α4β7 peptide monomer and dimer antagonists
AssigneeProtagonist Therapeutics, Inc.
InventorsAshok Bhandari, Dinesh V. Patel, Genet Zemede, Larry C. Mattheakis, David Liu
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Abstract
The invention relates to peptide dimer compounds and peptide monomer compounds that potently inhibit binding of α4β7 to the mucosal addressin cell adhesion molecule (MAdCAM) in vivo, possess high selectivity against α4β1 binding, and have high stability under gastrointestinal conditions.
Claims14
A method for treating an inflammatory bowel disease in a subject, the method comprising administering to the subject an effective amount of a pharmaceutical composition comprising a peptide dimer compound comprising two monomer subunits, wherein each monomer subunit comprises the amino acid sequence:
- Pen-(N-Me-Arg)-Ser-Asp-Thr-Leu-Pen-Phe(4-tBu)-(β-homo-Glu)-(D-Lys),
- or a pharmaceutically acceptable salt thereof,
- and wherein the two monomer subunits are linked by a linker moiety.
Dependencies are inferred from the claim text.