9 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 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 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.