55 results about "Statine" patented technology

Described is an antibody-drug conjugate (ADC) having the formula A-L, wherein A is an antibody or an antibody fragment and wherein L is a linker, said linker comprising: as a first payload a topoisomerase I inhibitor which is cell-permeable, e.g., a camptothecin cytotoxic molecule which is cell-permeable; as a second payload a topoisomerase I inhibitor which is not cell-permeable, e..g., a camptothecin cytotoxic molecule which is not cell-permeable; and as a as a third payload a toxin or a cytotoxin, e.g., an auristatin such asMMAE (Monomethyl auristatin E). Moreover, described is a pharmaceutical composition comprising said ADC and at least one pharmaceutically acceptable ingredient. Further, described method of treating a patient suffering from, being at risk of developing, and / or being diagnosed for a neoplastic disease.

An antibody-drug conjugate as shown in formula I, a preparation method therefor, and a use thereof in prevention and / or treatment of diseases related to abnormal cell activity, including but not limited to a use in prevention and / or treatment of tumor diseases.

The present invention provides methods for treating patients suffering from familial hypercholesterolemia, including both HeFH and HoFH. The methods of the invention provide for lowering at least one lipid parameter in the patient by administering a therapeutically effective amount of an antibody or antigen-binding fragment thereof that specifically binds to ANGPTL3 in combination with a therapeutically effective amount of a statin, a first lipid lowering agent other than a statin, and a second lipid lowering agent other than a statin. The first non-statin lipid lowering agent is an agent that inhibits cholesterol uptake (e.g. ezetimibe) and the second non-statin lipid-lowering agent is an inhibitor of microsomal triglyceride transfer protein (e.g. lomitapide). The combination therapy is useful in treating hypercholesterolemia, as well as hyperlipidemia, hyperlipoproteinemia and dyslipidemia, including hypertriglyceridemia, chylomicronemia, and to prevent or treat diseases or disorders, for which abnormal lipid metabolism is a risk factor, such as cardiovascular diseases.

The application discloses an inhibitor for inhibiting KRAS phase separation to play an anti-tumor role and application, and relates to the fields of tumor molecular biology and targeted therapy.The application aims at solving the problems of limited effect, strong drug resistance and limited application range of KRAS tumor treatment methods, and the inhibitor is a statin.The KRAS protein can form a liquid condensate in cells, and the application discloses the mechanism of the KRAS protein in promoting KRAS protein processing, transportation and downstream signal activation, and further provides a technical scheme for inhibiting tumor growth and enhancing the therapeutic effect of a KRAS inhibitor by inhibiting the formation of KRAS condensates, so as to provide a new target and intervention approach for tumor treatment.

This invention relates to the field of ovarian tissue in vitro culture technology, and discloses a formulation for activating and increasing follicles and its application. The formulation consists of a PI3K / Akt / mTOR pathway activator and / or a PTEN inhibitor SF1670. The PI3K / Akt / mTOR pathway activator is a 5-15 μM statin, and the PTEN inhibitor is a 20-50 μM SF1670. Using this formulation can achieve the follicle activation and increase effect of existing technologies, contributing to the development and selection of in vitro follicle activators in clinical practice. Furthermore, the use of this formulation opens up a new technological application area for statins.

The present invention relates to a composition for preventing, alleviating or treating metabolic diseases, the composition comprising a rosuvastatin and ursodeoxycholic acid conjugate or a pharmaceutically acceptable salt thereof, in which the statin conjugates to an ursodeoxycholic acid transporter and has the effects of function inhibition, cholesterol level reduction, antilipid toxicity, body weight reduction, blood lipid reduction, fatty liver alleviation, inflammation alleviation, and kidney damage alleviation. The composition, in the form of a single formulation, has the characteristics of maintaining the therapeutic effects of rosuvastatin and ursodeoxycholic acid while reducing the side effects of existing statins, and thus can be widely used as a substitute for complex formulations in the treatment of metabolic diseases.

Provided herein are compositions, systems, and methods for treating wounds with the combination of statins and cholesterol to help prevent and reduce scar formation.

The invention relates to the technical field of biological medicine. The invention provides a PCSK9-targeted PROTAC oral drug as well as a preparation method and application thereof. The drug comprises the following structures: a PCSK9 binding peptide, an E3 ubiquitin ligase ligand, a cell penetrating peptide and a flexible linker. The medicine provided by the invention can be used for preparing products for treating lipid metabolism disorder diseases such as hypercholesteremia and atherosclerosis. In addition, the medicine disclosed by the invention can also be combined with statins to synergistically enhance the lipid-lowering curative effect.

Described herein are formulations for the controlled release of statin therapies and methods related thereto.

A preparation method of a tumor microparticle encapsulating a metabolic inhibitor includes following steps. A tumor cell is cultivated, and a statin drug is added to a culture medium after the tumor cell grows stably. Then, the tumor cell is irradiated with an ultraviolet, and then the tumor cell is incubated in a cell incubator for 22˜26 hours. After the incubation, cell supernatant is collected and the tumor microparticle encapsulating the metabolic inhibitor is obtained through a gradient centrifugation. The preparation method uses tumor cell-derived microparticles as drug delivery platforms, with a simple preparation process that preserves functions such as biosafety, biocompatibility, targeting, and intercellular communication. The preparation method discovers new uses of a statin drug, which can inhibit tumor growths with the statin drug, regulate tumors metabolism and improve a tumor microenvironment, and have a potential to enhance a chemotherapy efficacy and delay a chemotherapy resistance.

Disclosed herein are therapeutics compositions including one or more active agents, for instance a statin, cyclodextrin, or combination thereof. The compositions are useful in the treatment of tissue injuries, including wounds, as well as skin inflammation and infections.

The invention discloses an efficient composite immobilized enzyme for preparing ethyl R (-)-4-cyano-3-hydroxybutyrate and a preparation method of the efficient composite immobilized enzyme, and relates to the technical field of biological catalysis. The composite immobilized enzyme comprises an active enzyme component, a Nicoordination modified mesoporous silica-chitosan composite carrier, and a sodium alginate auxiliary embedding-glutaraldehyde covalent cross-linking composite immobilization mode. The preparation method comprises the following steps: preparing a modified carrier, preparing an active enzyme mixed solution, carrying out an embedding-crosslinking reaction, collecting and drying. The compound immobilized enzyme can catalytically prepare ethyl R (-)-4-cyano-3-hydroxybutyrate, the substrate conversion rate is still kept at an extremely high level after the compound immobilized enzyme is repeatedly used for more than 15 times, and the compound immobilized enzyme is stable in enzyme activity, low in cost and suitable for industrial green production of statin drug intermediates.

The present invention relates to a pharmaceutical combination comprising 6α-ethyl-3α, 7 a-dihydroxy-24-nor-5 β-cholan-23-ol or a pharmaceutically acceptable salt thereof and a statin and to a combination comprising 6α-ethyl-3α, 7α-dihydroxy-24-nor-5β-cholan-23-ol and ursodesoxycholic acid and the use thereof for the treatment of non-alcoholic liver steatosis and non-alcoholic steatohepatitis.

Described herein are methods for reducing or preventing blood flow in a neurovascular blood vessel of a subject. The method involves injecting a composition composed of water, one or more polycationic polyelectrolytes and anionic counterions, one or more one polyanionic polyelectrolytes and cationic counterions, and a statin, an anti-cancer agent, or a combination thereof, wherein the composition has an ion concentration that is (i) sufficient to prevent association of the polycationic polyelectrolytes and the polyanionic polyelectrolytes in water and (ii) greater than the concentration of ions in the subject. Upon introduction of the composition into a subject, a solid is produced in situ. The injectable compositions have unique distal penetration properties, which make the injectable compositions described herein very useful as embolics for neurovascular blood vessels.

Described herein are formulations for the controlled release of statin therapies and methods related thereto.

The invention belongs to the technical field of traditional Chinese medicines, and particularly relates to a traditional Chinese medicine composition for treating atherosclerosis and a preparation method thereof. The traditional Chinese medicine composition for treating atherosclerosis is prepared from the following raw materials in parts by weight: 20 to 40 parts of radix astragali seu hedysari, 7 to 10 parts of radix notoginseng, 10 to 20 parts of poria cocos, 5 to 15 parts of lotus leaves, 10 to 15 parts of raw fructus crataegi, 10 to 20 parts of radix salviae miltiorrhizae, 10 to 15 parts of radix angelicae sinensis and 2 to 10 parts of ramulus cinnamomi. The traditional Chinese medicine composition can intervene in the atherosclerosis process through multiple ways of adjusting the blood fat level, improving aorta pathological injury, inhibiting inflammatory response, increasing intestinal flora diversity and the like, and the comprehensive treatment effect of the traditional Chinese medicine composition is equivalent to that of clinical conventional medicine statins.

The present disclosure provides pharmaceutic compositions for oral delivery comprising an antisense oligonucleotide (e.g., CIVI 008) and an oral delivery agent such as 5-CNAC. In some aspects, the disclosure provides a capsule comprising a dry blend of CIVI 008 and 5-CNAC, and optionally a statin.

The present invention relates to a pharmaceutical composition comprising a combination of an FXR agonist and at least one lipid lowering agent (e.g., PPAR-alpha agonist, PPAR-delta agonist, PPAR-alpha and delta dual agonist, and / or statin). Also disclosed is use of the combination for the treatment or prevention of a FXR mediated disease or condition, such as primary biliary cirrhosis (PBC), primary sclerosing cholangitis (PSC), portal hypertension, bile acid diarrhea, NAFLD (nonalcoholic fatty liver disease), NASH (non-alcohol-induced steatohepatitis), and other chronic liver diseases. The combination of the present invention is useful for the treatment or prevention of conditions related to elevated lipid and liver enzyme levels. The present invention also relates to packs or kits including the pharmaceutical combination.

The application provides a method for improving 2-deoxy-D-ribose-5-phosphate aldolase (DERA) activity through immobilization. The method can significantly activate the aldolase activity of DERA, and is simple, mild, simple and easy to operate, and can be applied to preparation of chiral side chains of statins.

A method of treating a wound may include topically administering a statin composition including a statin selected from atorvastatin, fluvastatin, lovastatin, pitavastatin, pravastatin, rosuvastatin, simvastatin, or combination thereof. The statin composition may be administered in an ointment, powder, or liquid format. The method may also include topically administering one or more antimicrobial drugs and / or naltrexone.

The present disclosure provides pharmaceutic compositions for oral delivery comprising an antisense oligonucleotide (e.g., CIVI 008) and an oral delivery agent such as 5-CNAC. In some aspects, the disclosure provides a capsule comprising a dry blend of CIVI 008 and 5-CNAC, and optionally a statin.

This disclosure provides medicaments and methods for treating envenomation using small molecule inhibitors of secretory phospholipase A2 (sPLA2). The sPLA2 inhibitor AZD2716 and related compounds can be used as monotherapy. Alternatively, the sPLA2 inhibitor varespladib and / or methyl varespladib can be used in combination with a statin. When a subject has been envenomed (for example, by a snake bite or bee sting), the medicaments can be administered to prevent lethal effects or tissues damage cause by the venom: for example, acute kidney injury, mast cell degranulation, or cerebral edema. The medicaments may be contained in an automatic injection device or an injection pen to deliver an effective dose as soon as possible following envenomation.

Described is an antibody-drug conjugate (ADC) having the formula A-L, wherein A is an antibody or an antibody fragment and wherein L is a linker, said linker comprising: as a first payload a topoisomerase I inhibitor which is cell-permeable, e.g., a camptothecin cytotoxic molecule which is cell-permeable; as a second payload a topoisomerase I inhibitor which is not cell-permeable, e.g., a camptothecin cytotoxic molecule which is not cell-permeable; and as a as a third payload a toxin or a cytotoxin, e.g., an auristatin such as MMAE (Monomethyl auristatin E). Moreover, described is a pharmaceutical composition comprising said ADC and at least one pharmaceutically acceptable ingredient. Further, described method of treating a patient suffering from, being at risk of developing, and / or being diagnosed for a neoplastic disease.

Systems and methods are provided for over the counter statin delivery to a subject. Survey results from the subject are run against a first plurality of filters. When a filter in the first plurality of filters is fired, the subject is deemed not qualified. The survey results are also run against a second plurality of filters. When a respective filter in the second plurality is fired, the subject is provided with a corresponding warning. The method proceeds to a fulfillment process when no filter in the first plurality fires and the subject has acknowledged each warning associated with each fired filter in the second plurality. The fulfillment stores the composition order, communicates a drug facts label for the statin to the subject, and authorizes, upon subject confirmation that the label has been read, provision of the statin to the subject, the authorization including a destination associated with the subject.

The present invention relates to a pharmaceutical composition comprising a combination of an FXR agonist and at least one lipid lowering agent (e.g., PPAR-alpha agonist, PPAR-delta agonist, PPAR-alpha and delta dual agonist, and / or statin). Also disclosed is use of the combination for the treatment or prevention of a FXR mediated disease or condition, such as primary biliary cirrhosis (PBC), primary sclerosing cholangitis (PSC), portal hypertension, bile acid diarrhea, NAFLD (nonalcoholic fatty liver disease), NASH (non-alcohol-induced steatohepatitis), and other chronic liver diseases. The combination of the present invention is useful for the treatment or prevention of conditions related to elevated lipid and liver enzyme levels. The present invention also relates to packs or kits including the pharmaceutical combination.

The invention belongs to the technical field of statins, and particularly relates to a gene detection kit and system for evaluating the medication of statins, the kit comprises primers and probes for detecting the rs4149056 site of an SLCO1B1 gene, the rs2231142 site of an ABCG2 gene and the rs1057910 site of a CYP2C9 gene, the kit also comprises a PCR reaction liquid, a positive quality control product and a negative quality control product, the system comprises a PCR reaction system, a PCR amplification system and a genotyping interpretation system, the PCR reaction system is composed of the gene detection kit for evaluating the medication of statins, the kit and the detection system have the advantages of being high in sensitivity, low in cost, high in specificity, easy and convenient to operate, short in detection period and the like, and individual SLCO1B1, ABCG2 and CYP2C9 gene polymorphism can be rapidly and accurately detected.

The application belongs to the technical field of medicine, and particularly relates to the use of icariin in the preparation of lipid-lowering drugs with muscle protection. In view of the adverse reactions such as myalgia and myositis caused by the existing statins in the lipid-lowering process, the muscle protection effect of icariin in the lipid-lowering process is evaluated by constructing a high-fat cell model and a high-fat Caenorhabditis elegans model. It is found through research that icariin can significantly reduce the content of triglyceride, total cholesterol and lipid droplet accumulation in high-fat cells, reduce the content of triglyceride and lipid droplet accumulation in high-fat C. elegans, and prolong the lifespan of high-fat C. elegans. Further research shows that icariin can improve the muscle state of high-fat C. elegans while lowering lipid, and the specific performance is the enhancement of the movement ability of C. elegans and the maintenance of the structural integrity of body wall muscle fibers. The application discloses the unique advantage of icariin in the lipid-lowering process, that is, the muscle protection effect, and can solve the adverse reactions such as myalgia and myositis caused by the existing statins, and has an important clinical application prospect.

The invention belongs to the crossing field of bioengineering and pharmaceutical technology, and particularly relates to a heterologous expression technology of 2-deoxyribose-5-phosphate aldolase derived from rhodococcus ruber SD3 and optimization of aldol condensation reaction conditions of substrates acetaldehyde and chloroacetaldehyde catalyzed by the aldolase. The enzyme can catalyze a substrate to specifically synthesize a statin drug key intermediate (3R, 5S)-6-chloro-2, 4, 6-trideoxy pyranoside, the conversion rate can reach 44.45%, and a new biological catalysis approach and technical support are provided for efficient and green production of statin drugs. The rhodococcus ruber SD3 is preserved in the China Center for Type Culture Collection, and the preservation number of the rhodococcus ruber SD3 is CCTCC NO: M 2012035.

This application relates to a platform for providing compounds and implants that provide long-lasting release of therapeutics, such as statins and steroids, in biological and therapeutic applications, such as in ocular administration and / or via implantation or insertion. In some embodiments, the compounds of the application comprise a first radical (D1) and a second radical (D2) (e.g., having the formula: D1-L-D2). In certain instances, D1 is a processable group such as a radical of a steroid, L is a linker, and D2 is a drug such as a statin. While there are some controlled delivery systems for delivering an active pharmaceutical ingredient (API) to a treatment site, the systems generally contain polymer carriers that can create technical and / or regulatory challenges, such as, for example, burst release kinetics, low drug loading, and adverse inflammatory responses. The present application presents a therapeutic consisting entirely or almost entirely of API which could address such technical and regulatory challenges.

The application belongs to the field of biomedicine, and particularly relates to application of a PCSK9 inhibitor in preparation of a drug for treating hypothyroidism with hyperlipidemia. In view of the problem that statins are prone to cause early liver and kidney function damage in the process of reducing lipids in the population with hypothyroidism and hyperlipidemia, the application proves through a mouse model experiment that the PCSK9 inhibitor (alirocumab) has a better effect on reducing LDL-C and VLDL-C in the mouse model, has no influence on thyroid function, can reduce liver and kidney damage, relieve inflammation and oxidative stress, and remodel lipid spectrum. For the population with hypothyroidism and hyperlipidemia, the PCSK9 inhibitor (alirocumab) has both efficacy and safety compared with statins, and has a good clinical application prospect.