760 results about "Anti cancer drugs" patented technology

Compositions and methods are disclosed in embodiments relating to induction of cell death such as in cancer cells. Compounds and related methods for synthesis and use thereof, including the use of compounds in therapy for the treatment of cancer and selective induction of apoptosis in cells are disclosed. Compounds are disclosed that have lower neurotoxicity effects than other compounds.

The invention discloses a VEGF-resistant and PD-1-resistant difunctional antibody and application thereof, belonging to the technical field of molecular immunology. The VEGF-resistant and PD-1-resistant difunctional antibody contains a light chain an a heavy chain, wherein the light chain has an amino acid sequence as shown in SEQ ID NO.2, and the heavy chain has an amino acid sequence as shown in SEQ ID NO.4 or SEQ ID NO.6. Meanwhile, the invention provides a gene for encoding the difunctional antibody and the application of the difunctional antibody. The difunctional antibody provided by the invention can be combined with PD-1 and VEGF, has very high affinity, can be used for effectively simulating T cells to secrete IL2 and induce T cells to secrete IFN-gamma and can also be used for remarkably inhibiting the growth of tumor of a mouse so as to have a huge potential in application to preparation of anti-cancer drugs.

The invention relates to a copper sulfide/mesoporous silicon dioxide core-shell nano material as well as a preparation method and an application thereof. The chemical formula of the core-shell nano material is Cu9S5/mSiO2-PEG. The preparation method comprises the following steps of: (1) raising the temperature of oleylamine under the protection of nitrogen; adding a mixed solution of copper dibutyldithiocarbamate and the oleylamine and dispersing the mixed solution into chloroform to prepare a D solution; (2) dissolving a surfactant into water; raising the temperature and adding the D solution to prepare an E solution; and (3) taking the E solution and adding ethanol; raising the temperature and adding an NaOH solution; immediately adding TEOS (Tetraethylorthosilicate) and reacting; adding PEG-silane; continually reacting and carrying out hydrothermal reaction; and adding into a scrubbing solution to centrifuge and wash to obtain the product. The copper sulfide/mesoporous silicon dioxide core-shell nano material is applied to near-infrared photo-thermal treatment, anti-cancer drugs, chemotherapy of tumors and infrared heat imaging. The nano material disclosed by the invention has very low cell toxicity and very high blood compatibility; and the united effects of thermal therapy and the chemotherapy are good.

The invention relates to small molecules which function as inhibitors of Stat3. The invention also relates to the use of these compounds for inducing cell death and sensitizing cells to the induction of cell death by anti-cancer drugs.

The invention provides a kit for detecting the epidermal growth factor receptor (EGFR) mutation by a primer specific fluorescence polymerase chain reaction (PCR), in particular to the diagnosis of the EGFR gene mutation in tumor tissues and peripheral blood serums of tumor patients. Aiming at specific mutant sites relative to the curative effects of molecular targeted anti-cancer drugs, the kit is provided with a specific oligonucleotide primer sequence and a probe sequence, carries out fluorescence PCR detection respectively through a wild type PCR system and a mutation type PCR system on each sample to be detected and judges whether the samples have the mutation of EGFR19 exons and 21 exons or not through the magnitude of a difference value (delta Ct) of Ct values of two times of reaction. The kit can detect whether the specific sites of the EDFR have the mutation or not and can be used for the curative effect forecast of new molecular targeted anti-cancer drugs and the guidance of clinical individualized medicine application programs of the tumor patients.

The present invention provides a method for treating tumors or tumor metastases in a patient, comprising administering to the patient simultaneously or sequentially a therapeutically effective amount of an EGFR kinase inhibitor and bortezomib combination, with or without additional agents or treatments, such as other anti-cancer drugs or radiation therapy. The invention also encompasses a pharmaceutical composition that is comprised of an EGFR kinase inhibitor and bortezomib combination in combination with a pharmaceutically acceptable carrier. A preferred example of an EGFR kinase inhibitor that can be used in practicing this invention is the compound erlitinib HCl (also known as Tarceva™).

The invention discloses a near-infrared fluorescent magnetic micro-emulsion nanometer particle, its preparation method and application in tumor treatment, wherein magnetic nano-particles and near-infrared luminescent quantum dot nano-particles or near-infrared luminescent organic dyestuff molecules are embedded into water-in-oil micro-emulsion, anti-cancer drugs can also be embedded into the micro-emulsion, the magnetic steering action of the magnetic nano particles will target the micro-emulsion embedded near-infrared fluorescent substances to tumor positions or secure them onto tumor positions under the excitation of near-infrared lights, the thermal effects produced by the near-infrared lights can kill tumor cells, the OH and O2 free radicals with high activity and the optical catalytic activity of the quantum dots can also have synergic actions in destroying tumor cells.

The present disclosure relates to methods and compositions to offset, ameliorate and/or alleviate one or more unwanted and/or adverse gastrointestinal effects. For example, in some embodiments, the present disclosure relates to compositions that include a bile acid, a carbohydrate and/or a pharmaceutical compound, wherein the pharmaceutical is associated with an adverse gastrointestinal effect in a subject (e.g., mammal or human). Non-limiting examples of pharmaceutical compounds may include a nonsteroidal anti-inflammatory drug, a gastric irritating drug (e.g., an antibiotic, an adrenal cortocoid steroid and an anti-cancer drug) and combinations thereof. The disclosure further relates to methods of ameliorating or eliminating at least one adverse gastrointestinal effects of a composition, comprising administering to a subject an aqueous solution comprising a bile acid and a carbohydrate.

The present invention is based, in part, on the identification of novel methods for defining predictive biomarkers of response to anti-cancer drugs.

Disclosed is an anti solid tumor medicine composition, which comprises medicinal adjuvant and DNA restoring enzyme inhibitor and/or Nitrosoureas anti-cancer drugs, wherein the DAN restoring enzyme inhibitor is selected from methoxamine, hydroxylamine and their analogues, which can effectively destroy the DNA restoring function in the tumor cells, and lower the survivability of tumor cell to Semustine anti-cancer drugs and their analogues, the medicinal adjuvant is biological compactable, degradable and absorbing macromolecular polymer, which can slowly release the DNA restoring enzyme inhibitor onto tumor partially during the degradation and absorption process, thus the whole body toxicity reaction is reduced appreciably , and the effective medicinal concentration can be sustained to the tumor partially. By dispensing the composition to the tumor partially, the whole body toxicity reaction of Nitrosoureas anti-cancer drugs and/or DNA restoring enzyme inhibitor can be lowered, selectively increase the tumor local medicinal concentration, and the treatment effect of the non-operative treatment methods such as chemotherapy, medicament and radiation can be improved.

The invention discloses a cancer driving gene screening method based on gene mutation frequency and belongs to the field of cancer medicine. The method comprises the steps that (1) tumor gene mutation data is acquired; (2) the mutation data is preprocessed; (3) adjacent genes of each gene are screened; (4) background mutation data of each kind of mutation is calculated; and (5) hypothesis testing is used to screen mutation genes according to mutation values. According to the method, a modern high-throughput sequencing technology, DNA data processing software, a classic clustering algorithm and a classic statistical method are utilized and combined with biotic factors influencing gene mutation, so that screening of cancer driving genes is more precise, and the method has an important meaning for both research and development of novel anti-cancer drugs and clinical diagnosis and treatment of cancers.

The invention provides a preparation method of a supramolecular anti-cancer drug (dicycloplatin). The preparation method comprises the following steps of: adding carboplatin and 1,1-cyclobutanedicarboxylic acid into water according to the mol ratio of 1:1, dissolving and uniformly mixing to obtain the mixed solution, and standing the mixed solution in a dark place at the temperature of more than 0 DEG C and less than or equal to 60 DEG C for 3-9 days, and concentrating under reduced pressure or freeze-drying so as to obtain dicycloplatin. The preparation method disclosed by the invention is moderate in condition and environment friendly; both the yield and the purity of dicycloplatin can be up to nearly 100%; the batch yield can reach 1000g; and thus, the preparation method is particularly applied to industrial production.

The invention discloses a nano-drug carrier with the magnetothermal and photothermal effects. The particle size is 50 nanometers to 300 nanometers, and the nano-drug carrier is prepared from mesoporous silica particles, Fe3O4 nanoparticles embedded into the mesoporous silica particles and graphene oxide with which the surfaces of the mesoporous silica particles are coated. The invention further provides a preparation method of the nano-drug carrier. The superparamagnetic Fe3O4 nanoparticles are prepared through a solvothermal method, the Fe3O4 nanoparticles are composited by taking hexadecyl trimethyl ammonium bromide as a structure-directing agent and taking tetraethoxysilane as a silicon source through the sol-gel self-assembling process, and then magnetic mesoporous nanoparticles Fe3O4/mSiO2 with the magnetic property adjustable and controllable are prepared; the surfaces of the Fe3O4/mSiO2 mesoporous nanoparticles are coated with graphene through the ion interaction or electrostatic interaction or hydrogen-bond interaction, and then the nano-drug carrier which both can efficiently deliver anti-cancer drugs and has the magnetothermal and photothermal effects is obtained. Accordingly, cancer treatment in which medical chemotherapy cooperates with magnetothermal and photothermal treatment can be achieved.

The invention discloses a method of catalyzing and synthesizing alpha-glyceryl linolenate with immobilized lipolytic enzyme in the manufacturing method field of a anti-cancer drug material, which comprises the following steps: making immobilized enzyme carrier including hole enlarge of dielectric hole material and the amido modification; making immobilized lipolytic enzyme, synthesizing alpha-glyceryl linolenate with immobilized enzyme in organic medium. The invention provides a good steady, and SBA-15 still shows regular hexagonal structure after modification, a uniform pore path, a big aperture and meets the need of synthesizing alpha-glyceryl linolenate; improvement of the lipase proper temperature improves the productivity; the product is provided with a light yellow color, a good quality, a good curative effect, enhancing heat stability.

The present invention provides a method for treating tumors or tumor metastases in a patient, comprising administering to the patient simultaneously or sequentially a therapeutically effective amount of an EGFR kinase inhibitor and capecitabine combination, with or without additional agents or treatments, such as other anti-cancer drugs or radiation therapy. The invention also encompasses a pharmaceutical composition that is comprised of an EGFR kinase inhibitor and capecitabine combination in combination with a pharmaceutically acceptable carrier. A preferred example of an EGFR kinase inhibitor that can be used in practicing this invention is the compound erlotinib HCl (also known as TARCEVA®).

Methods for treating and preventing the onset and maintainance of multiple drug resistance (MDR) in animals undergoing chemotherapy for cancer are provided. According to the methods, target cells are depleted of adenosine 5'-monophosphate (AMP) and adenosine 5'-triphosphate (ATP) such that the cells are unable to support P-glycoprotein activity. According to one method, a population of target cells is obtained from a host and assayed for loss of methylthioadenosine phosphorylase (MTAse) activity. MTAse catabolizes methylthioadenosine to adenine for endogenous salvage incorporation into the intracellular AMP pool. MTAse deficient cells are treated with a purine synthesis inhibitor, such as L-alanosine, which starves the cells of adenine and suppresses P-glycoprotein activity. MTAse competent cells are also treated for MDR with purine synthesis inhibitors. In conjunction with treatment according to the invention, MTAse competent and deficient cells are also treated for malignancy with other anti-cancer drugs. A method for protecting non-malignant cells from adenine starvation during treatment of malignant cells according to the invention is provided.

The invention belongs to the field of synthesis of drug carrier base materials and provides a nano particle-polymer injectable composite hydrogel double drug loading system and a preparation method thereof. The double drug loading system is loaded with not only an anti-cancer drug I of which polymer nano particles are synthesized through a disulfide bond cross-linking agent by taking acrylic acidand 4-vinylphenylboric acid as monomers, but also an anti-cancer drug II of which injectable hydrogel is synthesized through Michael addition reaction between a macromolecular cross-linking agent witha sulfhydryl functional group and a polymer containing a catechol functional group aiming at the drug loading capacity, the action time, the treatment effect and other demands. The bi-stimulus response is pH stimulus response and reducing stimulus response of glutathione to the disulfide bond cross-linking agent in a tumor cell environment respectively, the interaction between the nano particlesand the drug I as well as the degradation process of the nano particle can be affected, and the long-term delivery of the drug I is realized. The nano particle-polymer injectable composite hydrogel double drug loading system provided by the invention realizes the effects of local long-time administration, step-by-step osmotic treatment and combined treatment of a variety of drugs.

This invention features methods of identifying genetic alterations that can modulate cancer cells' sensitivity to an anti-cancer drug. Information on such genetic alterations can be used to predict cancer therapeutic outcomes and to stratify patient populations to maximize therapeutic efficacy.

The present invention relates to integrin ligand modified long circulation liposome carrying anticarcinogen for injection, and is especially one kind of injected anticarcinogen carrying targeting liposome administration system. The efficient administration system is obtained through modifying the surface of liposome simultaneously with both polyethylene glycol and integrin containing arginine-glycine-asparagic acid sequence or RGD analogue.

The paclitaxel has broad spectrum antineoplastic activity, which is used to treat oophoron cancer and breast cancer, has the significant effect, and is known as a anti-cancer drug with the wide developing prospect, but the particle diameter of paclitaxel medicine powder is bigger so that the paclitaxel medicine powder isn't absorbed by administer orally, has the lower bioavailability, and limits the clinic application of paclitaxel. The invention makes Paclitaxel fine with supercritical flow new technique. The experiment makes Paclitaxel fine with above-critical CO2 as the dissolvent and with supercritical flow forced disperse solution technique, which researches the influence of the pressure, the temperature, the concentration of the solution and the flow speed of the solution for the shape, grain diameter and the distribution of fine paclitaxel. The result indicates that the nanometer grain diameter can be changed in the finite range by changing the technology parameter, wherein the prepared surface of the nanometer grain is smooth, and has the good sphericity, and the average grain diameter is 670nm-940nm, the concentration of the solution and the flow speed is the main factor.

The invention relates to a tumor vessel-tumor cell membrane-cell nucleus continuous targeted drug delivery system, as well as a preparation method and application thereof. The tumor vessel-tumor cell membrane-cell nucleus continuous targeted drug delivery system comprises mesoporous silica nano-particles, RGD polypeptide which is linked to the surfaces of the mesoporous silica nano-particles in a covalent manner and serves as a tumor vessel/tumor cell membrane targeting ligand, and a nuclear localization signal polypeptide sequence serving as a cell nucleus targeting ligand. Under the condition of intravenous injection, the drug-loaded system can be enriched in a tumor tissue by means of the targeting effect of the tumor vessel to reduce the uptake of normal tissues and reduce toxic and side effect, is capable of increasing the phagocytosis amount of tumor cells by means of the identification effect on the tumor cell membrane, and can be used for directly delivering anti-cancer drugs into a cell nucleus by means of the delivery performance of the cell nucleus to increase the concentration of effective drugs, so that an optimal treatment effect can be achieved.

The invention discloses a multifunctional multilayered micro/nano core-shell structure. The core-shell structure is a micro/nanoscale spherical structure, and the ''multilayer'' includes three or more layers. At least one layer of material is a liquid phase. The liquid phase can selectively be removed. Thickness of each shell is controllable, and each shell can effectively and independently coat multiple materials or anti-cancer drugs with different properties at the same time. By adding functional auxiliary materials into each phase, combination of multifunctional characteristics can be realized. By integrating advantages of the multilayered core-shell structure and excellent optical, electrical, magnetic, sound and biological characteristics, drug controlled release and medical imaging application can be realized. The multifunctional multilayered micro/nano core-shell structure has an application prospect especially in aspects of disease treatment and medical imaging and is used as a bimodal ultrasonic/magnetic imaging diagnosis contrast agent and drug release control carrier.

The invention relates to a new synthesis technology of anti-cancer drug Raltitrexed. The technology comprises the following steps: 1) using L-glutamic acid as raw material to perform esterification with alcohol under the action of halogenating agent and obtain L-glutamic acid diester hydrochloride; 2) using 2-amino-5-methyl-benzoic acid as raw material to prepare 6-bromomethyl-3,4-dihydro-2-methyl-4-oxo-6-quinazoline through cyclization, amination and bromination; 3) using 2-thienyl-propanedioic acid as raw material to prepare N-[5-[N-(tert-butoxycarbonyl)-N-methylamino]-2-thenoyl]-L-glutamic acid diethyl ester through nitrification, esterification, reduction, amino protection, N-methylation and device-esterification; 4) using L-glutamic acid diester hydrochloride and N-[5-[N-(tert-butoxycarbonyl)-N-methylamino]-2-thenoyl]-L-glutamic acid diethyl ester to prepare N-[5-(N-methylamino)-2-thenoyl]-L-glutamic acid diester through dehydrant condensation and deamination protection; and 5) using N-[5-(N-methylamino)-2-thenoyl]-L-glutamic acid diester and 6-bromomethyl-3,4-dihydro-2-methyl-4-oxo-6-quinazoline to perform condensation under the catalysis of alkali, recycling preparative chromatography, purifying, and performing de-esterification to obtain Raltitrexed.

Disclosed is an anti-cancer drugs slow release agent containing Epothilone which comprises slow release microspheres and dissolvent, wherein the slow release microballoons comprise anti-cancer active constituents and slow release auxiliary materials, the dissolvent being specific dissolvent containing suspension adjuvant. The anticancer active constituents include Epothilone, Epothilone derivatives, Epothilone B, Epothilone D and combination of anti-cancer drugs selected from phosphoinositide-3-kinase inhibitor, of pyrimidine analogues and/or DNA restoring enzyme inhibitor, the slow release auxiliary materials include polylactic acid and its copolymer, polyethylene glycol, PLA-COOH copolymer, di-aliphatic acid and sebacylic acid copolymer, poly(erucic aciddipolymer-sebacylic acid), poly(fumaric acid-sebacylic acid), Polifeprosan, polylactic acid and other biocompatible high polymers, the viscosity of the suspension adjuvant is 100-3000cp (at 20-30 deg C), and is selected from sodium carboxymethylcellulose. The anticancer active constituents and the slow release microspheres can also be prepared into slow release implanting agent for intra-tumor or around-tumor injection or placement for the effective suppression of tumor growth and for the appreciable enhancement for curative effects of non-operative treatments such as chemotherapy.

The invention relates to an anti-cancer sustained release injection containing epothilone derivative, consisting of sustained microspheres and menstruum. The sustained microspheres comprise anti-cancer drugs selected from taxane, alkylating agent and/or plant alkaloid and the like, the epothilone derivative and sustained release auxiliary material. The menstruum is a special menstruum containing suspending agent. The epothilone derivative is selected from epothilone B, epothilone D, iso-epothilone D, BMS-247550, azaepothilone B, furan epothilone D or BMS-310705. The sustained release auxiliary material is selected from poly-dl-lactide, the glycolic acid copolymer of the poly-dl-lactide, polyethyleneglycol, the polylactide copolymer of the polyethyleneglycol, carboxyl terminated polylactide copolymer, fatty acid and decanedioic acid copolymer, etc. The suspending agent is selected from carboxymethyl cellulose and the like with the viscosity of 100cp to 3000cp (under the temperature of 25 DEG C to 30 DEG C). The sustained release microsphere can also be made into a sustained release implant. The sustained release injection is injected or arranged in or around the tumour and can release drug at partial position for 40 days approximately, therefore, the sustained release injection improves the local drug concentration selectively and enhances the treatment effect of non-operative treatments, such as radiotherapy, chemotherapy and the like at the same time.

Methods for preparing and isolating polymer conjugates that include a recurring unit of Formulae (I) and (Ia) are described herein. The polymer conjugates can include an anti-cancer drug.

The invention relates to an anti-cancer sustained release injection containing epothilone derivative, consisting of sustained microspheres and menstruum. The sustained microspheres comprise anti-cancer drugs selected from taxane, alkylating agent and/or plant alkaloid and the like, the epothilone derivative and sustained release auxiliary material. The menstruum is a special menstruum containing suspending agent. The epothilone derivative is selected from epothilone B, epothilone D, iso-epothilone D, BMS-247550, azaepothilone B, furan epothilone D or BMS-310705. The sustained release auxiliary material is selected from poly-dl-lactide, the glycolic acid copolymer of the poly-dl-lactide, polyethyleneglycol, the polylactide copolymer of the polyethyleneglycol, carboxyl terminated polylactide copolymer, fatty acid and decanedioic acid copolymer, etc. The suspending agent is selected from carboxymethyl cellulose and the like with the viscosity of 100cp to 3000cp (under the temperature of 25 DEG C to 30 DEG C). The sustained release microsphere can also be made into a sustained release implant. The sustained release injection is injected or arranged in or around the tumour and can release drug at partial position for 40 days approximately, therefore, the sustained release injection improves the local drug concentration selectively and enhances the treatment effect of non-operative treatments, such as radiotherapy, chemotherapy and the like at the same time.

The invention provides methods and materials for screening for polymorphic variants in ABCB1 and diagnosing altered susceptibilities for drug-induced heart rhythm irregularities based on the same. These methods allow better treatment regimens for using drugs that bind a protein encoded by the ABCB1 and/or induce heart rhythm irregularities such as the anti-cancer drug FK228.

The invention discloses a plant anti-cancer targeting nano-preparation, and a preparation method of the nano-preparation. The nano-preparation comprises (by weight) 43-60% of human blood albumin, 1.5-7.5% of plant anti-cancer drug, 24-40% of hyaluronic acid with molecular weight of 3,000-1,800,000 Da, 3.5-15 % of nanoparticle stabilizer, and the balance of water. The preparation method includes preparation of hyaluronic acid-albumin conjugate; preparation of plant anti-cancer drug solution; and preparation of the targeting nano-preparation. The plant anti-cancer targeting nano-preparation has good stability and bio-targeting function.

A computerized decision support system and method for predicting which of one or more drugs suitable to treat a cancerous condition in a patient are the optimum drug(s), where such selection is based upon the particular patient's genotype. A PCR kit and/or a gene chip detects multiple genes, expressions and/or mutations associated with a particular cancer using a sample of the patient's tissue or blood. A detector accepts the gene chip and analyzes the patient's genotype; and a computerized system using a database which associates patient genotypes and the efficacy and toxicity of various anti-cancer drugs used in treating patients with a particular cancerous condition connected to the detector correlates the output of the detector to the database to provide a recommendation as to which drugs are optimum for treating the patient's cancer.