Patent classifications
A61K47/6889
DIELS-ALDER CONJUGATION METHODS
Described herein are protein-payload conjugates and compositions thereof that are useful, for example, for target-specific delivery of therapeutic and/or imaging agent moieties. In certain embodiments, provided are specific and efficient methods for producing protein-payload constructs (e.g., antibody-drug conjugates) utilizing a combination of transglutaminase and Diels-Alder techniques. Antibody-drug conjugates and compositions which comprise glutaminyl-modified antibodies, Diels-Alder adducts, and reactive payloads and are provided.
TRANSGLUTAMINASE-MEDIATED CONJUGATION
The present disclosure provides for antibody-oligonucleotide conjugates, methods of preparation thereof, and methods of use thereof. Also provided are related compounds, compositions and kits.
A Camptothecin Drug and Its Antibody Conjugate Thereof
The present application discloses a camptothecin drug and its antibody conjugate. Based on a comprehensive understanding of ADC drugs, the inventor designed a series of active anti-tumor exatecan-derivatives. The designed anti-tumor molecular compound showed good anti-tumor activity in the experiment.
ANTIBODY-IMMUNE AGONIST CONJUGATE AND APPLICATIONS THEREOF
The present disclosure relates to a linking unit molecule for targeting molecule-drug conjugate, and the corresponding conjugate, the preparation and use thereof, and in particular relates to an antibody-immune agonist conjugate (AIAC) as a novel type of cancer therapy.
Hydrophilic antibody-drug conjugates
Hydrophilic Linkers, Drug-Linker compounds, Drug-Ligand Conjugate compounds and Ligand-Linkers and methods of making and using the same are provided.
Antibody drug conjugate for anti-inflammatory applications
Antibody drug conjugates (ADCs) comprising an antibody conjugated to an anti-inflammatory therapeutic agent via a phosphate-based linker with tunable extracellular and intracellular stability are described.
B-LYMPHOCYTE SPECIFIC AMATOXIN ANTIBODY CONJUGATES
The present application relates to conjugates comprising an amatoxin, a target-binding moiety wherein the target is CD37, i.e., a CD37-binding moiety, and optionally a linker linking said amatoxin and said CD37-binding moiety. The invention further relates to the synthesis of said conjugates. In addition, the invention relates to a pharmaceutical composition comprising such conjugate for use in the treatment of immune cell-, particularly B-cell and/or lymphoma associated diseases and/or malignancies.
Antibody-conjugates with improved therapeutic index for targeting CD30 tumours and method for improving therapeutic index of antibody-conjugates
The present invention concerns novel and improved antibody-conjugates for targeting CD30. The inventors found that when antibody-conjugates were prepared using a specific mode of conjugation, they exhibit an improved therapeutic index. The mode of conjugation comprises a first step (i) of contacting a glycoprotein comprising 1-4 core N-acetylglucosamine moieties with a compound of the formula S(F.sup.1).sub.x-P in the presence of a catalyst, wherein S(F.sup.1).sub.x is a sugar derivative comprising x functional groups F.sup.1 capable of reacting with a functional group Q.sup.1, x is 1 or 2 and P is a nucleoside mono- or diphosphate, and wherein the catalyst is capable of transferring the S(F.sup.1).sub.x moiety to the core-GlcNAc moiety, to obtain a modified antibody; and a second step (ii) of reacting the modified antibody with a linker-conjugate comprising a functional group Q.sup.1 capable of reacting with functional group F.sup.1 and a target molecule D connected to Q.sup.1 via a linker L.sup.2 to obtain the antibody-conjugate wherein linker L comprises S—Z.sup.3-L.sup.2 and wherein Z.sup.3 is a connecting group resulting from the reaction between Q.sup.1 and F.sup.1. The invention also relates to a use for improving the therapeutic index of an antibody-conjugate and to a method for targeting CD30-expressing cells.
PYRROLOBENZODIAZEPINE-ANTIBODY CONJUGATES
The present invention relates to pyrrolobenzodiazepines (PBDs) having a labile protecting group in the form of a linker to an antibody.
A CONJUGATE OF AN AMANITA TOXIN WITH BRANCHED LINKERS
- Robert Yongxin Zhao ,
- Qingliang YANG ,
- Jun LEI ,
- Yuanyuan HUANG ,
- Linyao ZHAO ,
- Hangbo YE ,
- Shun GAI ,
- Mingjun CAO ,
- Qianqian TONG ,
- Lu BAI ,
- Zhixiang GUO ,
- Chengyu YANG ,
- Xiaomai ZHOU ,
- Hongsheng XIE ,
- Yifang XU ,
- Huihui GUO ,
- Junxiang JIA ,
- Jun ZHENG ,
- Cheng LIN ,
- Xiaotao ZHUO ,
- Wenjun LI ,
- Yong DU ,
- Xiangfei KONG ,
- Binbin CHEN ,
- Yanlei YANG ,
- Yanhong TONG ,
- Xiaoxiao CHEN ,
- Yanhua LI ,
- Xiuzheng ZHANG ,
- Juan LAI
Provided herein is the conjugation of an amanita toxin compound to a cell-binding molecule with branched linkers for having better targeted treatment of abnormal cells. It also relates to a branched-linkage method of conjugation of an amanita molecule to a cell-binding ligand, as well as methods of using the conjugate in targets treatment of cancer, infection and autoimmune disease.