27 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.

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.

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.

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.

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 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.

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.

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.

A composition including an amphiphilic compound capable of self-assembling into liquid crystalline particles and a statin for systemic administration via oral mucosa. A method of lowering blood cholesterol levels in a subject comprising administering the self-assembling liquid crystalline particles and statin via oral mucosa. Preferred dosage forms result in prolonged release of the statin.

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

Provided herein are functionalized oretastatins, e.g., compounds of Formula (I) and pharmaceutical compositions thereof. Also provided herein are methods of their use in treating, preventing, or ameliorating one or more symptoms of a proliferative disease.

The present invention relates to a composition for cancer prevention, comprising a statin-based drug as an active ingredient, and disclosed is that a statin drug known for hyperlipidemia treatment may effectively prevent cancer progression. More specifically, a novel use of rosuvastatin is provided so as to enable providing a composition for multiple myeloma (MM) prevention for inhibiting progression from monoclonal gammopathy of undetermined significance (MGUS) to MM. In addition, the composition may exhibit a greater tumor growth inhibition effect when bortezomib and rosuvastatin are co-administered compared to when each medicine is administered alone.

The invention relates to the technical field of biological medicine. The invention provides a PCSK9-targeted PROTAC medicine as well as a preparation method and application thereof. The medicine 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.

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 invention provides a combination of a 5HT3-antagonist and / or a NK-1 antagonist with 6-propylamino-4,5,6,7-tetrahydro-1,3-benzothiazole-2-amine and with fluoxetine or a pharmaceutically acceptable salt or solvate thereof, zonisamide or a pharmaceutically acceptable salt or solvate thereof, or a statin or a pharmaceutically acceptable salt or solvate thereof, for use for treating a protein misfolding neurodegenerative disease such as Alzheimer's disease, Lewy body disease, Parkinson's disease, or Huntington's disease.

The invention provides a preparation method of an inhalable immune sensitization drug compound suitable for lung cancer immunotherapy and a drug compound prepared by using the method. The drug compound comprises a MoS2-statin nano platform and a liposome layer, wherein the MoS2-statin nano platform is formed by loading statins on MoS2 nanosheets, and the nano platform is coated with the liposome layer. According to the platform, the combination of MoS2 nanosheets and statins is precisely regulated and controlled, and further lipidosome wrapping is carried out, so that the particle size of nanoparticles is optimized to be 100 nm, the requirement of inhalable drug delivery is met, the drug can be efficiently deposited on lung tumor tissue, and the whole body exposure risk is reduced. Meanwhile, statins are used for inducing lung cancer cell ferroptosis and releasing tumor antigens to activate an immune system, good drug loading and biocompatibility of the MoS2 nanosheets are combined, the tumor immune microenvironment is cooperatively adjusted, the treatment effect of the immune checkpoint inhibitor is enhanced, the difficulty of immune drug resistance is broken through, and the application prospect is broad. And an innovative treatment means with strong targeting property, obvious curative effect and small side effect is provided for lung cancer patients.

The present invention provides methods for treating a PCSK9-mediated disease or a PCSK9-mediated condition. Specifically, the invention relates to methods comprising the administration of a proprotein convertase subtilisin / kexin type 9 (PCSK9) antibody or antigen binding protein, in the absence of a statin, to a subject in need thereof.