Erenumab
Erenumab Uses, Dosage, Side Effects, Food Interaction and all others data.
Erenumab (AMG-334) (INN; trade name Aimovig) is a human monoclonal antibody designed specifically to bind and antagonize the calcitonin gene-related peptide receptor (CGRPR) as a means to prevent migraines. Aimovig, as released and marketed by Novartis and Amgen, is in fact a novel therapeutic approach as the first and only FDA approved treatment specifically developed to prevent migraine by blocking the CGRP receptor, which is believed to play a critical role in migraine .
In particular, erenumab-aooe is a human immunoglobulin G2 monoclonal antibody that has high affinity binding to the CGRP receptor . The antibody is produced utlilizing recombinant DNA technology in Chinese hamster ovary cells . It is composed of 2 heavy chains, each containing 456 amino acids, and 2 light chains of the lambda subclass, each containing 216 amino acids, with an approximate molecular weight of 150 kDa .
As a human monoclonal antibody designed to specifically bind with and antagonize the calcitonin gene-related peptide (CGRP) receptor, there is the possibility that erenumab could interfere with natural activities of CGRP that may not be immediately or directly associated with migraines. For example, at peripheral synapses, CGRP released from trigeminal terminals results in vasodilation by way of CGRP receptor on smooth muscle cells of meningeal and cerebral blood vessels, making CGRP a potent general arterial vasodilator . Antagonism of CGRP receptors responsible for such vasodilation could theoretically result in vasoconstriction and raises in blood pressure.
| Trade Name | Erenumab |
| Availability | Prescription only |
| Generic | Erenumab |
| Erenumab Other Names | Erenumab, erenumab-aooe |
| Related Drugs | propranolol, atenolol, topiramate, nifedipine, Depakote, verapamil |
| Weight | 140mg/ml, 70mg/ml |
| Type | Subcutaneous solution |
| Formula | C6472H9964N1728O2018S50 |
| Protein binding | Readily accessible data regarding the protein binding of erenumab is not available, although it is reported that erenumab is capable of 50% to 99% total inhibition of calcitonin gene-related peptide receptors with dosages of 255 ng/mL and 1134 ng/mL, respectively . |
| Groups | Approved, Investigational |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | United States |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Erenumab is a calcitonin-gene related peptide antagonist used to prevent migraines.
Erenumab is indicated for the preventative treatment of migraine in adults .
Erenumab is also used to associated treatment for these conditions: Migraine
How Erenumab works
Erenumab is a human monoclonal antibody that has been designed to bind specifically to the calcitonin gene-related peptide (CGRP) receptor and antagonize the CGRP receptor function .
Studies since 1985 have demonstrated that CGRP levels increase during acute migraine attacks in migraine-suffering patients but normalize after efficacious sumatriptan therapy . Moreover, research has also shown that intravenous administration of CGRP can induce migraine-like attacks in migraine-suffering patients . For all these reasons, the binding and antagonism of CGRP receptors was designed to be mechanism of action for erenumab to take advantage of in reversing the migraine-inducing activity of natural CGRP.
CGRP and its receptor are expressed in both the peripheral and the central nervous system . In addition to playing a role in cranial nociception, CGRP is also a potent general arterial vasodilator . At peripheral synapses, CGRP released from trigeminal terminals results in vasodilation via CGRP receptors on the smooth muscle cells of meningeal and cerebral blood vessels .
Toxicity
The most common side effects of erenumab include pain, redness, or swelling at the injection site, and constipation. Information regarding overdosage is not available .
Food Interaction
No interactions found.Erenumab Hypertension interaction
[Moderate] Hypertension and worsening of preexisting hypertension have been reported in the postmarketing period with erenumab; some patients required pharmacologic treatment and some required hospitalization to control blood pressure.
Many patients had preexisting hypertension or risk factors for hypertension.
Monitor patients for new onset or worsening hypertension and consider discontinuing therapy if no other cause for hypertension is identified.
Erenumab Disease Interaction
Volume of Distribution
After a single 140 mg intravenous dose, the mean (SD) volume of distribution during the terminal phase (Vz) was estimated to be approximately 3.86 (0.77) L .
Elimination Route
Following a single subcutaneous dose of 70 mg or 140 mg erenumab administered to healthy adults, the median peak serum concentrations were attained in about 6 days, and the estimated absolute bioavailability was approximately 82% .
Half Life
Erenumab exhibits non-linear kinetics as a result of binding to the CGRP receptor . Lower than 2-fold accumulation was recorded in trough serum concentrations (Cmin) for episodic and chronic migraine patients following subcutaneous administration of 70 mg once-monthly and 140 mg once-monthly doses . Serum trough concentrations approached steady state by 3 months of dosing . The effective half-life of erenumab was observed to be 28 days .
Clearance
Certain studies show that the population estimate of linear clearance is independent of erenumab concentrations and stays approximately constant at 0.214 L/day (95% CI: 0.191–0.243) . In contrast, the nonlinear clearance is dependent on the target receptor density and the amount of erenumab bound to the receptors . Nevertheless, the maximal nonlinear clearance was observed to be about 1.84L/day .
Elimination Route
Two elimination phases are observed for erenumab. At low concentrations, the elimination is mainly through saturable binding to target (CGRP receptor), while at higher concentrations the elimination of erenumab is primarily through a non-specific, non-saturable proteolytic pathway . These phases correspond to studies that demonstrated two parallel elimination pathways: (a) a slow non-specific elimination pathway through the hepatic reticuloendothelial system, and (b) a rapid saturable elimination pathway mediated by degradation or internalization of the erenumab-receptor complex .
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