46 results about "Binding drugs" patented technology

A multiparticulate, modified release composition for oral administration has been developed. The formulation is made by complexing a drug with an ion-exchange resin in the form of small particles, typically less than 150 microns. The present invention provides novel extended release coated ion exchange particles comprising drug-resin complexes, produced by binding the salt form of the drug, that do not require impregnating agents to insure the integrity of the extended release coat. To prepare a modified release formulation, one or more of the following types of particles are formulated into a final dosage form: (a) Immediate release particles, (b) Enteric coated particles, (c) Extended release particles, (d) Enteric coated-extended release particles; and (e) Delayed release particles. The various drug-containing particles described above can be further formulated into a number of different easy-to-swallow final dosage forms including, but not limited to, a liquid suspension, gel, chewable tablet, crushable tablet, rapidly dissolving tablet, or unit of use sachet or capsule for reconstitution

The invention describes a vitamin receptor binding drug delivery conjugate, and preparations therefor. The drug delivery conjugate consists of a vitamin receptor binding moiety, a bivalent linker (L), and a drug. The vitamin receptor binding moiety includes vitamins, and vitamin receptor binding analogs and derivatives thereof, and the drug includes analogs and derivatives thereof. The vitamin receptor binding moiety is covalently linked to the bivalent linker, and the drug, or the analog or the derivative thereof, is covalently linked to the bivalent linker, wherein the bivalent linker (L) includes components such as spacer linkers, releasable linkers, and heteroatom linkers, and combinations thereof. Methods and pharmaceutical compositions for eliminating pathogenic cell populations using the drug delivery conjugate are also described.

The invention describes a vitamin receptor binding drug delivery conjugate, and preparations therefor. The drug delivery conjugate consists of a vitamin receptor binding moiety, a bivalent linker (L), and a drug. The vitamin receptor binding moiety includes vitamins, and vitamin receptor binding analogs and derivatives thereof, and the drug includes analogs and derivatives thereof. The vitamin receptor binding moiety is covalently linked to the bivalent linker, and the drug, or the analog or the derivative thereof, is covalently linked to the bivalent linker, wherein the bivalent linker (L) includes components such as spacer linkers, releasable linkers, and heteroatom linkers, and combinations thereof. Methods and pharmaceutical compositions for eliminating pathogenic cell populations using the drug delivery conjugate are also described.

Described herein are compositions and methods for use in targeted drug delivery using cell receptor binding drug delivery conjugates containing hydrophilic spacer linkers for use in imaging, diagnosing, and / or treating diseases and disease states caused by pathogenic cell populations.

Provided are means for the direct and continuous connection of a catheter to the lumen of any tubular anatomical structure, or ductus, without medically significant leakage. A port implanted at the body surface with piping to a periductal collar allows drug or radionuclide delivery that bypasses the upstream lumen. The port allows injection, infusion, or attachment of an automatic ambulatory pump. A superparamagnetic nanoparticle carrier-bound drug, for example, can be introduced into the lumen to pass downstream until the carrier particles, with or without the drug still bound, are drawn into the lumen wall by a magnetized jacket surrounding the ductus. Such constitutes a method of drug targeting whereby a segment of a vessel or the territory supplied by a branch of that segment can be circumscribed for exposure to the drug. A jacket with side-entry connector positioned in surrounding relation to a lesion requiring treatment can itself be magnetized.

The invention discloses a novel conjugate composed of a hydrophilic polymer and resveratrol, a pharmaceutical composition including the conjugate, their preparation methods and applications in the preparation of drugs for treating tumor, diabetes and cardio cerebrovascular disease, wherein the hydrophilic polymer is selected from the group consisting of polyethylene glycol, polyglutamic acid, polyaspartic acid, polypropylene glycol, polyvinyl alcohol, polypropylene morpholine, polyethylene glycol-amino acid oligopeptide and their copolymer. Through modification of the hydrophilic polymer, a bound drug can be protected, stability and water solubility of the conjugate are raised, and active period of the conjugate in organisms is prolonged.

The invention describes a vitamin receptor binding drug delivery conjugate, and preparations therefor. The drug delivery conjugate consists of a vitamin receptor binding moiety, a bivalent linker (L), and a drug. The vitamin receptor binding moiety is a vitamin, or a vitamin receptor binding analog or a derivative thereof, and the drug includes analogs or derivatives thereof. The vitamin receptor binding moiety is covalently linked to the bivalent linker, and the drug, or the analog or the derivative thereof, is covalently linked to the bivalent linker, wherein the bivalent linker (L) comprises one or more spacer linkers, releasable linkers, and heteroatom linkers. Methods and pharmaceutical compositions for eliminating pathogenic cell populations using the drug delivery conjugate are also described.

Described herein are compositions and methods for use in targeted drug delivery using cell receptor binding drug delivery conjugates containing hydrophilic spacer linkers for use in imaging, diagnosing, and / or treating diseases and disease states caused by pathogenic cell populations.

Linkers for binding drugs to cell binding agents are modified to hydrophilic linkers by incorporating a polyethylene glycol spacer. The potency or the efficacy of the cell-binding agent-drug conjugates is surprisingly enhanced several folds in a variety of cancer cell types, including those expressing a low number of antigens on the cell surface or cancer cells that are resistant to treatment. A method for preparing maytansinoids bearing a thioether moiety and a reactive group which allows the maytansinoid to be linked to a cell-binding agent in essentially a single step is also provided.

The invention describes a vitamin receptor binding drug delivery conjugate, and preparations therefor. The drug delivery conjugate consists of a vitamin receptor binding moiety, a bivalent linker (L), and a drug. The vitamin receptor binding moiety is a vitamin, or a vitamin receptor binding analog or a derivative thereof, and the drug includes analogs or derivatives thereof. The vitamin receptor binding moiety is covalently linked to the bivalent linker, and the drug, or the analog or the derivative thereof, is covalently linked to the bivalent linker, wherein the bivalent linker (L) comprises one or more spacer linkers, releasable linkers, and heteroatom linkers. Methods and pharmaceutical compositions for eliminating pathogenic cell populations using the drug delivery conjugate are also described.

A method of treatment of neurodegenerative diseases using neuronal cell transplants is provided. The growth, survival and integration of the transplanted neuronal cells is enhanced by a method of culturing the neuronal cells with drugs having an affinity for immunophilins. Immunophilin binding drugs are optionally administered to the patient during transplantation and / or post-operatively. Neurotrophic factors can also be administered to the neuronal cells in vitro, or to the patient during the transplantation procedure and / or post-operatively.

The invention discloses a drug repositioning method for a COVID-19 treatment drug and application thereof. The method comprises the following steps: s1, collecting a COVID-19 diagnosis and treatment scheme report, and constructing a treatment scheme data set of known COVID-19 diseases; s2, expanding drug-disease-target point relationship data; s3, standardizing entity naming and constructing a network; s4, performing network representation and association degree calculation; and s5, sorting the potential therapeutic drugs. According to the method, the drug disease similarity and the similaritybetween the drug targets are considered, and meanwhile, the drug network structure similarity and the target network structure similarity are combined, so that the prediction accuracy of the drug target interaction relationship is improved. Potential drugs for treating COVID-19 diseases are mined on the basis of the constructed COVID-19 data set, and the potential drugs contributing to COVID-19 treatment in the drugs on the market can be effectively found.

Methods are disclosed for preventing toxic drug-drug interactions during combination cancer therapy with a drug that is an anti-ErbB3 agent, such as an anti-ErbB3 antibody, together with a drug that is a tyrosine kinase inhibitor and / or a drug that binds to alpha-1 acid glycoprotein (e.g., erlotinib). Health care practitioners obtaining any one of the drugs are warned that when co-administering the drug that is an anti-ErbB3 agent with either or both of a drug that is a tyrosine kinase inhibitor and a drug that binds to alpha-1 acid glycoprotein, at least one of the co-administered drugs should be administered using a reduced dosage to prevent toxicity. In a reduced dosage, the amount of drug administered per unit time is reduced as compared to a dose that would be administered if the drug was administered as monotherapy. The reduced dosage can be, for example, a reduced drug dose or a reduced drug dosing frequency, or both. Compositions useful in practicing the disclosed methods are also provided.

The site-specific expression of selectins on endothelial cells of blood vessels during angiogenesis provides an opportunity to target anti-cancer drugs to the vascular endothelium to extend the range of the therapeutic effect. This invention describes an innovative drug targeting strategy for the selective delivery of the anticancer drugs to endothelial cells by means of polymer-drug conjugates modified with a carbohydrate ligand for the vascular selectins. A model chemotherapeutic drug, doxorubicin, and the E-selectin ligand, sLex, are attached to a biocompatible polymer (HPMA). The selective binding, cellular uptake, intracellular fate, and cell cytotoxicity of the polymer-bound drug are investigated in human endothelial cells.

The present application relates to novel binder drug conjugates (ADCs), to active metabolites of these ADCs, to processes for preparing these ADCs, to the use of these ADCs for the treatment and / or prophylaxis of diseases and to the use of these ADCs for preparing medicaments for treatment and / or prophylaxis of diseases, in particular hyperproliferative and / or angiogenic disorders such as, for example, cancer diseases. Such treatments can be effected as monotherapy or else in combination with other medicaments or further therapeutic measures.

The invention discloses a drug target interaction relationship prediction method based on collaborative matrix decomposition, which considers drug attribute similarity and target attribute similarity,and combines drug topological structure similarity and target topological structure similarity to improve drug target interaction relationship prediction accuracy. The method comprises the followingsteps of: acquiring drug attribute similarity and target attribute similarity data and drug target interaction relationship data; constructing a drug attribute feature similarity matrix, a target point attribute feature similarity matrix, a drug topological similarity matrix and a target point topological similarity matrix; performing graph regularization-based collaborative matrix decomposition on the drug target incidence matrix, and integrating attribute feature similarity and topological structure similarity information of the drug and the target to obtain a final target function; and performing iterative updating by using a Newton method to obtain the feature representation of the drug and the target, reconstructing a drug-target interaction relationship matrix, and predicting the drug-target interaction relationship.

The invention discloses a method for predicting drug-target affinity based on protein multi-source feature fusion, which comprises the following steps: firstly, constructing a PPI network and an SSN network, extracting protein features from the networks, and then collecting protein features such as subcellular positions, sequence codes, functional sites and structural domains for protein characterization; and fusing multi-source features by using a variational graph auto-encoder, and finally, inputting the multi-source features into a full-connection layer in combination with drug branches to carry out affinity prediction. According to the invention, a PPI network and an SSN network are constructed, so that biological priori knowledge between a target protein and other proteins is learned in addition to focusing on the characteristics of the target protein; according to the method, the protein characteristics are extracted and fused from the aspects of protein interaction, sequence similarity and protein subcellular positions for the first time, so that the drug-target affinity is predicted, and the prediction accuracy is improved; in addition, the characteristic source of the protein does not comprise a protein structure, so that the dependence on the protein structure is abandoned.

The present invention proposes a design to incorporate drug(s) in the hard capsule shells (body and cap) composition. Drug(s) in the cap and body of the capsule shell may be the same or may be different. Other drug(s) in the form of granules, beads etc. can be filled into the capsules as a core material. The drug(s) in the capsule core material may be the same as in the shell-composition or may be different. Thus, the same capsule may contain different drug(s) as the core material and in the shell. The key advantages of incorporation of drug in the capsule shell compositions are to minimize drug-drug interaction and to obtain a desired rate of release of the drug(s), mainly for potent ones. The concept can be applied to the hard gelatin, and hard non-gelatin capsules.

A method for producing an antibody-drug conjugate composition, comprising: (i) a step of reacting an antibody with a reducing agent in a buffer to reduce interchain disulfides, and (ii) a step of reacting drug linker intermediates with the antibody having thiol groups obtained in the step (i), wherein the reaction temperature in the step (i) is −10° C. to 10° C., and the average number of bound drugs in the produced antibody-drug conjugate composition is 3.5 to 4.5, and the content of antibody-drug conjugates in which four drug linkers are bound to heavy-light interchain thiols, in the produced antibody-drug conjugate composition is 50% or more; and an antibody-drug conjugate composition, wherein the content of antibody-drug conjugates wherein the average number of bound drugs is 3.5 to 4.5, and the content of antibody-drug conjugates in which four drug linkers are bound to heavy-light interchain thiols, is 50% or more.

The site-specific expression of selectins on endothelial cells of blood vessels during angiogenesis provides an opportunity to target anti-cancer drugs to the vascular endothelium to extend the range of the therapeutic effect. This invention describes an innovative drug targeting strategy for the selective delivery of the anticancer drugs to endothelial cells by means of polymer-drug conjugates modified with a carbohydrate ligand for the vascular selectins. A model chemotherapeutic drug, doxorubicin, and the E-selectin ligand, sLex, are attached to a biocompatible polymer (HPMA). The selective binding, cellular uptake, intracellular fate, and cell cytotoxicity of the polymer-bound drug are investigated in human endothelial cells.

The present invention proposes a design to incorporate drug(s) in the hard capsule shells (body and cap) composition. Drug(s) in the cap and body of the capsule shell may be the same or may be different. Other drug(s) in the form of granules, beads etc. can be filled into the capsules as a core material. The drug(s) in the capsule core material may be the same as in the shell-composition or may be different. Thus, the same capsule may contain different drug(s) as the core material and in the shell. The key advantages of incorporation of drug in the capsule shell compositions are to minimize drug-drug interaction and to obtain a desired rate of release of the drug(s), mainly for potent ones. The concept can be applied to the hard gelatin, and hard non-gelatin capsules.

The present invention provides compounds of Formula (I), compositions comprising an effective amount of a compound of Formula (I), optionally with chemotherapeutic drugs such as a tubulin-binding drug, and methods of their use for reducing the toxicity of cytotoxic agents, treating or preventing cancer or a neuropathic disorder, inducing a chemoprotective phase II enzyme, DNA, or protein synthesis, enhancing the immune system, treating inflammation, improving and enhancing general health or well-being, and methods for making compounds of Formula (I).

A method for producing an antibody-drug conjugate composition, comprising: (i) a step of reacting an antibody with a reducing agent in a buffer to reduce interchain disulfides, and (ii) a step of reacting drug linker intermediates with the antibody having thiol groups obtained in the step (i), wherein the reaction temperature in the step (i) is −10° C. to 10° C., and the average number of bound drugs in the produced antibody-drug conjugate composition is 3.5 to 4.5, and the content of antibody-drug conjugates in which four drug linkers are bound to heavy-light interchain thiols, in the produced antibody-drug conjugate composition is 50% or more; and an antibody-drug conjugate composition, wherein the content of antibody-drug conjugates wherein the average number of bound drugs is 3.5 to 4.5, and the content of antibody-drug conjugates in which four drug linkers are bound to heavy-light interchain thiols, is 50% or more.

The invention belongs to the technical field of hydrogel preparation, and specifically discloses a preparation method of a hydrogel for targeted treatment of cancer cells. The method comprises the following steps: mixing acrylic acid and a Fe3O4 magnetic nanoparticle in mixing equipment according to a molar ratio of 1:1, then carrying out a reaction in a reactor at 35-42 DEG C for 10-15 min for combination of acrylic acid with the Fe3O4 magnetic nanoparticle to obtain a composite hydrogel, and finally wrapping the anticancer drug Adriamycin in the composite hydrogel obtained in step S2. The magnetic nanoparticle is used for a drug carrier and disease diagnosis and treatment, acrylic acid and the Fe3O4 magnetic nanoparticle are combined to form the composite hydrogel, and the anticancer drug Adriamycin is wrapped in the composite hydrogel. The hydrogel can be quickly released to achieve the role of targeted treatment of cancer cells. The nano-Fe3O4 magnetic material as a targeted drug carrier can bind drug molecules on the one hand and protect the drug molecules on the other hand.

The invention discloses a fluorescent probe for screening drugs acting on a ryanodine receptor. The structural formula of the probe is shown as a formula (I) which is described in the specification. The fluorescent probe for screening the drug acting on the ryanodine receptor can directly and specifically bind to a ryanodine receptor existing in a cell system of an insect, and can be replaced by other drugs binding to the ryanodine receptor of the insect, so the fluorescent probe can be used for screening drugs interacting with the ryanodine receptor of the insect.

Disclosed is a method for detection of ligand-cell membrane protein binding by solid state NMR spectroscopy. The method starts by forming a lipid bilayer inside nanopores of an anodic aluminum oxide (AAO) substrate, the lipid bilayer containing a membrane protein sample. The AAO substrate is treated with multiple candidate ligands having potential binding affinity for the membrane protein. Solid-state NMR analysis is performed on the treated AAO / lipid preparation so as to generate an NMR spectrum for the treated membrane protein. The solid-state NMR spectrum of the treated membrane protein is compared with the spectrum of the same preparation of membrane protein in the absence of the ligands. It is then determined whether the solid-state NMR spectrum of the treated membrane protein has shifted from the NMR spectrum of the untreated membrane protein, a shift being indicative of protein binding by the candidate ligand.

The invention relates to the technical field of artificial intelligence, and discloses a drug recommendation method based on machine learning, which comprises the following steps: constructing sub-graph data of drug molecules by processing drug molecular structures; the sub-graph data of the drug molecular structure and an electronic medical record of a patient are input into a pre-trained drug recommendation model for prediction, at least one recommended drug is obtained, and the drug recommendation model is used for extracting characterization vectors of drug molecules according to the sub-graph data of the drug molecular structure, outputting at least one recommended drug in combination with drug properties and the electronic medical record of the patient; and filtering the at least one recommended drug by using a mutual constraint relationship among different drugs to generate a drug recommendation result. according to the method, the molecular structure of the medicine can be considered, medicine recommendation is carried out from the medicine function, and a more accurate medicine recommendation result is provided.

The invention provides methods of identifying drug targets in dopaminergic and / or noradrenergic neurons and to the drug targets identified by such methods. This invention also provides a method of screening for agents that modulate dopaminergic neurons and / or noradrenergic neuron activity, function and / or drug target expression, and agents that bind drug targets and to kits for use in the methods described herein.

Disclosed is a method for detection of ligand-cell membrane protein binding by solid state NMR spectroscopy. The method starts by forming a lipid bilayer inside nanopores of an anodic aluminum oxide (AAO) substrate, the lipid bilayer containing a membrane protein sample. The AAO substrate is treated with multiple candidate ligands having potential binding affinity for the membrane protein. Solid-state NMR analysis is performed on the treated AAO / lipid preparation so as to generate an NMR spectrum for the treated membrane protein. The solid-state NMR spectrum of the treated membrane protein is compared with the spectrum of the same preparation of membrane protein in the absence of the ligands. It is then determined whether the solid-state NMR spectrum of the treated membrane protein has shifted from the NMR spectrum of the untreated membrane protein, a shift being indicative of protein binding by the candidate ligand.

The present invention relates to compositions comprising an effective amount of a Panaxytriol Compound and a tubulin-binding drug, methods for treating or preventing cancer or a neurotrophic disorder comprising administering to a subject in need thereof an effective amount of a Panaxytriol Compound and a tubulin-binding drug, and methods for making a Panaxytriol Compound.