fremanezumab   Click here for help

GtoPdb Ligand ID: 9208

Synonyms: Ajovy® | fremanezumab-vfrm | LBR-101 | PF-04427429 | PF-4427429 | RI-307 | RN-307 | RN307 | TEV-48125
Approved drug
fremanezumab is an approved drug (FDA (2018), EMA (2019))
Compound class: Antibody
Comment: Fremanezumab (TEV-48125) is a humanised IgG2a monoclonal antibody targeting calcitonin gene-related peptide (CGRP) [3,5], a peptide known to play a role in causing migraines. TEV-48125 was originally formulated as an intravenous agent, but has been re-formulated to allow sub-cutaneous administration. Anti-CGRP antibodies are being developed as an alternative to CGRP receptor antagonists (such as telcagepant) which have already been shown to effectively reduce migraine headache and inhibit neurogenic vasodilatation in humans, and validated the CGRP/CGPR pathway as a target for the acute and preventive treatments of migraine [4]. Anti-CGRP antibodies have the advantage of longer half-lives compared to small molecule antagonists and are expected to exhibit fewer toxicities attributed to off-target interactions, toxitities which have thwarted the development of CGRP receptor antagonists.
The original patent claiming anti-CGRP antibodies held by Rinat Neuroscience Corp. who originally developed TEV-48125 (as RN307) is WO2007054809 [6].
Fremanezumab is the second CGRP/CGPR pathway targeting agent to receive marketing authorisation, following approval of the anti-CGPR monoclonal erenumab earlier in 2018.
References
1. Bigal ME, Dodick DW, Rapoport AM, Silberstein SD, Ma Y, Yang R, Loupe PS, Burstein R, Newman LC, Lipton RB. (2015)
Safety, tolerability, and efficacy of TEV-48125 for preventive treatment of high-frequency episodic migraine: a multicentre, randomised, double-blind, placebo-controlled, phase 2b study.
Lancet Neurol, 14 (11): 1081-90. [PMID:26432182]
2. Bigal ME, Edvinsson L, Rapoport AM, Lipton RB, Spierings EL, Diener HC, Burstein R, Loupe PS, Ma Y, Yang R et al.. (2015)
Safety, tolerability, and efficacy of TEV-48125 for preventive treatment of chronic migraine: a multicentre, randomised, double-blind, placebo-controlled, phase 2b study.
Lancet Neurol, 14 (11): 1091-100. [PMID:26432181]
3. Bigal ME, Escandon R, Bronson M, Walter S, Sudworth M, Huggins JP, Garzone P. (2014)
Safety and tolerability of LBR-101, a humanized monoclonal antibody that blocks the binding of CGRP to its receptor: Results of the Phase 1 program.
Cephalalgia, 34 (7): 483-92. [PMID:24366980]
4. Edvinsson L. (2018)
The CGRP Pathway in Migraine as a Viable Target for Therapies.
Headache, 58 Suppl 1: 33-47. [PMID:29697153]
5. Walter S, Bigal ME. (2015)
TEV-48125: a review of a monoclonal CGRP antibody in development for the preventive treatment of migraine.
Curr Pain Headache Rep, 19 (3): 6. [PMID:25754596]
6. Zeller J, Poulsen KT, Abdiche YN, Pons J, Collier SJ, Rosenthal A. (2007)
Antagonist antibodies directed against calcitonin gene-related peptide and methods using same.
Patent number: WO2007054809. Assignee: Rinat Neuroscience Corp.. Priority date: 14/11/2005. Publication date: 18/05/2007.