erenumab

Ligand id: 9250

Name: erenumab

Classification
Compound class Antibody
Approved drug? Yes (FDA & EMA (2018))
International Nonproprietary Names
INN number INN
10296 erenumab
Synonyms
Aimovig® | AMG 334 | AMG-334 | erenumab-aooe
Comments
Erenumab (erenumab-aooe, AMG-334) is a first-in-class monoclonal antibody targeting the calcitonin gene-related peptide receptor (CGRPR) [7] (and the first approved GPCR targeted monoclonal). Antibody production was initiated by immunising mice with polypeptides from the N-terminal extracellular domains of human CRLR and human RAMP1, which are subunits of the CGRPR protein complex. Erenumab (a fully human monoclonal) is being a preventative treatment for adults suffering from migraine headache.

Anti-CGRPR antagonistic monoclonals are being developed in place of non-peptide small molecule CGRPR antagonists as these have suffered from hepatotoxicity liability when tested as migraine prophylactics. Antibodies have the positive attributes of being able to span the relatively large binding domain across the CGRPR complex to provide effective blockade, offer the potential for selectivity given the similarity with other receptors in the family, and exhibit a prolonged serum half-life which facilitates longer dosing intervals [1].
Database Links
Specialist databases
IMGT/mAb-DB 618
Other databases
GtoPdb PubChem SID 315661325
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