Cleavable conjugates for the delivery and release of agents in n

Details Cleavable conjugates for the delivery and release of agents in n Cleavable conjugates for the delivery and release of agents in n

1994-05-13

1996-10-08

Kim, Kay K. A.

Organic compounds -- part of the class 532-570 series

Organic compounds

Carbohydrates or derivatives

536 6, 536 61, 536 62, 536 172, 536 173, 536 175, 536 182, 536 183, 536 184, 536 187, 536 221, 536 53, 536 54, 536115, 536122, 546243, 546244, 546246, 546248, 548543, 548550, 548551, 548558, 549 28, 549 62, 549 65, 549 68, 549 72, 549 73, 549416, 549417, 549419, 549476, 549480, 549491, 549497, C07H 302, C07H 502, C07H 504, C07D20704, C07D29504, C07D30712, C07D30714, C07D33300

Patent

active

055632505

ABSTRACT:
The present invention provides cleavable conjugates whose linkers contain a labile bond that is cleavable under a variety of mild conditions, including weakly acidic. Since the agent may be bonded directly to the linker, cleavage can result in release of native agent. The invention also provides methods for producing cleavable conjugates. Preferred agents include drugs, toxins, biological response modifiers, radiodiagnostic compounds, radiotherapeutic compounds, and derivatives thereof. The targeting molecule employed in the invention may be an intact molecule, a fragment thereof, or a functional equivalent thereof. In a particularly preferred embodiment, the targeting molecule is a monoclonal antibody directed towards a tumor-associated antigen in man. The invention further provides methods for delivering to the cytoplasm of a target cell an agent free of its targeting molecule carrier. A diagnostically/therapeutically effective dose of a cleavable conjugate is administered to a warm-blooded animal such as man.

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