|
Synonyms: clone III | Emgality® | galcanezumab-gnlm | LY-2951742 | LY2951742
galcanezumab is an approved drug (FDA (2018))
Compound class:
Antibody
Comment: Galcanezumab (LY2951742) is a monoclonal antibody targeting calcitonin A and B (CALCA a.k.a. α-CGRP and CALCB a.k.a. β-CGRP respectively), whose anti-migraine and analgesic actions can be applied clinically.
Annotated peptide sequences for this antibody are available from its IMGT/mAb-DB record. Protein BLAST analysis reveals 100% matches with peptides claimed in patent WO2007076336 [1]. |
| No information available. |
Summary of Clinical Use  |
| Following encouraging results from a proof-of-concept clinical trial (NCT01625988) [2], galcanezumab (LY2951742) was evaluated in Phase 3 clinical trials as a potential treatment for migraine and cluster headaches. FDA approval (for the preventive treatment of migraine in adults) was granted in September 2018, and this was the third CGRP/CGRPR pathway-targeting anti-migraine therapy to gain FDA approval in that year (the other two being the anti-CGRPR erenumab and the anti-CGRP fremanezumab). |
| Mechanism Of Action and Pharmacodynamic Effects |
| CGRP is a sensory neuropeptide with vasodilatory and pro-inflammatory actions, which are believed to underlie this neurotransmitters role in the pathophysiology of migraine and cluster headaches. LY2951742 acts as a CGRP-scavenger, and this action is thought to reduce circulating CGRP levels. However, the exact location of the antibody's molecular action is presently undetermined, as it is not known if, or how, LY2951742 could breach the blood-brain barrier to act in the CNS- see Dodick et al. (2014) [2] and the article's accompanying comments for further explanation. |
| Clinical Trials | |||||
| Clinical Trial ID | Title | Type | Source | Comment | References |
| NCT01625988 | A Study of LY2951742 in Participants With Migraine | Phase 2 Interventional | Eli Lilly and Company | ||
| External links |
|
For extended ADME data see the following: Drugs.com |
