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Fremanezumab

Fremanezumab
Monoclonal antibody
TypeWhole antibody
SourceHumanized
TargetCGRP α, β
Clinical data
Trade namesAjovy
Other namesTEV-48125
AHFS/Drugs.comMonograph
MedlinePlusa618053
Routes of
administration
Subcutaneous injection
Drug classCalcitonin gene-related peptide antagonist
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability55–66%
MetabolismProteolysis
Elimination half-life30–31 days (estimated)
ExcretionKidney
Identifiers
CAS Number
DrugBank
ChemSpider
  • none
UNII
KEGG
Chemical and physical data
FormulaC6470H9952N1716O2016S46
Molar mass145507.54 g·mol−1

Fremanezumab, sold under the brand name Ajovy, is a medication used to prevent migraines.[1] It is given by injection under the skin.[1]

The most common side effect is pain and redness at the site of injection.[1] Other side effects include allergic reactions.[1] It is in the calcitonin gene-related peptide antagonist class of medications.[1]

It was approved for medical use in the United States in 2018.[1] The wholesale cost in the United States as of 2019 is $US 369.90 per month.[2]

Medical uses

Fremanezumab was shown to be effective in adults with four or more attacks per month.[3]

Adverse effects

The most common adverse effects are reactions at the injection site, which occurred in 43 to 45% of people in studies (as compared to 38% under placebo). Hypersensitivity reactions occurred in fewer than 1% of patients.[4][5]

Interactions

Fremanezumab does not interact with other antimigraine drugs such as triptans, ergot alkaloids and analgesics. It is expected to generally have a low potential for interactions because it is not metabolised by cytochrome P450 enzymes.[4]

Pharmacology

Mechanism of action

Fremanezumab is a fully humanized monoclonal antibody directed against calcitonin gene-related peptides (CGRP) alpha and beta.[6] The precise mechanism of action is unknown.[5] It is the only approved anti-CGRP monoclonal antibody that can be given with a quarterly interval.

Pharmacokinetics

After subcutaneous injection, fremanezumab has a bioavailability of 55–66%. Highest concentrations in the body are reached after five to seven days. Like other proteins, the substance is degraded by proteolysis to small peptides and amino acids, which are reused or excreted via the kidney. The elimination half-life is estimated to be 30 to 31 days.[5]

History

Fremanezumab was discovered and developed by Rinat Neuroscience, was acquired by Pfizer in 2006, and was then licensed to Teva.[7] It was approved by the US Food and Drug Administration in September 2018.[8] In April 2019, fremanezumab was approved for marketing and use in the European Union.[9]

The drug has been and is still being evaluated for diseases other than migraine, where the endogenous substance CGRP has been implicated in the pathology. Teva is still developing it for episodic cluster headache but stopped development of fremanezumab for the treatment of chronic cluster headache in 2018 after the primary endpoint of a Phase III trial was not met.[10]

See also

Other antibodies blocking the CGRP pathway:

References

  1. ^ a b c d e f "Fremanezumab-vfrm Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Retrieved 15 July 2019.
  2. ^ "NADAC as of 2019-07-10 | Data.Medicaid.gov". Centers for Medicare and Medicaid Services. Retrieved 15 July 2019.
  3. ^ Dodick, David W.; Silberstein, Stephen D.; Bigal, Marcelo E.; Yeung, Paul P.; Goadsby, Peter J.; Blankenbiller, Tricia; Grozinski-Wolff, Melissa; Yang, Ronghua; Ma, Yuju; Aycardi, Ernesto (15 May 2018). "Effect of Fremanezumab Compared With Placebo for Prevention of Episodic Migraine". JAMA. 319 (19): 1999. doi:10.1001/jama.2018.4853.
  4. ^ a b FDA Professional Drug Information on Ajovy. Accessed 2019-05-02.
  5. ^ a b c "Ajovy: EPAR - Product Information" (PDF). European Medicines Agency. 2019-04-17.
  6. ^ "International Nonproprietary Names for Pharmaceutical Substances (INN)" (PDF). WHO Drug Information. WHO. 31 (1). 2017.
  7. ^ "Fremanezumab - Teva Pharmaceutical".
  8. ^ "Teva Announces U.S. Approval of AJOVY (fremanezumab-vfrm) Injection, the First and Only Anti-CGRP Treatment with Both Quarterly and Monthly Dosing for the Preventive Treatment of Migraine in Adults". Teva Pharmaceutical Industries Ltd Pharmaceutical Industries Ltd. Teva Pharmaceutical Industries Ltd Pharmaceutical Industries Ltd. Retrieved 7 October 2018.
  9. ^ "Teva's AJOVY Receives EU Approval Offering Patients the First and Only Anti-CGRP Treatment with Both Quarterly and Monthly Dosing for the Prophylaxis of Migraine in Adults". Business Wire. Retrieved 6 April 2019.
  10. ^ "Teva Pulls Out of Chronic Cluster Headache Trial of Fremanezumab". MD Magazine. Retrieved 2018-06-19.