Patent classifications
A61K47/6889
Modified antibody and radioactive metal-labelled antibody
Described is a labeling technique which can facilitate the metabolism in the liver after administration to patients without the reduction in the antibody function, thereby reducing accumulation of radionuclides in an organ such as the liver, and a modified antibody containing an IgG antibody and an IgG-binding peptide bound to the IgG antibody. The IgG-binding peptide has an amino acid sequence consisting of 13 to 17 amino acid residues, such as GPDCAYH(Xaa1)GELVWCTFH (SEQ ID NO: 2) wherein Xaa1 represents a lysine residue, a cysteine residue, an aspartic acid residue, a glutamic acid residue, 2-aminosuberic acid, or diaminopropionic acid, and a compound represented by the following formula (II-1) is linked at a position of the lysine residue via a modification linker to the N terminus of the IgG-binding peptide. ##STR00001##
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.
PARA-AMINO-BENZYL LINKERS, PROCESS FOR THEIR PREPARATION AND THEIR USE IN CONJUGATES
The present invention relates to para-amino-benzyl linker compounds useful for linking drug moieties to antibodies, to linker-drug compounds in which said para-amino-benzyl linker compounds are covalently linked to drug moieties, and to antibody-drug conjugates in which said para-amino-benzyl linker compounds are covalently linked to drug wherein said drug is enzymatically cleaved from the conjugate at a particular cell or tissue type targeted by said antibody.
SUGAR COMPOUND HAVING POLYETHYLENE GLYCOL CHAIN, AND PRECURSOR OF ANTIBODY-DRUG COMPLEX
The object of the present invention is to provide a synthetic method for ADC synthesis with controllable regioselectivity and number of drugs introduced, as well as synthetic intermediates and synthetic raw materials for such methods. The object can be solved by a sugar compound having a polyethylene glycol chain, of the following general formula (1).
##STR00001##
wherein each X is independently a single bond, an oxygen atom, —NH—, —COHN—, —COO—, or a group of formula (5) or (6), (wherein R.sup.1 is trivalent branched hydrocarbon group having 1 to 6 carbon atoms, R.sup.2 and R.sup.3 are each independently an alkylene group having 1 to 3 carbon atoms), any one or more of Y1 to Y3 are present and are independently a PEG chain, a substituted PEG chain, or a PEG chain containing an oxygen atom, —NH—, —COHN—, or —COO— in the main chain, a structure of the PEG chain is linear or branched, and the number of branches is 2 to 10 in the case of branched structure, Z is independently a hydroxy group, a methoxy group, an azido group, a tetrazine group which may be optionally substituted, a norbornene group, a trans-cyclooctene group, a dibenzylcyclooctyl group, or a bicyclo[6.1.0]nona-4-yn-9-ylmethyl group, or a cyanobenzothiazole group which may be optionally substituted, wherein at least one of Z is not a hydroxy group or methoxy group, when any of Y1 to Y3 is not present, Z is hydrogen and X is oxygen, when X is the group of formula (5) or (6), Y1 to Y3 are bonded to each of R.sup.2 and R.sup.3 of the branched chains thereof, when the PEG chain is branched structure, Z is bonded to each of branched chains.
Methods and materials for treating cancer
This document provides methods and materials involved in treating cancer. For example, methods and materials for using a BiPE that can include (a) one or more molecules having the ability to bind to a cancer cell (e.g., a human breast cancer cell), (b) an optional linker component, and (c) one or more molecules having the ability to bind to an antigen presenting cell (e.g., a human macrophage) to treat cancer are provided.
AEROSOLIZED MUCUS-TETHERING NANOBODIES TO PROTECT AGAINST VIRAL AND MICROBIAL CONTAMINATION IN CLOSED AND SEMI-ENCLOSED SPACES
Provided are innovative compositions for tethering blocking an inactivating of airborne respiratory infectious viruses. The compositions comprise bispecific proteins with two different antigen binding regions (ABR), which are typically configured as immunoglobulin “single variable domains” (ISV). A first ISV binds to a surface protein found on an airborne infectious virus. A second ISV binds to a mucin protein, e.g. a mucin protein present on ocular, nasopharyngeal, tracheal and/or oral surfaces of a mammal. The two ISV are joined by a polypeptide linker.
Site-specific glycoengineering of targeting moieties
The current disclosure provides binding polypeptides (e.g., antibodies), and targeting moiety conjugates thereof, comprising a site-specifically engineered glycan linkage within native or engineered glycans of the binding polypeptide. The current disclosure also provides nucleic acids encoding the antigen-binding polypeptides, recombinant expression vectors and host cells for making such antigen-binding polypeptides. Methods of using the antigen-binding polypeptides disclosed herein to treat disease are also provided.
ERIBULIN ANTIBODY-DRUG CONJUGATES AND METHODS OF USE
Antibodies, antigen-binding fragments, and conjugates (e.g., antibody-drug conjugates such as those comprising eribulin) thereof that bind to mesothelin are disclosed. The disclosure further relates to methods and compositions for use in the treatment of cancer by administering the compositions provided herein.
ANTIBODY MUTANT AND APPLICATION THEREOF
Provided is a mutant of an antibody or fragment thereof, characterized in that the antibody or fragment thereof contains a light-chain constant region, and according to the Kabat numbering system, the amino acid at position 166 is mutated to cysteine.
CONJUGATES
The present disclosure provides conjugates comprising a binding moiety and an immunomodulatory imide compound, e.g., substituted isoindoline compound, wherein the immunomodulatory imide compound is conjugated to a binding moiety via an optional linker. Also provided are compositions comprising the conjugates. The conjugates and compositions are useful for treating a disease or condition, e.g., cancer, in a subject in need thereof.