Erenumab
Identification
- Summary
Erenumab is a calcitonin-gene related peptide antagonist used to prevent migraines.
- Brand Names
- Aimovig
- Generic Name
- Erenumab
- DrugBank Accession Number
- DB14039
- Background
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 3.
In particular, erenumab-aooe is a human immunoglobulin G2 monoclonal antibody that has high affinity binding to the CGRP receptor Label. The antibody is produced utlilizing recombinant DNA technology in Chinese hamster ovary cells Label. 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 Label.
- Type
- Biotech
- Groups
- Approved, Investigational
- Biologic Classification
- Protein Based Therapies
Monoclonal antibody (mAb) - Protein Chemical Formula
- C6472H9964N1728O2018S50
- Protein Average Weight
- Not Available
- Sequences
> Erenumab (Heavy chain) QVQLVESGGGVVQPGRSLRLSCAASGFTFSSFGMHWVRQAPGKGLEWVAVISFDGSIKYS VDSVKGRFTISRDNSKNTLFLQMNSLRAEDTAVYYCARDRLNYYDSSGYYHYKYYGMAVW GQGTTVTVSSASTKGPSVFPLAPCSRSTSESTAALGCLVKDYFPEPVTVSWNSGALTSGV HTFPAVLQSSGLYSLSSVVTVPSSNFGTQTYTCNVDHKPSNTKVDKTVERKCCVECPPCP APPVAGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVQFNWYVDGVEVHNAKTKP REEQFNSTFRVVSVLTVVHQDWLNGKEYKCKVSNKGLPAPIEKTISKTKGQPREPQVYTL PPSREEMTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPMLDSDGSFFLYSKLT VDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPGK
> Erenumab (Light chain) QSVLTQPPSVSAAPGQKVTISCSGSSSNIGNNYVSWYQQLPGTAPKLLIYDNNKRPSGIP DRFSGSKSGTSTTLGITGLQTGDEADYYCGTWDSRLSAVVFGGGTKLTVLGQPKANPTVT LFPPSSEELQANKATLVCLISDFYPGAVTVAWKADGSPVKAGVETTKPSKQSNNKYAASS YLSLTPEQWKSHRSYSCQVTHEGSTVEKTVAPTECS
Download FASTA Format- Synonyms
- Erenumab
- erenumab-aooe
- External IDs
- AMG 334
- AMG-334
- AMG334
Pharmacology
- Indication
Erenumab is indicated for the preventative treatment of migraine in adults Label.
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- Pharmacodynamics
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 1. Antagonism of CGRP receptors responsible for such vasodilation could theoretically result in vasoconstriction and raises in blood pressure.
In a randomised, double-blind, placebo-controlled study in healthy volunteers, concomitant administration of erenumab (140 mg intravenous, single dose) with sumatriptan (12 mg subcutaneous, given as two 6 mg doses separated by one hour) had no effect on resting blood pressure compared with sumatriptan alone, however Label. Please note that erenumab is indicated for subcutaneous use only, though Label.
- Mechanism of action
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 Label.
Studies since 1985 have demonstrated that CGRP levels increase during acute migraine attacks in migraine-suffering patients but normalize after efficacious sumatriptan therapy 1. Moreover, research has also shown that intravenous administration of CGRP can induce migraine-like attacks in migraine-suffering patients 1. 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 2. In addition to playing a role in cranial nociception, CGRP is also a potent general arterial vasodilator 2. 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 1.
Target Actions Organism UCalcitonin gene-related peptide type 1 receptor Not Available Humans - Absorption
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% Label.
- 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 Label.
- 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 2.
- Metabolism
Erenumab CGRP antibodies demonstrate a low risk for drug-drug interactions and hepatotoxicity since they are predominantly metabolized by degradation into peptides and single amino acids 1.
- Route of elimination
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 Label. 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 2.
- Half-life
Erenumab exhibits non-linear kinetics as a result of binding to the CGRP receptor Label. 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 Label. Serum trough concentrations approached steady state by 3 months of dosing Label. The effective half-life of erenumab was observed to be 28 days Label.
- 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) 2. In contrast, the nonlinear clearance is dependent on the target receptor density and the amount of erenumab bound to the receptors 2. Nevertheless, the maximal nonlinear clearance was observed to be about 1.84L/day 2.
- Adverse Effects
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- 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 Label.
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAbciximab The risk or severity of adverse effects can be increased when Abciximab is combined with Erenumab. Adalimumab The risk or severity of adverse effects can be increased when Adalimumab is combined with Erenumab. Adenovirus type 7 vaccine live The risk or severity of adverse effects can be increased when Erenumab is combined with Adenovirus type 7 vaccine live. Aducanumab The risk or severity of adverse effects can be increased when Aducanumab is combined with Erenumab. Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Erenumab. Alirocumab The risk or severity of adverse effects can be increased when Alirocumab is combined with Erenumab. Amivantamab The risk or severity of adverse effects can be increased when Erenumab is combined with Amivantamab. Anifrolumab The risk or severity of adverse effects can be increased when Anifrolumab is combined with Erenumab. Ansuvimab The risk or severity of adverse effects can be increased when Erenumab is combined with Ansuvimab. Anthrax immune globulin human The risk or severity of adverse effects can be increased when Erenumab is combined with Anthrax immune globulin human. Identify potential medication risksEasily compare up to 40 drugs with our drug interaction checker.Get severity rating, description, and management advice.Learn more - Food Interactions
- No interactions found.
Products
- Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Aimovig Injection, solution 140 mg Subcutaneous Novartis Europharm Limited 2020-12-16 Not applicable EU Aimovig Injection, solution 70 mg Subcutaneous Novartis Europharm Limited 2020-12-16 Not applicable EU Aimovig Injection 70 mg/1mL Subcutaneous AMGEN INC 2018-05-22 Not applicable US Aimovig Solution 140 mg / mL Subcutaneous Novartis Not applicable Not applicable Canada Aimovig Solution 70 mg / mL Subcutaneous Novartis 2018-12-04 Not applicable Canada Aimovig Injection, solution 140 mg Subcutaneous Novartis Europharm Limited 2020-12-16 Not applicable EU Aimovig Injection, solution 140 mg/1mL Subcutaneous AMGEN INC 2019-03-15 Not applicable US Aimovig Injection, solution 70 mg Subcutaneous Novartis Europharm Limited 2020-12-16 Not applicable EU Aimovig Injection, solution 140 mg Subcutaneous Novartis Europharm Limited 2020-12-16 Not applicable EU Aimovig Injection, solution 140 mg/1mL Subcutaneous AMGEN INC 2019-03-15 Not applicable US
Categories
- ATC Codes
- N02CD01 — Erenumab
- Drug Categories
- Amino Acids, Peptides, and Proteins
- Analgesics
- Antibodies
- Antibodies, Monoclonal
- Antimigraine Preparations
- Blood Proteins
- Calcitonin Gene-Related Peptide (CGRP) Antagonists
- Calcitonin Gene-Related Peptide Receptor Antagonists
- Central Nervous System Agents
- Globulins
- Immunoglobulins
- Immunoproteins
- Nervous System
- Peripheral Nervous System Agents
- Proteins
- Sensory System Agents
- Serum Globulins
- Chemical TaxonomyProvided by Classyfire
- Description
- Not Available
- Kingdom
- Organic Compounds
- Super Class
- Organic Acids
- Class
- Carboxylic Acids and Derivatives
- Sub Class
- Amino Acids, Peptides, and Analogues
- Direct Parent
- Peptides
- Alternative Parents
- Not Available
- Substituents
- Not Available
- Molecular Framework
- Not Available
- External Descriptors
- Not Available
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- I5I8VB78VT
- CAS number
- 1582205-90-0
References
- General References
- Deen M, Correnti E, Kamm K, Kelderman T, Papetti L, Rubio-Beltran E, Vigneri S, Edvinsson L, Maassen Van Den Brink A: Blocking CGRP in migraine patients - a review of pros and cons. J Headache Pain. 2017 Sep 25;18(1):96. doi: 10.1186/s10194-017-0807-1. [Article]
- Vu T, Ma P, Chen JS, de Hoon J, Van Hecken A, Yan L, Wu LS, Hamilton L, Vargas G: Pharmacokinetic-Pharmacodynamic Relationship of Erenumab (AMG 334) and Capsaicin-Induced Dermal Blood Flow in Healthy and Migraine Subjects. Pharm Res. 2017 Sep;34(9):1784-1795. doi: 10.1007/s11095-017-2183-6. Epub 2017 Jun 7. [Article]
- Press Release: Novartis and Amgen announce FDA approval of Aimovig(TM) (erenumab), a novel treatment developed specifically for migraine prevention [Link]
- FDA Approved Drug Products: AIMOVIG (erenumab-aooe) injection, for subcutaneous use [Link]
- External Links
- FDA label
- Download (1.57 MB)
- MSDS
- Download (35.7 KB)
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Completed Health Services Research Migraine 1 4 Completed Prevention Migraine 3 4 Completed Supportive Care Migraine 1 4 Completed Treatment Episodic Migraine 1 4 Completed Treatment Facial Pain / Rhino Sinusitis 1 4 Completed Treatment Migraine 5 4 Recruiting Other Headache / Migraine 1 4 Recruiting Other Migraine 1 4 Terminated Prevention Migraine 1 4 Terminated Treatment Migraine 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Injection Subcutaneous Injection Subcutaneous 70 mg/1mL Injection, solution Subcutaneous 140 mg/1mL Injection, solution Subcutaneous 140 MG Injection, solution Subcutaneous 70 MG Solution Subcutaneous 140 mg / mL Solution Subcutaneous 70 mg / mL Injection, solution Subcutaneous 70 mg/1ml Injection, solution Subcutaneous 70 mg/ml Injection, solution Subcutaneous 140 MG/ML Solution Subcutaneous 70.000 mg Solution Subcutaneous 140 mg/ml Solution Subcutaneous 140 mg Solution Subcutaneous 70 mg - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Liquid
- Experimental Properties
- Not Available
Targets

- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Receptor for calcitonin-gene-related peptide (CGRP) together with RAMP1 and receptor for adrenomedullin together with RAMP3 (By similarity). Receptor for adrenomedullin together with RAMP2. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase.
- Specific Function
- Adrenomedullin receptor activity
- Gene Name
- CALCRL
- Uniprot ID
- Q16602
- Uniprot Name
- Calcitonin gene-related peptide type 1 receptor
- Molecular Weight
- 52928.98 Da
Drug created at May 18, 2018 13:55 / Updated at June 03, 2022 07:24