A process for preparing a glycoprotein-conjugate is provided, comprising: (a) providing an N-glycoprotein having an exposed tyrosine residue, wherein the exposed tyrosine residue is located within 10 amino acids of an N-glycosylation site, but the N-glycosylation site has been modified such that the glycoprotein does not contain a glycan longer than two monosaccharide residues within 10 amino acids of the exposed tyrosine residue; (b) converting the phenol moiety of the exposed tyrosine residue into an ortho-quinone moiety by contacting the glycoprotein with an oxidative enzyme capable of oxidizing tyrosine; and (c) reacting the ortho-quinone moiety with an alkene or alkyne compound via a [4+2] cycloaddition, wherein the compound comprises a (hetero)cycloalkene or (hetero)cycloalkyne moiety and (i) a chemical handle to further modify the compound with a payload, or (ii) a payload. The resulting glycoprotein-conjugates and pharmaceutical compositions and methods of treatment comprising same are also disclosed.

The present invention relates to pyrrolobenzodiazepines (PBDs) having a labile protecting group in the form of a linker to an antibody.

The present invention relates to new antibody-drug conjugates (ADCs) targeting ROR1, active metabolites of such ADCs, methods for preparation of such ADCs, uses for such ADCs in treatment and/or prevention of illnesses, and uses for such ADCs in production of drugs for treatment and/or prevention of diseases, more specifically diseases associated with over-expression of ROR1, for example cancer. More specifically, the present invention relates to an antibody-drug conjugate comprising an antibody that binds to ROR1 or an antigen-binding fragment thereof, and a pharmaceutical composition comprising the same.

Therapeutic combinations of immunoconjugates that bind to CD123 (e.g., IMGN632) with BCL-2 inhibitors (e.g., venetoclax), and/or a hypomethylating agent (e.g., azacitidine or decitabine) are provided. Methods of administering the combinations to treat hematological malignancies with clinical efficacy and/or decreased toxicity are also provided. Methods of treating hematological malignances present as minimal residual disease using immunoconjugates that bind to CD123 (e.g., IMGN632) are also provided.

A conjugate of formula (I) wherein Ab is a modified antibody having at least one free conjugation site on each heavy chain.

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This disclosure is directed to antibody-drug conjugates. More specifically, this disclosure is directed to compositions comprising (i) antibody-drug conjugates comprising benzodiazepines, and (ii) a small hydrophobic molecule, methods of treatment using the compositions, and methods of formulating the compositions. Furthermore, this disclosure is directed to methods of reducing reversible self-association in antibodies and in antibody-drug conjugates.

The present disclosure relates to antibody-drug conjugates (ADCs) wherein one or more active agents are conjugated to an anti-CD19 antibody through a linker. The linker may comprise a unit that covalently links active agents to the antibody. The disclosure further relates to monoclonal antibodies and antigen binding fragments, variants, multimeric versions, or bispecifics thereof that specifically bind CD19, as well as methods of making and using these anti-CD19 antibodies and antigen-binding fragments thereof in a variety of therapeutic, diagnostic and prophylactic indications.

Provided herein are antibodies and uses of the same.

The present disclosure further relates to a linker-payload compound including an oligosaccharide group, especially a disaccharide group, where the oligosaccharide group is linked to the remainder of the compound by an amide bond. The present disclosure further relates to an antibody-drug conjugate (ADC) containing the linker-payload compound, where the glycan chain in an antibody is remodeled with the oligosaccharide moiety in the linker-payload compound. The present disclosure further relates to preparation methods and use of the above-mentioned substances.

Provided herein are methods of treating cancer in a human subject, comprising administering to the subject: i) an antibody-drug conjugate (ADC) comprising an antibody, a cleavable linker and a cytotoxic agent, and ii) a bispecific checkpoint inhibitor. Further provided herein are kits comprising i) an antibody-drug conjugate (ADC) comprising an antibody, a cleavable linker and a cytotoxic agent, and ii) a bispecific checkpoint inhibitor.