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US 8,617,558 B2Granted
Camptothecin-binding moiety conjugates
AssigneeImmunomedics, Inc.
InventorsSerengulam V. Govindan, David M. Goldenberg, Sung-Ju Moon
Life of this patent
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Abstract
The invention relates to therapeutic conjugates with improved ability to target various diseased cells containing a targeting moiety (such as an antibody or antibody fragment), a linker and a camptothecin as a therapeutic moiety, and further relates to processes for making and using the said conjugates.
Claims24
A method for delivering a camptothecin drug, comprising administering to a subject a composition comprising a conjugate of a camptothecin drug and a targeting moiety of the formula:
- TM-[L3]-[L2]-[L1]mAAn-CPT, where TM is a targeting moiety selected from the group consisting of a murine, chimeric, primatized, humanized, and human monoclonal antibody (MAb), and said antibody is an intact antibody, an antibody fragment selected from the group consisting of Fab, Fab′, F(ab)2 and F(ab′)2, or a single-chain construct antibody sub-fragment;
- CPT is camptothecin or an analog thereof;
- L3 is a component of a cross-linker comprising an antibody-coupling moiety;
- L2 comprises a defined PEG (polyethylene glycol) with 1-12 monomeric units attached to L3 at one end with a triazole moiety, is attached to L1 at the other end by an amide, hydrazide, carbonate or ester bond, or to CPT by a carbonate bond when L1 and AA are absent, or attached to AA by an amide bond when L1 is absent;
- L1 comprises a collapsible linker, or a peptidase-cleavable moiety optionally attached to a collapsible linker, or an acid-cleavable moiety;
- AA is an amino acid;
- m is an integer with values of 0 or 1, and n is an integer with values of 0, 1, 2, 3, or 4;
- and when n is >1, the amino acids represented by AA can be the same or different.
5 more elements
Dependencies are inferred from the claim text.