erenumab   Click here for help

GtoPdb Ligand ID: 9250

Synonyms: Aimovig® | AMG 334 | AMG-334 | erenumab-aooe
Approved drug
erenumab is an approved drug (FDA & EMA (2018))
Compound class: Antibody
Comment: Erenumab (erenumab-aooe, AMG-334) is a first-in-class fully human 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 is used clinically to prevent migraine headache. The selectivity of erenumab for the CGRPR vs. the AMY1 receptor has not been fully established.

Anti-CGRPR antagonistic monoclonals are being developed in place of non-peptide small molecule CGRPR antagonists as these have suffered from hepatotoxicity liability (although this has been largely overcome by using different chemotypes) 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].
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Compound class Antibody
Approved drug? Yes (FDA & EMA (2018))
International Nonproprietary Names Click here for help
INN number INN
10296 erenumab
Synonyms Click here for help
Aimovig® | AMG 334 | AMG-334 | erenumab-aooe
Database Links Click here for help
Specialist databases
IMGT/mAb-DB 618
Other databases
GtoPdb PubChem SID 315661325
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