100 results about "Cardiotoxicities" patented technology

The present invention provides a method, system and composition for screening drug candidates for cardiotoxicity and for novel drugs that effect cardiomyocyte contractility and function. The invention provides an efficient and reliable screening assay to detect the effect of new and potential drug candidates on cardiomyocyte calcium flux, membrane depolarization, and / or the propagation of action potentials.

This disclosure provides methods and pharmaceutical compositions for reducing or eliminating cardiotoxicity, particularly cardiotoxicity induced by a cancer treatment or other therapy. In some cases, the methods and compositions prevent or reduce cardiotoxicity caused by anthracycline treatment. The methods provided herein often comprise administering a protective agent such as myricetin, tricetin, robinetin, ficetin, vitexin, quercetin, dihydrorobinetin, kaempferol, 7,3′,4′,5′-tetrahydroxyflavone, and myricitrin in conjunction with the administration of a cancer drug or other treatment. They may comprise administering a protective agent in combination with dexrazoxane. The compositions provided herein include co-formulations of a protective agent with a different protective agent or with a cancer treatment (e.g., anthracycline drug).

The present invention relates to therapeutic uses of ErbB ligands, including betacellulin. The therapeutic uses include methods of using ErbB ligand family compounds alone, or in conjunction with other agents, for reducing blood glucose levels, treating Type I and Type II diabetes, obesity, muscle wasting diseases, and cardiotoxicity.

The invention discloses an application of endogenous small molecular substances to rapid detection of early cardiotoxicity, wherein the endogenous small molecular substances refers to nine early cardiotoxicity biomarkers: L-carnitine, L-tryptophan, L-palmitoyl carnitine, 19-hydroxyl deoxycorticosterone, cholic acid, lysophosphatidyl choline (14: 0), lysophosphatidyl choline (22: 6), lysophosphatidyl choline (20: 2) and lysophosphatidyl choline (16: 0), and also refers to four early cardiotoxicity exclusive biomarkers: L-carnitine, 19-hydroxyl deoxycorticosterone, lysophosphatidyl choline (14: 0) and lysophosphatidyl choline (20: 2). According to the application of the endogenous small molecular substances to the rapid detection of the early cardiotoxicity, the screened early cardiotoxicity biomarkers are capable of giving rapid alarms to the toxicity before the heart tissues suffer pathological damages, so that the toxicity discovery time is early than the conventional biochemical detection indexes, more flexible judgement is carried out on the drug toxicity and diseases, and more time is provided for the early discovery and early treatment of the clinic cardiotoxicity.

The invention discloses an application of chiral chloroquine, hydroxychloroquine or pharmaceutically acceptable salts of the chiral chloroquine and hydroxychloroquine in preparation of drugs used forpreventing and / or treating coronavirus pneumonia by using a coronavirus key drug target 3CL hydrolase (Mpro) as an action target. The chiral chloroquine and hydroxychloroquine have high bonding strength with the Mpro causing inflammation of the lung and the like; the activity of the Mpro can be significantly inhibited; and the chiral chloroquine and hydroxychloroquine are indicated to have the effect of preventing and treating pneumonia caused by coronaviruses and be able to be used as anti-pneumonia drugs. Through evaluation on the inhibitory activity of an hERG potassium ion channel, the concentration at which the chloroquine, hydroxychloroquine and enantiomers of the chloroquine and hydroxychloroquine are likely to generate cardiotoxicity to the hERG potassium ion channel is provided. The chiral chloroquine and hydroxychloroquine are prepared through chiral high-performance liquid chromatography and chiral synthesis; S-configuration chloroquine, hydroxychloroquine or salts of the chloroquine and hydroxychloroquine can be selected as a drug independently, or form a pharmaceutical composition for treating diseases caused by the coronaviruses; and due to higher activity and low cardiotoxicity of the chloroquine, hydroxychloroquine or salts of the chloroquine and hydroxychloroquine, the administration dosage range is greatly widened.

The present invention discloses new rocaglaol derivatives and the use of rocaglaol derivatives to prevent or to limit the cardiotoxicity of an antineoplastic agent, in particular to prevent or to limit the apoptosis of cardiomyocytes induced by such agent.

The invention provides a method for evaluating various types of cardiotoxicity of tumor patients, and for the tumor patients, the evaluation factors related to the existing Meio cardiotoxicity scoring are limited, and the evaluation suggestions are general. According to the method provided by the invention, risk factors which have been researched and proved to have influences on cardiotoxicity are introduced, values are assigned to the risk factors according to the correlation degrees of the risk factors and various cardiotoxicity risks, an evaluation model is established by referring to a Meio scoring system, risk grading is carried out on the six types of cardiotoxicity, and corresponding evaluation suggestions are given; and according to the method, an existing evaluation system is expanded, the blank of domestic cardiotoxicity evaluation is filled, and reliable basis and suggestions are provided for clinicians to treat and follow up tumor patients.

The invention provides a method and a system for evaluating cardiotoxicity of an immune checkpoint inhibitor, and a storage device. In the prior art, oncology department doctors and surgeons cannot clearly determine the risk of cardiovascular disease complications, and early clinical manifestations of CVD are easily ignored, so that adverse clinical events caused by delayed treatment can be caused. A purpose of the invention is to solve the problem in the prior art. According to the invention, a risk assessment calculation method is adopted to assist a non-cardiologist to assess the risk of acardiovascular event, so that the non-cardiologist can be helped to quickly identify high-risk groups in the early stage, professional treatment suggestions are sought for the cardiac specialist, theoccurrence of the cardiovascular event can be reduced, and the severity of the event can be reduced.

The invention discloses application of remdesivir in preparation of a medicine for inhibiting cardiotoxicity of anti-tumor medicines. The invention confirms significant potential of the retegravir asa medicine for inhibiting the cardiotoxicity of anti-tumor medicines, discloses good curative effects of the retegravir on the cardiotoxicity caused by the anti-tumor medicines for the first time, provides an effective novel potential alternative medicine for treating the cardiotoxicity of the anti-tumor medicines, expands indications of the retegravir, and greatly improves application potential and market prospect of the retegravir.

The present invention relates to anthracycline derivatives that are based on an Aloe-emodin (AE) backbone attached to a glycoside (an amino sugar or amino carba-sugar). These derivatives are useful as chemotherapeutic agents. Advantageously, these derivatives are potent cytotoxic agents against a variety of anthracycline-resistant tumors. In addition, they may have reduced cardiotoxicity. As such, the novel compounds of the invention offer an advantage over currently available drugs. The present invention further relates to methods for preparing the novel Aloe-Emodin Glycoside (AEG) based derivatives, pharmaceutical compositions including such compounds, and methods of using these compounds and compositions, especially as chemotherapeutic agents for prevention and treatment of cancers.

The invention discloses a sulfhydryl compound serving as a histone deacetylase inhibitor, and an application thereof. Pharmacological experiment results show that the composition has high anti-proliferative activity on various tumor cells, shows a protective effect on glutamic acid-induced neuronal cell damage on a cell model, has low toxicity to normal cells, low potential cardiotoxicity, ideal pharmacokinetic characteristics and high blood-brain barrier permeability, and has a development prospect as a high-efficiency low-toxicity antitumor or neurodegenerative disease treatment agent. The sulfhydryl compound is a compound with a structural general formula represented by formula (I) shown in the description, or a pharmaceutically acceptable salt, an ester or a prodrug thereof.

The invention provides safe coxsackie virus for treating KRAS mutant tumors, and a pharmaceutical composition thereof, specifically coxsackie virus capable of specifically infecting tumor cells, wherein the coxsackie virus specifically infects tumor cells, and the ratio R1 (F1 / F0) of the infection rate F1 of the coxsackie virus to normal myocardial cells to the infection rate F0 of wild type coxsackie virus subtype 3 to normal myocardial cells is less than or equal to 1 / 500. The coxsackie virus disclosed by the invention infects tumor cells with high specificity, and hardly infects normal cells, so that the cardiotoxicity of the coxsackie virus is greatly reduced and even eliminated.

The invention relates to the technical field of traditional Chinese medicines, in particular to a drug composition for preventing and treating cardiotoxicity induced by anthracycline antibiotics and application for the drug composition. Experiments prove that glycyrrhizin can weaken the cardiotoxicity caused by doxorubicin, lower a myocardial enzyme level and improve an inflammatory response, so that the lethality caused by doxorubicin cardiotoxicity is lowered, and the drug composition has the remarkable protective effect to the cardiotoxicity induced by the doxorubicin. The drug compositioncan be used for preventing and lightening the cardiotoxicity induced by anthracycline antibiotics and has the clinical practicability.

The invention relates to double-layer microspheres loaded with parecoxib, interleukin-4 and bovine serum albumin and used for treating osteoarthritis and a preparation method of the double-layer microspheres, and belongs to the technical field of drug carrier research. Drugs carrying different physical and chemical properties are prepared by two-time multiple emulsion solvent volatilization method, the purpose of the invention is to solve the bottleneck problems of clinically restricting osteoarthritis drug treatment at present or meet urgent requirements of people for handling of pain and mobility inconvenience problems caused by inflammatory reaction during osteoarthritis attack, infection problem caused by repeated injection in articular cavity injection, and the problem of poor patient medication dependency caused by cardiotoxicity and gastrointestinal reaction caused by oral administration of non-steroidal anti-inflammatory drugs, and long-term chronic properties of osteoarthritis.

The Cardiac Tissue Engineered Model (TEEM) invention provides a robust in vitro model for cardiotoxicity evaluation using three-dimensional (3D) human heart microtissues to quantify dose-dependent changes in electromechanical activity, resulting in a comprehensive cardiotoxicity and arrhythmia risk assessment of test compounds. The invention also provides a predictive in vitro screening platform for pro-arrhythmic toxicity testing using human three-dimensional cardiac microtissues. The invention enables the screening of environmental and pharmaceutical compounds, chemicals, and toxicants to establish safe human exposure levels.

The invention discloses a traditional Chinese medicinal prescription for relieving the syndrome of cardiotoxicity due to radiotherapy and chemotherapy and a preparation method thereof. The prescription comprises the following raw materials by weight: 5g of liquorice, 8g of stephanotis, 8g of dadvid bushclover root or herb, 6g of polygonum chinense L., 12g of nanocnide lobata, 4g of velvety clovershrub root, 6g of impatiens balsamina, 8g of cottonrose hibiscus flower, 5g of ficus lyrata, 10g of begonia fimbristipula, 3g of coral lodiscus flabellate, and 6g of paramichelia baillonii. The traditional Chinese medicinal prescription for relieving syndrome of cardiotoxicity due to radiotherapy and chemotherapy is remarkable in curative effect, does not have side effects, and can be used for treating complications due to cardiotoxicity.

The invention provides a method of reducing anthracycline-induced cardiotoxicity by administering a toxicity-reducing compound, such as a compound of Formulas (I), (II) or (III) or a combination thereof, and / or diphenyl urea (DPU), dexrazoxane (DEX), to a patient receiving an anthracycline. The invention also provides a method of identifying toxicity-reducing compounds.

The invention discloses a HER-2 humanized monoclonal antibody long-acting sustained-release preparation. The preparation comprises 2-50 wt% of an amphiphilic block copolymer mixture, 0.05-10 wt% of anHER-2 humanized monoclonal antibody and 40-88 wt% of a menstruum, and the storage modulus and the loss modulus of an amphiphilic block copolymer mixture aqueous solution have an intersection point at0-55 DEG C. By utilizing the dual action of the diffusion of the HER-2 humanized monoclonal antibody along with drugs and gel degradation, the stable and slow release is realized, so that tumor recurrence is inhibited, and the drug utilization rate is increased; within the dosage range of 0.05-10 wt%, the cardiotoxicity of the preparation can be remarkably reduced; and moreover, the release kinetics of the drugs can be effectively regulated and controlled by changing the mixing ratio of a block copolymer carrier, and the administration frequency can be effectively reduced. Besides, the invention further discloses a preparation method of the HER-2 humanized monoclonal antibody long-acting sustained-release preparation, and the method is simple in condition and high in practicability and has good market application potential.

A method of screening a composition for cardiotoxicity comprising contacting the composition with cardiomyocytes that have increased fatty acid oxidation and / or diminished glucose oxidation. The cardiomyocytes are preferably prepared by overexpression of COX7A1. The cardiomyocytes are preferably provided in a micropatterned co-culture to provide a mature functional hPSC-CM cardiotoxicity model.

The invention discloses a compound represented by the following formula I and a racemate, a stereoisomer, a tautomer, an isotope marker, a nitrogen oxide, a solvate, a polymorph, a metabolite, an ester, a pharmaceutically acceptable salt or a prodrug thereof. The compound shown in the formula I has excellent ROCK inhibition activity. In addition, the compound shown in the formula I has good safetyand metabolic stability. Furthermore, the potential cardiotoxicity risk of the compound shown in the formula I is low. Finally, the compound shown in the formula I is simple in preparation method andeasy to purify, so that the compound has a good application prospect.

The invention belongs to the technical field of medicines for preventing and treating cardiotoxicity, and particularly relates to application of breviscapine as a chemotherapeutic medicine for preventing and treating cardiotoxicity. According to the defect of the existing listed product-dexrazolidone, the breviscapine shows the characteristics and advantages of the breviscapine in prevention and treatment application in the aspects of cardiotoxicity protection of anthracycline chemotherapeutics and the like, and meanwhile, the breviscapine is low in raw material cost, good in safety basis and suitable for industrial production. The compound can be used as an active component or a medicine composition component for myocardial protection of anthracycline chemotherapeutics, the cardiotoxicity caused by the chemotherapeutics is reduced, and the life quality and the treatment prognosis of tumor patients are improved.

The invention provides a compound with a central nervous system disease treatment effect and a structure shown in a formula I. The compound has 5-HT2A receptor antagonist or inverse agonist activity, and has the advantages of high selectivity to 5-HT2A receptors, low cardiotoxicity, good metabolic stability, and no toxic or side effect. The compound can be used for treating certain mental diseases (such as depression, anxiety, psychosis, schizophrenia, insomnia and autism) and mental disorder symptoms related to or concurrent with central nervous system degenerative diseases (such as Alzheimer's disease, Parkinson's disease, Huntington's disease and Lewy small body dementia).

The invention belongs to the technical field of medicines, relates to application of a mitoxantrone and berberine composition in preparation of anti-tumor drugs, and also relates to application of themitoxantrone and berberine composition in reduction of mitoxantrone cardiotoxicity. The composition contains mitoxantrone or salt thereof, and berberine or salt thereof. In the pharmaceutical composition, the mass ratio of the mitoxantrone or the salt thereof to the berberine or the salt thereof is (10:1)-(1:10), preferably (2:1)-(1:10). The invention also provides double-drug-loading liposome ofthe composition. The double-drug-loading liposome has relatively high drug loading capacity, and two drugs can be maintained in a synergistic effect proportion range for a long time in a blood circulation process, so that the synergistic proportion delivery at tumor tissues is favorably realized, and the anti-tumor effect is further improved. The cardiotoxicity of a patient to the mitoxantrone can be further reduced, and higher safety is achieved.

The invention provides a compound with a central nervous system disease treatment effect and a structure shown in a formula I. The compound has 5-HT2A receptor antagonist or inverse agonist activity, and has the advantages of high selectivity to 5-HT2A receptors, low cardiotoxicity, good metabolic stability, and no toxic or side effect. The compound can be used for treating certain mental diseases (such as depression, anxiety, psychosis, schizophrenia, insomnia and autism) and mental disorder symptoms related to or concurrent with central nervous system degenerative diseases (such as Alzheimer's disease, Parkinson's disease, Huntington's disease and Lewy small body dementia).

The invention provides a compound with a central nervous system disease treatment effect and a structure shown represented by formula I. The compound has 5-HT2A receptor antagonist or inverse agonist activity, and has the advantages of high selectivity to 5-HT2A receptors, low cardiotoxicity, good metabolic stability, and no toxic or side effect. The compound can be used for treating certain mental diseases (such as depression, anxiety, psychosis, schizophrenia, insomnia and autism) and mental disorder symptoms related to or concurrent with central nervous system degenerative diseases (such as Alzheimer's disease, Parkinson's disease, Huntington's disease and Lewy small body dementia).

The invention relates to the field of anticancer drug compounds, in particular to a doxorubicin-containing composition and application thereof. The doxorubicin-containing composition comprises the following components in parts by weight: 0.01-10 parts of doxorubicin and 1-100 parts of formononetin. The invention also provides an application of the composition in preparation of a pharmaceutical composition for treating tumors, wherein the tumors refer to breast cancer, liver cancer or glioma. The combination of the doxorubicin and the formononetin can reduce the cardiotoxicity of the doxorubicin, the combination of the doxorubicin and the formononetin has a synergistic effect on tumor treatment, and the dosage of the doxorubicin can be reduced.

The invention belongs to the field of pharmaceutical compositions, and particularly relates to a pharmaceutical composition containing NAD (Nicotinamide Adenine Dinucleotide) and application thereof. The invention provides a pharmaceutical composition containing NAD (Nicotinamide Adenine Dinucleotide). The pharmaceutical composition comprises NAD and a CD38 inhibitor. The pharmaceutical composition enhances the prevention and / or treatment effect of NAD on cardiotoxicity caused by cancer chemotherapy drugs, and expands the treatment range of NAD.

The invention discloses an anthraquinonotriazole antibiotic nucleoside analog, a synthetic method and application of the anthraquinonotriazole antibiotic nucleoside analog in the preparation of an antineoplastic or antiviral drug, and belongs to the field of chemical and medical technologies. According to the key points of the technical scheme, the structural formula of the anthraquinonotriazole antibiotic nucleoside analog is as shown in the specification. The invention also specifically discloses a synthetic method of the anthraquinonotriazole antibiotic nucleoside analog and application ofthe anthraquinonotriazole antibiotic nucleoside analog in the preparation of an antineoplastic or / and antiviral drug. A series of anthraquinonotriazole antibiotic nucleoside analogs with novel structure and bioactivity are prepared in the invention. It is found through biological activity tests that the compounds have good antineoplastic and antiviral activity and can be used for preparation of anantineoplastic or antiviral drug so as to furthermore effectively overcome toxic and side effect such as cardiotoxicity, drug resistance and the like generated by the current long-term use of anthracene nucleus antibiotic drugs.