Synonyms: ALD-403 | ALD403 | eptinezumab-jjmr | Vyepti®
eptinezumab is an approved drug (FDA (2020), EMA (2022))
Compound class:
Antibody
Comment: Eptinezumab is a humanized IgG1 anti-calcitonin gene-related peptide (CGRP) monoclonal antibody for the prevention of migraine [6]. It was developed by Lundbeck and their subsidiary Alder Biopharmaceuticals (Alderbio). The INN record for eptinezumab indicates that it binds to CALCA (α-CGRP) and CALCB (β-CGRP). Peptide sequence alignment using NCBI BLAST Protein reveals 100% matches with sequences claimed in Alderbio's patent WO2012162257A2, and distinguish eptinezumab as the monoclonal referred to as Ab5 in the patent document.
CGRP plays an important role in migraine pathophysiology [2], and both the CGRP peptide and its receptor (CGRPR) are targets of anti-migraine therapeutics [1,4-5]. Eptinezumab is the fourth anti-CGRP pathway monoclonal to reach the clinic: the others are erenumab (anti-CGRPR), galcanezumab (anti-CALCA/B) and fremanezumab (anti-CALCA/B). These antibodies are used as alternatives to CGRPR antagonists such as ubrogepant (FDA approved in 2019). |
References |
1. Edvinsson L. (2018)
The CGRP Pathway in Migraine as a Viable Target for Therapies. Headache, 58 Suppl 1: 33-47. [PMID:29697153] |
2. Edvinsson L. (2019)
Role of CGRP in Migraine. Handb Exp Pharmacol, 255: 121-130. [PMID:30725283] |
3. Garcia-Martinez LF, Kaiser EA, Kovacevich BR, Kuburas A, Latham JA, Raddant AC, Recober A, Russo AF, Smith JTL. (2012)
Use of anti-cgrp antibodies and antibody fragments to prevent or inhibit photophobia or light aversion in subjects in need thereof, especially migraine sufferers. Patent number: WO2012162257A2. Assignee: Alderbio Holdings Llc, The University Of Iowa Research Foundation. Priority date: 20/05/2011. Publication date: 29/11/2012. |
4. Mitsikostas DD, Reuter U. (2017)
Calcitonin gene-related peptide monoclonal antibodies for migraine prevention: comparisons across randomized controlled studies. Curr Opin Neurol, 30 (3): 272-280. [PMID:28240610] |
5. Raffaelli B, Reuter U. (2018)
The Biology of Monoclonal Antibodies: Focus on Calcitonin Gene-Related Peptide for Prophylactic Migraine Therapy. Neurotherapeutics, 15 (2): 324-335. [PMID:29616494] |
6. Scuteri D, Corasaniti MT, Tonin P, Bagetta G. (2019)
Eptinezumab for the treatment of migraine. Drugs Today, 55 (11): 695-703. [PMID:31840684] |