Cleavable conjugates for the delivery and release of agents in native form
US5563250A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | May 13, 1994 |
| Grant date | Oct 8, 1996 |
| Priority date | — |
| Expiry date | May 13, 2014 |
Classification
- Technology area (CPC A)Human Necessities
- CPC primaryA61K2123/00
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
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.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.