Erenumab, sold under the brand name Aimovig, is a

medication Medication (also called medicament, medicine, pharmaceutical drug, medicinal product, medicinal drug or simply drug) is a drug used to medical diagnosis, diagnose, cure, treat, or preventive medicine, prevent disease. Drug therapy (pharmaco ...

which blocks the calcitonin gene-related peptide receptor (CGRPR) for the prevention of

migraine Migraine (, ) is a complex neurological disorder characterized by episodes of moderate-to-severe headache, most often unilateral and generally associated with nausea, and light and sound sensitivity. Other characterizing symptoms may includ ...

. It is administered by

subcutaneous injection Subcutaneous administration is the insertion of medications beneath the skin either by injection or infusion. A subcutaneous injection is administered as a bolus (medicine), bolus into the subcutis, the layer of skin directly below the dermis and ...

. Erenumab, which was developed by

Amgen Amgen Inc. (formerly Applied Molecular Genetics Inc.) is an American multinational biopharmaceutical Corporation, company headquartered in Thousand Oaks, California. As one of the world's largest independent biotechnology companies, Amgen has a ...

and

Novartis Novartis AG is a Swiss multinational corporation, multinational pharmaceutical company, pharmaceutical corporation based in Basel, Switzerland. Novartis is one of the largest pharmaceutical companies in the world and was the eighth largest by re ...

, was approved in May 2018, and was the first CGRPR antagonist to be approved by the U.S.

Food and Drug Administration The United States Food and Drug Administration (FDA or US FDA) is a List of United States federal agencies, federal agency of the United States Department of Health and Human Services, Department of Health and Human Services. The FDA is respo ...

. In 2020, it was the 234th most commonly prescribed medication in the United States, with more than 1million prescriptions.

Medical uses

Erenumab is indicated for the prevention of

in adults.

Side effects

Common side effects are

constipation Constipation is a bowel dysfunction that makes bowel movements infrequent or hard to pass. The Human feces, stool is often hard and dry. Other symptoms may include abdominal pain, bloating, and feeling as if one has not completely passed the ...

pruritus An itch (also known as pruritus) is a sensation that causes a strong desire or reflex to scratch. Itches have resisted many attempts to be classified as any one type of sensory experience. Itches have many similarities to pain, and while both ...

, muscle

spasm A spasm is a sudden involuntary contraction of a muscle, a group of muscles, or a hollow organ, such as the bladder. A spasmodic muscle contraction may be caused by many medical conditions, including dystonia. Most commonly, it is a musc ...

s, as well as mild and mostly transient reactions at the injection site.

Interactions

Erenumab was shown not to interact with

ethinylestradiol Ethinylestradiol (EE) is an estrogen medication which is used widely in birth control pills in combination with progestins. Ethinylestradiol was widely used for various indications such as the treatment of menopausal symptoms, gynecological ...

, norgestimate or the migraine drug

sumatriptan Sumatriptan, sold under the brand name Imitrex among others, is a medication used to treat migraine headaches and cluster headaches. It is taken Oral administration, orally, Nasal administration, intranasally, or by Subcutaneous injection, su ...

. It is expected to generally have a low potential for interactions because it is not metabolized by

cytochrome P450 Cytochromes P450 (P450s or CYPs) are a Protein superfamily, superfamily of enzymes containing heme as a cofactor (biochemistry), cofactor that mostly, but not exclusively, function as monooxygenases. However, they are not omnipresent; for examp ...

enzymes.

Pharmacology

Mechanism of action

Erenumab is a fully human

monoclonal antibody A monoclonal antibody (mAb, more rarely called moAb) is an antibody produced from a cell lineage made by cloning a unique white blood cell. All subsequent antibodies derived this way trace back to a unique parent cell. Monoclonal antibodie ...

blocking the calcitonin gene-related peptide receptor (CGRPR).

Pharmacokinetics

After

, the erenumab has an estimated

bioavailability In pharmacology, bioavailability is a subcategory of absorption and is the fraction (%) of an administered drug that reaches the systemic circulation. By definition, when a medication is administered intravenously, its bioavailability is 100%. H ...

of 82%. Highest

blood plasma Blood plasma is a light Amber (color), amber-colored liquid component of blood in which blood cells are absent, but which contains Blood protein, proteins and other constituents of whole blood in Suspension (chemistry), suspension. It makes up ...

concentrations are reached after four to six days. Like other proteins, the substance is degraded by

proteolysis Proteolysis is the breakdown of proteins into smaller polypeptides or amino acids. Protein degradation is a major regulatory mechanism of gene expression and contributes substantially to shaping mammalian proteomes. Uncatalysed, the hydrolysis o ...

to small

peptide Peptides are short chains of amino acids linked by peptide bonds. A polypeptide is a longer, continuous, unbranched peptide chain. Polypeptides that have a molecular mass of 10,000 Da or more are called proteins. Chains of fewer than twenty am ...

s and

amino acid Amino acids are organic compounds that contain both amino and carboxylic acid functional groups. Although over 500 amino acids exist in nature, by far the most important are the 22 α-amino acids incorporated into proteins. Only these 22 a ...

s. It has an

elimination half-life Biological half-life (elimination half-life, pharmacological half-life) is the time taken for concentration of a biological substance (such as a medication) to decrease from its maximum concentration ( Cmax) to half of Cmax in the blood plasma. ...

of 28 days.

History

Erenumab was developed by Amgen Inc. in conjunction with

. In the phase III STRIVE

clinical trial Clinical trials are prospective biomedical or behavioral research studies on human subject research, human participants designed to answer specific questions about biomedical or behavioral interventions, including new treatments (such as novel v ...

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 A placebo ( ) can be roughly defined as a sham medical treatment. Common placebos include inert tablets (like sugar pills), inert injections (like saline), sham surgery, and other procedures. Placebos are used in randomized clinical trials ...

(0-mg) group.

Society and culture

Economics

As of 2018, the list price was reported to be per year. In the United Kingdom, Erenumab was approved by the Scottish Medicines Consortium, but the

National Institute for Health and Care Excellence The National Institute for Health and Care Excellence (NICE) is an executive non-departmental public body of the Department of Health and Social Care (United Kingdom), Department of Health and Social Care. As the national health technolog ...

rejected the drug on the basis that its cost-effectiveness was not sufficiently proven.

Legal status

The United States

approved the medication for the preventive treatment of migraine in adults in May 2018. It was the first CGRPR antagonist to be approved. It was approved for medical use in the European Union on 26 July 2018.

Names

Erenumab is the international nonproprietary name and the United States Adopted Name.

References

{{Portal bar , Medicine Antimigraine drugs Calcitonin gene-related peptide receptor antagonists Monoclonal antibodies Amgen Drugs developed by Novartis