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US 2008/0166363 A1Published application
Camptothecin-Binding Moiety Conjugates
AssigneeImmunomedics, Inc.
InventorsSerengulam V. Govindan, David M. Goldenberg, Sung-Ju Moon
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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.
Claims29
A conjugate of a camptothecin drug and a targeting moiety of the formula:
- TM-[L3]-[L2]-[L1]mAAn-CPT, where TM is a disease-targeting moiety;
- CPT is camptothecin or an analog thereof;
- L3 is a component of a cross-linker comprising an antibody-coupling moiety and one or more acetylene or azide groups;
- L2 comprises a defined PEG with azide or acetylene at one end, complementary to the acetylene or azide moiety in L3, and a reactive group such as carboxylic acid or hydroxyl group at the other end;
- 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.