Calcitonin gene-related peptide (CGRP) is a protein in the brain and nervous system. Research indicates that CGRP is one of the causes of migraine. Taking CGRP migraine medications that block this protein could manage or treat migraine.

CGRP migraine medications are also known as:

  • CGRP antagonist treatments
  • CGRP inhibitors
  • CGRP-blocking medications
  • CGRP medications

CGRP medications block CGRP by attaching to the protein or blocking receptor sites. Blocking CGRP helps prevent inflammation in the membranes covering the brain, which can help manage migraine.

Migraine is a common condition, with some evidence suggesting it affects almost 16% of adults in the United States. It involves severe, recurring headaches, among other symptoms.

This article discusses CGRP-blocking migraine treatment. We examine how the medication works for migraine, its benefits and risks, and its effectiveness.

A pharmacist reaching for CGRP medication.Share on Pinterest
Sergio Marcos/Stocksy

CGRP is a protein that neurons produce in the peripheral and central nervous systems. It plays a role in dilating blood vessels and the transmission of pain.

Clinical studies have shown that, for some people, CGRP plays an important role in inducing migraine. Elevated CGRP levels are present in some people’s plasma, saliva, and tear fluid in those with spontaneous migraine.

Researchers have investigated the potential role of CGRP in developing migraine for more than 30 years. Evidence suggests an association between higher levels of CGRP and migraine.

Research indicates that targeting and blocking the CGRP protein with CGRP-targeted treatments may help relieve migraine pain and prevent migraine attacks.

Currently, two types of drugs target CGRP or the CGRP receptor, monoclonal antibodies and gepants. Monoclonal antibodies are injectable CGRP medications, and gepants are oral CGRP medications.

CGRP monoclonal antibodies

Monoclonal antibodies are molecules scientists produce in a laboratory to serve as substitute antibodies. They can bind to specific targets in the body. For example, CGRP monoclonal antibody medications attach to CGRP or its receptor and prevent migraine from developing.

The Food and Drug Administration (FDA) approved three CGRP-targeting monoclonal antibodies in 2018 and another in 2020. These include:

Research indicates that CGRP monoclonal antibodies are a safe and effective way to reduce the frequency and severity of migraine attacks. They also have fewer side effects than other preventive medications for migraine.

Gepants

Gepants are another form of CGRP-blocking medication that blocks CGRP receptors. There are three gepants with FDA approval, including:

Each of these medications has different uses. Rimegepant and atogepant are preventive medications, which means a person takes them to stop migraine symptoms before they occur. People may also take rimegepant to ease symptoms once they occur. Ubrogepant is only suitable if a person already has symptoms.

Gepants bind to the CGRP receptor on the trigeminal nerve and prevent the nerves from releasing CGRP and the blood vessel from dilating.

Monoclonal antibody migraine treatments require a person to administer them with a needle or automatic pen. A subcutaneous injection under the skin allows the body to absorb the medication slowly and steadily.

As these medications have a long duration of action or half-life. A person may only need to complete this injection monthly or quarterly to prevent a migraine attack.

Unlike the other CGRP monoclonal antibodies, a doctor administers Vyepti via intravenous infusion every 3 months.

Gepants are available to take orally in tablet form. Individuals take them at the onset of migraine pain to give immediate relief.

CGRP-blocking drugs are generally effective at reducing and preventing symptoms of migraine. They may work for people who do not experience relief from other migraine medications.

According to a 2018 study, nearly one-third of people taking CGRP-targeting drugs experienced a 50% reduction in migraine episodes compared to a placebo group.

Anti-CGRPs have a similar level of effectiveness to other migraine treatments but typically carry a lower risk of side effects.

According to the American Migraine Foundation, people usually see a benefit from CGRP medications within 1 month. Many people notice a step reduction in migraine days within 1–4 weeks, and this reduction typically stabilizes at around 3 months.

As with all medications, the cost of CGRP-blocking medications can vary. The price will also depend on a person’s insurance coverage and the drugstore they use.

The manufacturers may provide programs or discounts to reduce the price of the medication.

CGRP medications are the first preventive medications explicitly developed for migraine. Before their development, preventive treatments for migraine consisted of drugs developed for other conditions, such as high blood pressure, epilepsy, and depression, but also proved helpful for migraine. CGRP antagonists have fewer side effects than these older medications.

According to a 2017 review, CGRP-blocking treatments are effective, and their benefits generally outweigh potential complications. They may benefit individuals who do not respond to other migraine treatments.

The review notes that in clinical trials, CGRP medications showed a 50% reduction in monthly migraine days.

Most people require monthly doses of CGRP medications or quarterly doses of Ajovy and Vyepti, so they may be less likely to miss a dose. Additionally, people do not need to wait to experience symptoms of migraine before taking the treatment to prevent a migraine attack.

Researchers need to conduct more studies to understand the potential risks of CGRP medications, particularly their long-term effects.

While CGRP plays a role in migraine, research also suggests it can influence the risk of heart conditions. CGRP can dilate blood vessels to help balance blood pressure, so blocking this protein could affect blood pressure and heart health.

There is limited safety information on taking CGRP-blocking medications during pregnancy, so a doctor is unlikely to suggest this treatment.

As many CGRP antagonists require administration by injection, there could be pain at the injection site.

CGRP is a protein that plays a role in the development of migraine. CGRP-blocking drugs block the effects of this protein to try to prevent migraine attacks. They can also shorten the duration of attacks and reduce pain and other symptoms.

Many of these drugs are monoclonal antibodies that a person receives via injection or gepants that people take orally. Current evidence suggests they are safe and effective treatments, but more research is necessary to understand the potential side effects.

People can ask a doctor about CGRP medications and discuss whether it is a suitable treatment for them.