Patent classifications
A61K47/6803
Antibody Conjugates and Methods of Making and Using the Same
Antibodies that include a sulfatase motif-containing tag in a constant region of an immunoglobulin (Ig) heavy chain polypeptide are disclosed. The sulfatase motif can be converted by a formylglycine-generating enzyme (FGE) to produce a formylglycine (fGly)-modified Ig heavy chain polypeptide. An fGly-modified Ig heavy chain polypeptide of the antibody can be covalently and site-specifically bound to a moiety of interest to provide an antibody conjugate. The disclosure also encompasses methods of production of such tagged Ig heavy chain polypeptides, fGly-modified Ig heavy chain polypeptides, and antibody conjugates, as well as methods of use of same.
CONJUGATION OF A CYTOTOXIC DRUG WITH BIS-LINKAGE
- Robert Yongxin Zhao ,
- Yuanyuan Huang ,
- Qingliang Yang ,
- Shun Gai ,
- Hangbo Ye ,
- Linyao Zhao ,
- Chengyu Yang ,
- Yifang Xu ,
- Huihui Guo ,
- Minjun CHAO ,
- Qianqian Tong ,
- Wenjun Li ,
- Xiang CAI ,
- Xiaomai Zhou ,
- Hongsheng Xie ,
- Junxiang Jia ,
- Haifeng ZHU ,
- Zhixiang GUO ,
- Shuihong GAO ,
- Chunyan WANG ,
- Chen Lin ,
- Yanlei YANG ,
- Zhicang YE ,
- Jie PENG ,
- Jun XU ,
- Xiaotao Zuo ,
- Qingyu SU
A conjugation of a cytotoxic drug to a cell-binding molecule with a bis-linker (dual-linker) as shown in Formula (I). Bis-linkage methods of making a conjugate of a cytotoxic drug/molecule to a cell-binding agent in a specific manner are also described, as well as application of the conjugates for the treatment of a cancer, or an autoimmune disease, or an infectious disease.
##STR00001##
wherein “” is an optional bond; X, Y, Z.sub.1, and Z.sub.2 are a functional group; m.sub.1 and n are a integer; L.sub.1 and L.sub.2 are a linker.
TROPHOBLAST CELL-SURFACE ANTIGEN-2 (TROP-2) ANTIBODIES
This application provides isolated antibodies, and antigen-binding fragments thereof, that specifically bind Trophoblast Cell-Surface Antigen-2 (Trop-2). These Trop-2 antibodies, or antigen-binding fragments thereof, have a highbinding affinity for Trop-2, are capable of inducing antibody- dependent cell-mediated cytotoxicity (ADCC), have good tumor penetration, can be internalized by cells expressing Trop-2, and can be used to diagnose, prognose, and treat Trop-2 -associated human diseases (e.g., cancer, infectious diseases, autoimmune diseases, asthma, transplant rejection, and inflammatory disorders).
COMBINATION OF ANTIBODY-DRUG CONJUGATE AND CDK9 INHIBITOR
A pharmaceutical product for administration of an anti HER2 antibody-drug conjugate in combination with a CDK9 inhibitor is provided. The anti-HER2 antibody-drug conjugate is an antibody-drug conjugate in which a drug linker represented by the following formula (wherein A represents the connecting position to an antibody) is conjugated to an anti-HER2 antibody via a thioether bond. Also provided is a therapeutic use and method wherein the antibody-drug conjugate and the CDK9 inhibitor are administered in combination to a subject: Formula (I):
##STR00001##
TREATMENT OF THERAPY-RESISTANT HER-2 POSITIVE BREAST CANCER
This invention concerns the treatment of HER-2 positive breast cancer cells by mediating the signal of GRB7 using an anti-HER-1 antibody, such as panitumumab.
AMHRII-BINDING ANTIBODY DRUG CONJUGATES AND THEIR USE THEREOF IN THE TREATMENT OF CANCERS
The present invention relates to an antibody drug conjugate (ADC) of general formula (I) (D-Lk.sub.1-C(O)-Lk.sub.2-C.sub.2H.sub.4—NH-Lk.sub.3).sub.n-Ab. A pharmaceutical composition comprising, in a pharmaceutically acceptable medium, the said ADC is also concerned by the present invention, as well as the use of this ADC or composition as a medicament, and in particular in the prevention and/or the treatment of an anti-Müllerian hormone type II receptor (AMHRII) expressing cancer in an individual.
OLIGONUCLEOTIDE CONJUGATES AND PREPARATION AND APPLICATIONS THEREOF
The present invention relates to oligonucleotide conjugates and preparation and applications thereof. In particular, the present invention relates to an oligonucleotide conjugated to a biomolecule (e.g. an antibody) and/or an agent of interest (e.g. a drug). In certain embodiments, the oligonucleotide of the present invention is a hybridized complex of a single strand oligonucleotide carrying a biomolecule and a complementary strand oligonucleotide bearing an agent of interest where the hybridized nucleotide segment acts as a linker to link the biomolecule and the agent of interest in one molecule.
NANOBODY (VHH) CONJUGATES AND USES THERE OF
Provided herein are compositions comprising VHH conjugates and their uses in treating diseases.
CONDITIONALLY ACTIVE ANTI-NECTIN-4 ANTIBODIES
Isolated polypeptides having a heavy chain variable region and/or light chain variable region that specifically binds to Nectin-4 protein as well as antibodies and antibody fragments containing the heavy chain variable region and/or the light chain variable region that bind to Nectin-4 protein. Pharmaceutical compositions and kits comprising the polypeptide and antibodies and antibody fragments containing the polypeptide are also provided.
BISPECIFIC ANTIBODY AND USE THEREOF
Provided are a bispecific antibody and use thereof. The bispecific antibody comprises a B7-H4-targeting antigen-binding domain and a 4-1BB-targeting antigen-binding domain. The bispecific antibody has one or two or three sites for binding to 4-1BB, along with a novel fully human B7-H4 antibody. The bispecific antibody specifically binds to tumor cells by targeting B7-H4, reducing toxicity induced by 4-1BB activation. In addition, the bispecific antibody of the present invention comprises a human Fc fragment, and thus retains the binding of Fc to FcRn and has a longer half-life.