Eribulin-based antibody-drug conjugates and methods of use
AssigneeEisai R&D Management Co., Ltd.
InventorsEarl F. Albone, Xin Cheng, Daniel W. Custar, Keiji Furuuchi, Jing Li, Utpal Majumder, Toshimitsu Uenaka
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Abstract
Linker toxins and antibody-drug conjugates that bind to human oncology antigen targets such as folate receptor alpha and/or provide anti-tubulin drug activity are disclosed. The linker toxins and antibody-drug conjugates comprise an eribulin drug moiety and can be internalized into target antigen-expressing cells. The disclosure further relates to methods and compositions for use in the treatment of cancer by administering the antibody-drug conjugates provided herein.
Claims6
1-183. (canceled)
A composition comprising -L-D, wherein D is eribulin;
- and L is a cleavable linker covalently attached to D, wherein the cleavable linker comprises Mal-(PEG)m-Val-Cit-pAB and m is an integer from 1 to 6,
- wherein the nitrogen atom in the Mal is attached to PEG, and
- wherein the pAB (p-aminobenzyloxycarbonyl) is attached to eribulin via a C-35 amine and the amino group in the pAB is attached to Cit.
The composition of claim 1, wherein m is an integer from 2 to 5.
The composition of claim 1, wherein m is 2, 3, or 4.
The composition of claim 1, wherein the cleavable linker comprises Mal-(PEG)2-Val-Cit-pAB.
The composition of claim 1, wherein the Mal is attached to a sulfhydryl group.
Dependencies are inferred from the claim text.