galcanezumab

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Ligands
galcanezumab

GtoPdb Ligand ID: 8967

Synonyms: clone III | Emgality® | galcanezumab-gnlm | LY-2951742 | LY2951742

galcanezumab is an approved drug (FDA (2018))

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).

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.

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

External links

For extended ADME data see the following:

Drugs.com