Erenumab (AMG 334) is the first human
monoclonal antibody antagonist against the Calcitonin Gene-Related Peptide
Receptor (CGRP) receptor. Like the small-molecule CGRP-receptor antagonists, Erenumab
fully antagonizes CGRP-receptor function and is dose-dependently effective in
an in vivo target coverage model that
exhibits translatability to humans.
Erenumab
fully inhibited CGRP-stimulated cAMP production with an IC50 of 2.3
nM in cell-based functional assays (human CGRP receptor) and was 5000-fold more
selective for the CGRP receptor than other human calcitonin family receptors,
including adrenomedullin, calcitonin, and amylin receptors.
