13 results about "Bound drug" patented technology

The invention belongs to the technical field of biological medicines, discloses a ganoderma lucidum oligopeptide for inhibiting tumor cell growth and a preparation method and application thereof, and aims to overcome the technical defects of unknown active ingredients, low yield, poor purity and high toxicity of the existing ganoderma lucidum oligopeptide. The sequence of the ganoderma lucidum oligopeptide is Trp-Gly-Ala-Pro-Arg, the molecular weight is 623.7 Da, the isoelectric point is 8.92, and the ganoderma lucidum oligopeptide plays a tumor inhibition role by reducing a PI3K / Akt / mTOR signal channel in a targeted manner. The preparation method comprises the following steps: carrying out superfine grinding on a lucid ganoderma raw material, carrying out composite enzymatic hydrolysis by using papain, alkaline protease and flavourzyme (5: 3: 2), and carrying out ultrafiltration, gel chromatography and RP-HPLC (Reverse Phase-High Performance Liquid Chromatography) purification, so that the yield is 1.16-1.20%, and the purity is greater than or equal to 98%. The ICs of the peptide to six tumor cells such as lung cancer A549 are 0.8-1.4 [mu] mol / L, and the ICs of the peptide to normal cells are ICgt; the therapeutic index is greater than or equal to 15.4; the cells PPappgt of Caco-2 are subjected to cell culture; 1 * 10 cm / s, the plasma protein binding rate is 65%-68%, LDgt; the density is 500 mg / kg. The compound can be prepared into dosage forms such as injections and the like, and the tumor inhibition rate reaches 85% when the compound is combined with cis-platinum, and CI is equal to 0.65. The process is stable, and the product is high in activity, safe, suitable for tumor treatment and adjuvant therapy and good in industrialization prospect.

The application discloses a method for determining the bismuth plasma protein binding rate of bismuth potassium citrate, and is characterized in that the method comprises plasma sample pretreatment and sample determination. The determination method can solve the stability problem of bismuth potassium citrate in plasma, can make protein binding more sufficient, can effectively promote the dissociation of bismuth and plasma protein, can make the detected protein binding rate closer to the real value, has great significance for guiding clinical medication, is simple and easy to operate, can realize rapid detection, and has low dependence on instruments.

The present invention provides a fungal drug carrier comprising an avirulent fungal pathogen cell, for example a Cryptococcus neoformans cell, linked to one or more surface-bound drug-loaded nanoparticles, and methods of making the fungal drug carrier. The invention provides methods of using the fungal drug carrier to deliver a drug to the central nervous system of a patient, wherein the fungal drug carrier is phagocytosed by an immune cell of a patient, transported across the blood-brain barrier, and vomocytosed to allow drug release from the surface-bound nanoparticle into the central nervous system of the patient. The methods involve treating a central nervous system in a patient comprising administering to the patient a pharmaceutical composition comprising a fungal drug carrier.

The application discloses a DNA binding small molecule high-throughput screening and characterization method, adopts a small molecule binding agent to program a toehold-mediated strand displacement (TMSD); performs one-stop comprehensive characterization of the interaction between the small molecule binding agent and double-stranded DNA, including dissociation constant, binding site size, thermodynamic parameters and sequence selectivity; performs high-throughput screening (HTS) identification of the small molecule binding agent by using a series of induced nucleic acid displacement BIND reaction system; and combines experimental measurement and computer simulation, and it is shown that the small molecule double-stranded DNA binding agent can be used in the reaction path of programming toehold-mediated strand displacement (TMSD), so that the molecular tool of comprehensive thermodynamic characterization can be performed by using the binding agent induced nucleic acid displacement (BIND) technology, and the high-throughput screening (HTS) of the small molecule double-stranded DNA binding agent can be performed without any special equipment, the application is widely used as a one-stop HTS and comprehensive characterization platform, so as to accelerate the pace of discovering novel small molecule double-stranded DNA binding drugs / tracers.

An ultrasound system for use in unbinding an active agent from a plasma protein in a target site in a subject includes a transducer configured to generate acoustic pressure waves and a controller coupled to the transducer. The controller is programmed to control the transducer to produce a plurality of pulsed acoustic pressure waves in the target site of the patient. The plurality of pulsed acoustic pressure waves disrupt a plasma protein binding between the active agent and the plasma protein within the target site. The disruption of the plasma protein binding causes an increase in an amount of unbound active agent in the target site.

The present invention relates to modular linker compounds for target-binding drug conjugates (TBDCs) and in particular to modular linker compounds for antibody-drug-conjugates (ADCs). The modular linker compounds comprise solubility enhancing groups and self-immolative spacers. The invention further relates to methods of synthesizing the modular linker compound, to target-binding drug conjugates comprising the modular linker compound of the invention as well as to pharmaceutical compositions comprising target-binding drug conjugates compound of the invention. Embodiments of the invention have been particularly developed as target-binding drug conjugates for use in the treatment of cancer and will be described hereinafter with reference to this application. However, it will be appreciated that the invention is not limited to this particular field of use.

The invention provides a method for rapidly and accurately detecting the plasma protein binding rate of siRNA (small interfering Ribonucleic Acid) drugs in human bodies and experimental animals, which is used for detecting the plasma protein binding rate by adopting the change of electrophoresis mobility and comprises the following steps: a, preparing a drug stock solution; b, preparing a sample; c, electrophoresis; d, dyeing; e, gel imaging; and f, data analysis. The binding rate measured by the method is more accurate, and the error is smaller; in the prior art, the strip is clear, and under general conditions, due to the existence of plasma, when a high-concentration sample is applied by using a page adhesive, a serious trailing phenomenon occurs in the strip, so that the subsequent calculation is influenced. According to the invention, after a dilution process before sample loading is added, a high-concentration sample can also run out of a clear strip, so that subsequent calculation is facilitated; the repeatability is good.

Disclosed herein are systems and methods for releasing controlled drug doses to cells within fluidic channels. In certain aspects, stimuli such are selectively provided to drug-containing substrates or surface-bound drug libraries to release one or more drugs in time, location, and dose-specific manners.

The present invention relates to modular linker compounds for target binding drug conjugates (TBDCs), and in particular to modular linker compounds for antibody-drug conjugates (ADCs). The modular linker compounds comprise a solubilizing group and a self-immolative spacer. The present invention further relates to methods of synthesizing the modular linker compounds, to target binding drug conjugates comprising the modular linker compounds of the present invention, and to pharmaceutical compositions comprising the target binding drug conjugate compounds of the present invention. Embodiments of the present invention are specifically developed for target binding drug conjugates for use in cancer therapy, and will be described hereinafter with reference to the present application. However, it will be appreciated that the present invention is not limited to this particular field of use.

The present invention relates to a medical implant comprising in its interior a device for electrically controllable ad- and desorption of molecules, said device comprising (a) two electrodes comprising a conductive surface, (b) a stationary phase between said two electrodes, wherein said stationary phase is not in direct contact with said electrodes, (c) a controller functionally associated with a power supply configured for applying and changing a voltage between said electrodes, wherein changing the voltage between said electrodes changes the affinity of molecules so as to adsorb said molecules to said stationary phase or desorb molecules from said stationary phase when said molecules are adsorbed to said stationary phase, and the use of said medical implant in the treatment of a medical condition.

The present application relates to the technical field of mass spectrum imaging analysis, and more particularly to a mass spectrum imaging analysis method for drugs in a tissue sample, obtaining a pretreated tissue slice and collecting a tissue optical image, determining a tissue effective area and generating scanning pixel points; forming a scanning collection locking event based on a displacement table to position reply, mass spectrum collection trigger reply and spectrum generation reply, establishing a scanning pixel event table; constructing a partition time drift field with overlapping boundary bands through spatial reference point re-measurement, correcting scanning pixel point coordinates; re-binding drug ion signal intensity under the constraint of the tissue effective area according to mapping confidence, generating a multi-layer traceable drug ion intensity spatial matrix and a drug distribution map, and improving spatial mapping accuracy and result traceability.

The present invention relates to a pharmaceutical combination comprising: (C) an anti-LY75 antibody, or an antigen-binding portion thereof, wherein the antibody or antigen-binding portion thereof comprises: (c) a variable heavy chain region comprising: (iv) a first vhCDR comprising SEQ ID NO: 5; (v) a second vhCDR comprising SEQ ID NO: 6, and (vi) a third vhCDR comprising SEQ ID NO: 7; and (d) a variable light chain region comprising: (iv) a first vlCDR comprising SEQ ID NO: 8; (v) a second vlCDR comprising SEQ ID NO: 9, and (vi) a third vlCDR comprising SEQ ID NO: 10; wherein the anti-LY75 antibody or antigen-binding portion thereof further comprises a covalently bound drug, wherein the drug is DM4 or DM1; and (D) Venetoclax a pharmaceutically acceptable salt thereof, for use in the treatment of diffuse large B-cell lymphoma (DLBCL) or non-Hodgkin lymphoma in patients.