Genentech, Inc.

F. Hoffmann-la Roche Ag

Jack Sadowsky

Peter Scott Dragovich

Thomas Pillow

BinQing Wei

Mark X Sliwkowski

Zhonghua Pei

Vishal Verma

Donglu Zhang

Steven T Staben

Wayne J Fairbrother

Nicole Blaquiere

Binqing Wei

Leanna Staben

John Wai

Ingrid Wertz

Pragya Adhikari

Jinhua Chen

The subject matter described herein is directed to antibody-PROTAC conjugates (PACs), to pharmaceutical compositions containing them, and to their use in treating diseases and conditions where targeted protein degradation is beneficial.

PROTAC antibody conjugates and methods of use

The invention relates generally to pyrrolobenzodiazepine monomer and dimer prodrugs having a glutathione-activated disulfide prodrug moiety, a DT-diaphorase-activated quinone prodrug moiety or a reactive oxygen species-activated aryl boronic acid or aryl boronic ester prodrug moiety. The invention further relates to pyrrolobenzodiazepine prodrug dimer-antibody conjugates.

Pyrrolobenzodiazepine prodrugs and antibody conjugates thereof

The invention relates generally to disulfide drug conjugates wherein a linker comprising a sulfur-bearing carbon atom substituted with at least one hydrocarbyl or substituted hydrocarbyl is conjugated by a disulfide bond to a cysteine sulfur atom of a targeting carrier, and wherein the linker is further conjugated to a drug moiety. The invention further relates to activated linker-drug conjugates suitable for conjugation to a targeting carrier by a disulfide bond. The invention further relates to methods for preparing hindered disulfide drug conjugates.

Hindered disulfide drug conjugates

The invention provides antibody-drug conjugates comprising an antibody conjugated to a pyrrolobenzodiazepine drug moiety via a disulfide linker, pyrrolobenzodiazepine linker-drug intermediates, and methods of using the antibody-drug conjugates.

Pyrrolobenzodiazepine antibody drug conjugates and methods of use

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Dublin, CA, United States of America

Jack Sadowsky