Merck Sharp + Dohme Corp.

Ambrx, Inc.

Sanjiv Shah

Ying Sun

Nick Knudsen

Robert M Garbaccio

Linda Liang

Jeffrey Curtis Kern

Philip E Brandish

Jianing Wang

Dennis P Gately

Anthony Manibusan

Andrew Beck

Dennis Zaller

Antibody drug conjugates (ADCs) comprising an antibody conjugated to an anti-inflammatory therapeutic agent via a phosphate-based linker with tunable extracellular and intracellular stability are described.

Antibody drug conjugate for anti-inflammatory applications

Phosphate-based linkers with tunable stability for intracellular delivery of drug conjugates are described. The phosphate-based linkers comprise a monophosphate, diphosphate, triphosphate, or tetraphosphate group (phosphate group) and a linker arm comprising a tuning element and optionally a spacer. A payload is covalently linked to the phosphate group at the distal end of the linker arm and the functional group at the proximal end of the linker arm is covalently linked to a cell-specific targeting ligand such as an antibody. These phosphate-based linkers have a differentiated and tunable stability in blood vs. an intracellular environment (e.g. lysosomal compartment).

Phosphate based linkers for intracellular delivery of drug conjugates

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Wakefield, MA, United States of America

Sanjiv Shah