Products
Erenumab was approved in many countries, in the EU, and in the United States in 2018 as a solution for injection in a prefilled pen and a prefilled syringe (Aimovig, Novartis / Amgen).
Structure and properties
Erenumab is a human IgG2 monoclonal antibody directed against the CGRP receptor. It has a molecular weight of approximately 150 kDa and is produced by biotechnological methods.
Effects
Erenumab (ATC N02CX07) blocks the calcitonin gene-related peptide receptor (CGRP). The natural ligand CGRP is a neuropeptide that plays an important role in triggering migraine attacks. It consists of 37 amino acids and is expressed in the peripheral and central nervous systems. Two isoforms exist, CGRP-α (Figure) and CGRP-β, which differ in three amino acids. Both are agonists at the CGRP receptor. CGRP has potent vasodilatory properties and plays a central role in pain initiation as well as neurogenic inflammation. Migraineurs have been found to have elevated levels of CGRP during an attack, and intravenous administration of the peptide can induce attacks in migraineurs. Triptans, which are administered for the treatment of migraine attacks, also inhibit the release of CGRP.
Indications
For the prevention of migraine attacks in adults.
Dosage
According to the SmPC. Erenumab has a long half-life of 28 days and therefore only needs to be injected subcutaneously once a month. This represents an advantage for treatment adherence.
Contraindications
- Hypersensitivity
For complete precautions, see the drug label.
Interactions
No drug-drug interactions are known to date.
Adverse effects
The most common potential adverse effects include injection site reactions, constipation, itching, and muscle cramps. Unlike some oral CGRP receptor antagonists, known as gepants, erenumab is not toxic to the liver. Successful therapy can also eliminate the need for pain medications, which are often overused in migraine therapy and can cause many side effects.
