Phosphate based linkers for intracellular delivery of drug conjugates

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