclobutyldicarboxylate radical).

The present invention relates to compositions and methods for reducing cell proliferation and / or promoting cell death by inhibiting Drp1. It is based, at least in part, on the discoveries that (i) Drp1 disruption-induced mitochondrial hyperfusion is functionally linked to the cell cycle regulation apparatus, so that Drp1 inhibition results in a disruption of the cell cycle and DNA aberrancies; (ii) inhibition of both Drp1 and ATR are synthetic lethal causing increased DNA damage and apoptotic cell death; and (iii) even in resistant cell lines, Drp1 inhibitor (e.g., mdivi-1) together with a second antiproliferative agent (e.g., cisplatin or carboplatin) act synergistically to promote apoptosis. Accordingly, the present invention provides for novel anticancer strategies.

A method for treating cancer in a mammal includes administering to the mammal in need thereof a therapeutically effective amount of artemisinin (ART) or its derivative, such as dihydroartemisinin (DHA), artemether (ARM), or artesunate (ARS) alone or in combination with a chemotherapeutic agent, such as gemcitabine and carboplatin. A method for inhibiting tumor cell proliferation includes contacting a tumor cell with ART or its derivative, such as DHA, ARM, and ARS, in an amount effective to inhibit tumor cell proliferation or in combination with a chemotherapeutic agent, such as gemcitabine and carboplatin.

The present invention relates to treatment of SCLC with therapeutic ADCs comprising a drug attached to an anti-Trop-2 antibody or antigen-binding antibody fragment. Preferably, the drug is SN-38. More preferably, the antibody is an hRS7 antibody and the ADC is sacituzumab govitecan. The ADC may be administered at a dosage of between 4 mg / kg and 16 mg / kg, preferably 4, 6, 8, 9, 10, 12, or 16 mg / kg, mostly preferably 8 to 10 mg / kg. When administered at specified dosages and schedules, the ADC can reduce solid tumors in size, reduce or eliminate metastases and is effective to treat cancers resistant to standard therapies, such as radiation therapy, chemotherapy or immunotherapy. Surprisingly, the ADC is effective to treat cancers that are refractory to or relapsed from irinotecan or topotecan. Preferably, the ADC is administered as a combination therapy with one or more other anti-cancer treatments, such as carboplatin or cisplatinum.

The invention discloses a fat soluble dual-core cobalt (III) anti-tumor coordination compound and a preparation method thereof. The fat soluble dual-core cobalt (III) anti-tumor coordination compound belongs to lipophilic cobalt anti-tumor coordination compounds. The coordination compound of the invention has a chemical name of N,N'-bis(salicylidene)diamine cobalt (III) ([Co2(C14H12N2O2)3] for short), a molecular formula of C42H33Co2N6O6 and a molecular weight FW of 834.63, and is prepared by using CoAc2.4H2O as a raw material and by the steps of performing a quantitative reaction of the CoAc2.4H2O and ligand N,N'-bis(salicylidene)diamine in a solvent of dimethyl formamide and separating out products. The anti-tumor activity of the coordination compound is 1.6 times that of cis-platinum and 5 times that of carboplatin; an anti-tumor G150 value is 0.35mu g / mL; the activity is higher than those of the cis-platinum and carboplatin; and the coordination compound is low in toxicity and high in fat solubility and is used for clinical tumor treatment.

The invention discloses a water-soluble carboxyl-bridge dicaryon Pt (II) anti-tumor complex, which has a chemical name of cis-tetrammine-miu-di (3-acetoxy-1, 1-cyclobutane dicarboxylate-O1, O2) dicaryon platinum (II), and can be synthesized by adopting the method preparing the conventional platinum based anti-cancer drug. The anticancer activity of the complex of the invention is higher than the platinum based drug of carboplatin commonly used in clinic, the toxic side effect of the invention is significantly lower than the toxic side effect of carboplatin, and the invention can be made into lyophilized powder or injecta to be used in the clinical cancer treatment.

The invention discloses application of cyclic dinucleotide cGAMP to prevention and treatment of tumors through drug combination, belonging to the technical field of biological medicine. The invention also discloses a plurality of drug compositions for prevention and treatment of tumors. The drug compositions for prevention and treatment of tumors are composed of cyclic dinucleotide and one selected from a group consisting of fluorouracil, cyclophosphamide, methotrexate, cisplatin, carboplatin, paclitaxel, vincristine, mitomycin, gemcitabine and actinomycin. Results of in-vivo research show that the drug compositions composed of cyclic dinucleotide and one selected from a group consisting of fluorouracil, cyclophosphamide, methotrexate, cisplatin, carboplatin, paclitaxel, vincristine, mitomycin, gemcitabine and actinomycin have obviously improved curative effect and obviously decreased toxicity.

The invention discloses a new application of brusatol serving as a chemotherapeutic drug synergist, which is combined with a chemotherapeutic drug when in use. The chemotherapeutic drug comprises cis-platinum, carboplatin, oxaliplatin, 5-fluorouracil, paclitaxel, adriamycin or adriamycin. The brusatol provided by the invention can be prepared into an oral preparation or a non-oral preparation accepted pharmaceutically. The beneficial effects of the brusatol applied in preparing the chemotherapeutic drug synergist are as follows: (1) the brusatol can be used in an Nrf2 path, and the killing effect of various chemotherapeutic drugs on the cancer cells can be enhanced; (2) the growth inhibition of low-dose cis-platinum on transplantable tumor of a naked mouse can be increased by the brusatol, thus having clinical application prospects; (3) the cis-platinum content in non-small cell lung cancer cell strains can be increased by the combined use of the brusatol and the cis-platinum; and (4)the toxicity is not discovered when the brusatol and the cis-platinum are together used in the cellular level and in the mouse test work concentration.

Novel lactones of polysaccharide carboxylic acids, and methods for the preparation of a variety of conjugates therefrom, as well as the novel conjugates, are provided. Conjugates include metallo-coordinated cisplatin (and carboplatin), as well as conjugates of ellipticinium, aminoglutethimide, mitoxantrone, mitoguazone, cis 3-hexen-1-ol, and other nucleophilic biologically effective agents. Also provided are conjugates via a coupling agent of biologically effective agents, such as Vitamin E, DTPA, TAXOL and TAXOTERE.

The present invention relates to compositions and methods for reducing cell proliferation and / or promoting cell death by inhibiting Drp1. It is based, at least in part, on the discoveries that (i) Drp1 disruption-induced mitochondrial hyperfusion is functionally linked to the cell cycle regulation apparatus, so that Drp1 inhibition results in a disruption of the cell cycle and DNA aberrancies; (ii) inhibition of both Drp1 and ATR are synthetic lethal causing increased DNA damage and apoptotic cell death; and (iii) even in resistant cell lines, Drp1 inhibitor (e.g., mdivi-1) together with a second antiproliferative agent (e.g., cisplatin or carboplatin) act synergistically to promote apoptosis. Accordingly, the present invention provides for novel anticancer strategies.

Anti-angiogenic gene therapy with a combination of soluble Vascular Endothelial Growth Factors (sVEGFR) improves the efficacy of chemotherapy with paclitaxel for reducing ovarian cancer mean tumor volume (in cubic millimetres) as measured using magnetic resonance imaging. The study groups were: AdLacZ control, combination of AdsVEGFR-1, -2 and -3, combination of AdsVEGFR-1, -2, -3 and paclitaxel, bevacizumab monotherapy, paclitaxel monotherapy and carboplatin monotherapy. Effectiveness was assessed by survival time and surrogate measures such as sequential MRI, immunohistochemistry, microvessel density and tumor growth. Antiangiogenic gene therapy combined with paclitaxel significantly prolonged the mean survival compared to the controls and all other treatment groups (p=0.001). Tumors of the mice treated by gene therapy were significantly smaller than in the control group (p=0.021). The mean vascular density and total vascular area were also significantly smaller in the tumors of the gene therapy group (p=0.01).

The invention relates to carboplatin microspheres for local injection and a method or preparing the same. The preparation is the microspheres which are formed by carboplatin and biologically degradable materials and can slowly release carboplatin in human tissues. The preparation method comprises the following steps of: suspending carboplatin crystals in a proper amount of organic solution of biologically degradable materials to prepare suspension; at room temperature, dropwise adding the suspension into mineral oil solution while stirring for emulsion; volatilizing, cleaning and solidifying the emulsified solution, and filtering to obtain carboplatin microspheres; washing the filtered carboplatin microspheres by using ultra pure water and performing decompression drying; and screening the microspheres with the grain size suitable for injection by using a medicinal screen, and collecting the microspheres for later use. The preparation can be used for tumor injection, locally form a sustained high-drug concentration zone in tumors and act on tumor cells for a long time, but cause a lower side effect on other normal cells.

The present invention relates to a novel class of supermolecular carboplatin derivatives represented by general formula (I), wherein B is a polycarboxylic acid represented by general formula (II), wherein R1, R2 and n are defined as in the description. The present invention also relates to a process for preparing the same, pharmaceutical compositions containing the same as active ingredient and the use of the derivatives in the preparation of pharmaceutical compositions which are useful in treating various cellular cancers including hepatoma, stomach cancer, lung cancer and the like. The derivatives have stable cage-like chemical structures and constitutions in solid and in aqueous solution. The derivatives can not only kill cancer cells at a rate significantly higher than that by carboplatin, in particular, in the case of hepatoma cells, at a rate one to two times higher than that by carboplatin, but also produce little side effects such as vomit, baldness, decreases of leucocytes and platelets, and the like, which can be induced by administration of other chemotherapeutics. In the acute toxicity tests on mice, the lethal dose (LD50) of the present derivatives is about 300 mg / kg and 260 mg / kg body weight for a subcutaneous(sc) and an intraperitoneal(ip) administration, respectively. Therefore, the present derivatives are a novel class of cis-platium which can be widely used as anticancer agents.