A61K47/68031

Fc GLYCAN REMODELING PLATFORM METHOD FOR SITE-SPECIFIC ANTIBODY CONJUGATION AND APPLICATIONS THEREOF

The present disclosure provides a one-pot chemoenzymatic method for site-specific modification and conjugation of antibodies at their Fc glycan site to produce structurally well-defined antibody conjugates carrying defined drugs and other entities. The method is enabled by the discovery that certain endoglycosidases have the ability to both deglycosylate an antibody and to recognize selectively modified small disaccharide oxazolines for transglycosylation on antibodies without hydrolysis of the resulting products.

TRANSGLUTAMINASE CONJUGATION METHOD WITH AMINO ACID-BASED LINKERS

The present invention relates to a method for generating an antibody-payload conjugate by means of a microbial transglutaminase (MTG). The method comprises a step of conjugating a linker comprising or having the structure (shown in N—>C direction) Aax-(Sp.sub.1)-B.sub.1-(Sp.sub.2) via a primary amine in the N-terminal residue Aax to a glutamine (Gln) residue comprised in the heavy or light chain of an antibody, wherein Aax is an amino acid having the structure NH.sub.2—Y—COOH, wherein Y comprises a substituted or unsubstituted alkyl or heteroalkyl chain; (Sp.sub.1) is a chemical spacer or is absent; (Sp.sub.2) is a chemical spacer or is absent; and B.sub.1 is a linking moiety or a payload. Further the present invention relates to antibody-linker conjugates that have been generated with the method of the invention and uses thereof.

ANTIBODY-DRUG CONJUGATE AND APPLICATION THEREOF
20230381336 · 2023-11-30 ·

The present invention relates to an antibody-drug conjugate and an application thereof, and specifically provides the antibody-drug conjugate, a pharmaceutically acceptable salt and solvate thereof, or a solvate of the salt. The antibody-drug conjugate has the structure represented by formula I, wherein Ab is an anti-Claudin 18.2 antibody. The antibody-drug conjugate of the present invention has good tumor cell growth inhibition activity in vivo and in vitro, low toxicity, and good application prospects.


Ab-(L-D).sub.p  Formula I

IMMUNOCONJUGATES TARGETING CD46 AND METHODS OF USE THEREOF
20220331443 · 2022-10-20 ·

Disclosed herein are immunoconjugates comprising a CD46 binding domain and effector agent. Further provided herein are methods of treating cancer comprising administering to a subject having cancer a pharmaceutical composition comprising immunoconjugates comprising a CD46 binding domain and effector agent.

ANTI-EGFR ANTIBODIES AND ANTIBODY DRUG CONJUGATES

The invention relates to anti-epidermal growth factor (EGFR) antibodies and antibody drug conjugates (ADCs), including compositions and methods of using said antibodies and ADCs.

ANTI-PD-1 ANTIBODY IN COMBINATION WITH AN ANTI-CD30 ANTIBODY IN CANCER TREATMENT

This disclosure provides methods for treating a tumor in a subject comprising administering to the subject an anti-PD-1 antibody and an anti-CD30 antibody. In some embodiments, the tumor is derived from a lymphoma (e.g., a Hodgkin lymphoma or a non-Hodgkin lymphoma). In certain embodiments, the anti-CD30 antibody is an antibody-drug conjugate, e.g., brentuximab vedotin.

INTERCELLULAR ADHESION MOLECULE 1 (ICAM1) ANTIBODY DRUG CONJUGATE AND USES THEREOF

The disclosure provides compositions comprising intercellular adhesion molecule 1 (ICAM1) antibody and methods for using the same for therapeutic applications, for example, treating pancreatic cancer and predicting drug response.

ANTI-TISSUE FACTOR ANTIBODY-DRUG CONJUGATES AND RELATED METHODS
20220257789 · 2022-08-18 ·

Provided herein are antibodies that specifically bind to human tissue factor (TF), anti-TF antibody-drug conjugates (ADCs), and compositions comprising the antibodies or ADCs. Also provided herein are methods of making and using the antibodies or ADCs, such as therapeutic and diagnostic methods.

ANTI-BCMA ANTIBODY, ANTIGEN-BINDING FRAGMENT THEREOF AND MEDICAL USE THEREOF
20220251228 · 2022-08-11 ·

Provided are an anti-BCMA antibody, an antigen-binding fragment thereof, and a medical use thereof. Further provided are a chimeric antibody and a humanized antibody containing a CDR region of the anti-BCMA antibody, a pharmaceutical composition containing the anti-BCMA antibody or the antigen-binding fragment thereof, and the use of same as an anti-cancer drug and for treating autoimmune diseases. Particularly, provided are a humanized anti-BCMA antibody, and the use of same in the preparation of a drug for treating BCMA-mediated diseases or conditions and the use of same in disease detection and diagnosis.

GLYCOSIDE DUAL-CLEAVAGE LINKERS FOR ANTIBODY-DRUG CONJUGATES
20220249686 · 2022-08-11 ·

The present disclosure provides antibody-drug conjugate structures, which include a cleavable linker that links the antibody to the drug and has a first enzymatically cleavable moiety and a second enzymatically cleavable moiety which includes a glycoside selected from a galactoside, a glucoside, a mannoside, a fucoside, O-GlcNAc, and O-GalNAc. The disclosure also encompasses compounds and methods for production of such conjugates, as well as methods of using the conjugates.