Erenumab

Erenumab (AMG-334) is a fully human monoclonal antibody. Erenumab inhibits the calcitonin gene-related peptide (CGRP) receptor. Erenumab prevents the increase in dermal blood flow in cynomolgus monkeys. Erenumab can be used in the research of episodic migraine^[1][2][3]. IC50 & Target:CALCRL/CGRPR In Vitro:Erenumab (1-100 nM) competitively inhibits the vasodilatory effect induced by aCGRP, with a pA₂ of 9.00 in cerebral arteries and an apparent pK_B of 7.50 in meningeal arteries, indicating that it is more potent in cerebral arteries^[2].
Erenumab (0.5 pM-10 μM, 3 h) competes with [¹²⁵I]-CGRP for binding to human CGRP receptors, with a K_i value of 0.02 nM. In cell-based functional assays (human CGRP receptors), AMG 334 fully inhibits CGRP-stimulated cyclic adenosine monophosphate (cAMP) production, with an IC₅₀ of 2.3 nM^[3].
Erenumab (0.5 pM-10 μM, 3 h) exhibits antagonistic potency at cynomolgus monkey CGRP receptors, with an IC₅₀ of 5.7 nM^[3]. In Vivo:Erenumab (0.1-30 mg/kg, i.v., single dose) dose-dependently inhibits capsaicin-induced increases in dermal blood flow in cynomolgus monkeys^[3].