12 results about "Toxin Conjugates" patented technology

An amatoxin-linker construct contains an amatoxin according to formula (I)wherein R1 and R2 are each —OH, R3 is NH2, or a linker which carries a reactive group Y for linking said amatoxin to a target-binding moiety, R4 is H or a linker which carries a reactive group Y for linking said amatoxin to a target-binding moiety, R5 is absent or ═O, and wherein R3 and R4 cannot be the same. The amatoxin-linker construct is used in the manufacture of a binding moiety-toxin conjugate for the treatment of a solid tumor, and a respective binding moiety-toxin conjugate can be used for the treatment of a solid tumor.

This invention relates to bicyclic toxin conjugates or bicyclic tumor-targeting immune agonists that are specific to Nectin-4, or pharmaceutically acceptable salts thereof or pharmaceutical compositions thereof, and their uses.

The invention discloses a preparation method of a CD44v6-VEGFR2 (vascular endothelial growth factor receptor 2) double antibody-toxin conjugate, which is characterized in that an anti-human CD44v6 monoclonal antibody and a VEGFR2 monoclonal antibody are coupled with cytotoxic load GGFG-Dxd through a linker to prepare the bispecific antibody drug conjugate capable of simultaneously targeting CD44v6 and VEGFR2. The invention also discloses application of the CD44v6-VEGFR2 double antibody-toxin conjugate prepared by the preparation method in targeted therapy of CD44v6 positive tumor cells and preparation of drugs for targeted therapy of the CD44v6 positive tumor cells. The invention designs, successfully expresses and couples to obtain the double-antibody ADC taking Dxd as toxin (DAR8), the double-antibody ADC can be combined with CD44v6 and VEGFR2 at the same time, and the targeting property is greatly enhanced, so that the accumulation amount of the double-antibody ADC in tumors is greatly increased, the off-target effect is reduced, and the double-antibody ADC has higher safety.

The bispecific antibody targeting two different epitopes or targets is coupled with camptothecin drugs to form a bispecific antibody-toxin conjugate with stable mass and good uniformity, and the toxin-to-antibody ratio (DAR) is 6.0-8.0. The antibody-toxin conjugate has the structure shown in general formula I, wherein Ab refers to the bispecific antibody targeting two different epitopes or targets and coupled with the linker-camptothecin drugs. Meanwhile, the application also discloses a preparation and purification method of the ADC drug, and application in tumor treatment. The application also relates to the linker-drug compound which can be coupled with Ab to form the antibody-toxin conjugate.

The present invention relates to an amatoxin-linker construct comprising an amatoxin according to formula (I) wherein: R1 and R2 are each —OH, R3 is NH2, or a linker which carries a reactive group Y for linking said amatoxin to a target-binding moiety, R4 is H or a linker which carries a reactive group Y for linking said amatoxin to a target-binding moiety, R5 is absent or ═O, wherein R3 and R4 cannot be the same, for use in the manufacture of a binding moiety-toxin conjugate for the treatment of a solid tumor, and a respective binding moiety-toxin conjugate for the treatment of a solid tumor.

The present invention relates to a Bicycle toxin conjugate or a Bicycle tumor-targeting immune agonist specific for Nectin-4, or pharmaceutically acceptable salts thereof, or pharmaceutical compositions thereof, and their uses.

The present invention relates to a Bicycle toxin conjugate BT5528, or pharmaceutically acceptable salts thereof, or pharmaceutical compositions thereof, and uses thereof.

The present invention relates to a saponin derivative based on a saponin, the saponin derivative comprising a triterpenoid aglycone and a first sugar chain and / or a second sugar chain, and comprising: an aglycone core structure comprising an aldehyde group which has been derivatized; and / or a first sugar chain, wherein the first sugar chain comprises a carboxyl group which has been derivatized; and / or a second sugar chain, wherein the second sugar chain comprises at least one acetoxy group which has been derivatized. The present invention further relates to a first pharmaceutical composition comprising the saponin derivative of the present invention. Furthermore, the present invention relates to a pharmaceutical combination comprising the first pharmaceutical composition of the present invention and a second pharmaceutical composition comprising any one or more of an antibody-toxin conjugate, a receptor-ligand-toxin conjugate, an antibody-drug conjugate, a receptor-ligand-drug conjugate, an antibody-oligonucleotide conjugate, or a receptor-ligand-oligonucleotide conjugate. The present invention further relates to the first pharmaceutical composition or the pharmaceutical combination of the present invention for use as a medicament or for use in the treatment or prevention of cancer, an infectious disease, a viral infection, hypercholesterolemia, primary hyperoxaluria, hemophilia A, hemophilia B, alpha-1 antitrypsin-related liver disease, acute hepatic porphyria, transthyretin-mediated amyloidosis, or an autoimmune disease. Furthermore, the present invention relates to an in vitro or ex vivo method for transferring a molecule from the outside of a cell to the inside of said cell, comprising contacting said cell with said molecule and the saponin derivative of the present invention.

A bispecific antibody simultaneously targeting two different epitopes or targets is coupled with a camptothecin drug to form a bispecific antibody-toxin conjugate that is stable in treatment and excellent in uniformity, and a drug-to-antibody ratio (DAR) thereof is 6.0-8.0. The antibody-toxin conjugate has a structure as represented by general formula (I), wherein Ab represents the bispecific antibody simultaneously targeting two different epitopes or targets, which is coupled with a linker-camptothecin drug. In addition, the present invention further relates to a preparation and purification method for the antibody-toxin conjugate, and an application thereof in tumor treatment. Furthermore, the present invention further relates to a linker-drug compound capable of being coupled with Ab to form the antibody-toxin conjugate.

The present invention relates to a Bicycle toxin conjugate BT8009, or pharmaceutically acceptable salts thereof, or pharmaceutical compositions thereof, for use in combination with an agent that inhibits the PD-1 / PD-L1 pathway in methods of therapy.

An antibody targeting human Claudin 18.2 is coupled with a camptothecin drug to form an antibody-toxin conjugate which is stable in quality and excellent in uniformity, and the toxin-antibody ratio (DAR) of the antibody-toxin conjugate is 6.0-8.0. The antibody-toxin conjugate has a structure as shown in a general formula I, and Ab refers to an antibody targeting Claudin 18.2 and is coupled with a linker-camptothecin medicine. Meanwhile, the invention also discloses a preparation method and a purification method of the ADC drug, and an application of the ADC drug in tumor treatment. The present invention also relates to linker-drug compounds that can be conjugated to Ab to form antibody-toxin conjugates. # imgabs0 #

The present application provides methods of treating a tumor or cancer in a subject using an antibody-toxin conjugate having a structure shown in Formula I, wherein Ab is conjugated to a camptothecin derivative via a linker. Ab refers to a bispecific antibody that targets two different epitopes or targets simultaneously. In one embodiment, Ab is a bispecific antibody having binding affinity for EGFR and HER3.