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Substance

Erenumab

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Part of the metabolic pathway of Erenumab. See the timeline on the metabolic highway.

Overview

Erenumab, sold under the brand name Aimovig, is a medication which blocks the calcitonin gene-related peptide receptor (CGRPR) for the prevention of migraine. It is administered by subcutaneous injection.[1][2][3] WP

Erenumab, which was developed by Amgen and Novartis, was approved in May 2018, and was the first CGRPR antagonist to be approved by the U.S. Food and Drug Administration. In 2020, it was the 234th most commonly prescribed medication in the United States, with more than 1 million prescriptions.[3–6] WP

Uses, dosage and effects

Medical uses

Erenumab is indicated for the prevention of migraine in adults.[1][2] WP

Risks and side effects

Side effects

Common side effects are constipation, pruritus, muscle spasms, as well as mild and mostly transient reactions at the injection site.[2][7] WP

Interactions

Interactions

Erenumab was shown not to interact with ethinylestradiol, norgestimate or the migraine drug sumatriptan. It is expected to generally have a low potential for interactions because it is not metabolized by cytochrome P450 enzymes.[7] WP

Pharmacology

Mechanism of action

Erenumab is a fully human monoclonal antibody blocking the calcitonin gene-related peptide receptor (CGRPR).[1][8][9] WP

Pharmacokinetics

After subcutaneous injection, the erenumab has an estimated bioavailability of 82%. Highest blood plasma concentrations are reached after four to six days. Like other proteins, the substance is degraded by proteolysis to small peptides and amino acids. It has an elimination half-life of 28 days.[7] WP

History

History

Erenumab was developed by Amgen Inc. in conjunction with Novartis.[3] WP

In the phase III STRIVE clinical trial 955 patients were divided into three groups in a 1:1:1 ratio. Each group was injected subcutaneously monthly with 0, 70 or 140 mg erenumab over a period of 6 months. The results were measured as mean monthly migraine days in months 4, 5, and 6. At baseline the patients experienced between 4 and 14 migraine days per month with an average of 8.3. The medication significantly reduced the number of migraine days per month by 3.2 in the 70-mg group and 3.7 in the 140-mg group, versus 1.8 in the placebo (0-mg) group.[3][10] WP

Chemistry

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Harm reduction information

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Sources

  1. Journal / agency Aimovig- erenumab-aooe injection Aimovig- erenumab-aooe injection, solution. 19 August 2022
  2. Journal / agency Aimovig EPAR. 8 August 2018
  3. Journal / agency Goadsby PJ, Reuter U, Hallström Y, Broessner G, Bonner JH, Zhang F, Sapra S, Picard H, Mikol DD, Lenz RA. A Controlled Trial of Erenumab for Episodic Migraine. The New England Journal of Medicine. November 2017. doi:10.1056/NEJMoa1705848 · PMID 29171821
  4. Other FDA Approves First-in-Class Drug Erenumab (Aimovig) for Migraine Prevention. 17 May 2018
  5. Other The Top 300 of 2020
  6. Other Erenumab - Drug Usage Statistics
  7. Journal / agency Aimovig: EPAR - Product Information. 2018-08-08
  8. Other Amgen Presents First-Of-Its-Kind Data At AAN Annual Meeting Reinforcing Robust And Consistent Efficacy Of Aimovig (erenumab) For Migraine Patients With Multiple Treatment Failures. 17 April 2018
  9. Journal / agency Edvinsson L. CGRP Antibodies as Prophylaxis in Migraine. Cell. December 2018. doi:10.1016/j.cell.2018.11.049 · PMID 30550780
  10. Other Erenumab to prevent migraine: results from phase III STRIBE", Pharma World, 14 December 2017. link 2
  11. Other Kolata, Gina. F.D.A. Approves First Drug Designed to Prevent Migraines. 2018-05-17
  12. Other Gallagher, James. 'Life-changing' migraine drug rejected for NHS. 2019-09-26
  13. Other New migraine drug not cost-effective NICE says in draft guidance
  14. Other First drug to prevent chronic migraines approved by EU. 31 July 2018
  15. Other Statement On A Nonproprietary Name Adopted By The USAN Council - Erenumab. 24 November 2015
  16. Journal / agency World Health Organization. International Nonproprietary Names for Pharmaceutical Substances (INN). Proposed INN: List 115. WHO Drug Information. 2016

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