Ubrogepant

Ubrogepant is a prescription migraine medicine called a gepant, or calcitonin gene-related peptide (CGRP) receptor antagonist. It is used for the acute treatment of migraine with or without aura in adults, meaning it treats a migraine attack once it has started rather than preventing one.

Ubrogepant is the active ingredient in the brand-name tablet Ubrelvy, and it is available in 50 mg and 100 mg strengths.

Ubrogepant is used to treat migraine attacks once they start in adults. It is not used to prevent migraine, and it is not approved for use in anyone younger than 18 years. Ubrogepant treats migraine with or without aura, which are the sensory warning signs, such as flashes of light, that some people notice before a migraine begins.

Ubrogepant belongs to a class of migraine medicines called gepants (also known as CGRP inhibitors or calcitonin gene-related peptide (CGRP) receptor antagonists). CGRP is a protein found in nerve endings that plays a key role in migraine pain. Gepants work differently from older migraine medicines called triptans, because they do not narrow (constrict) blood vessels.

Ubrogepant works by blocking CGRP receptors, which stops the CGRP protein from triggering the inflammation, blood vessel widening (dilation), and pain that occur during a migraine attack. This CGRP-blocking action is the ubrogepant mechanism of action. By blocking this pathway, it helps ease migraine pain and related symptoms such as nausea and sensitivity to light and sound. Unlike some traditional migraine treatments, it does not constrict blood vessels.

How is ubrogepant processed by the body?

After it is swallowed, ubrogepant is absorbed quickly and reaches its highest level in the blood at about 1.5 hours, and levels rise in proportion to the dose across the recommended range. It can be taken with or without food. A high-fat meal slows absorption, delaying the peak level by about 2 hours and lowering it by about 22%, but the total amount absorbed does not change.

It has an elimination half-life of about 5 to 7 hours, which is the time the body takes to clear half of a dose.

Ubrogepant levels rise in people with reduced liver function, with exposure increasing by about 7% in mild, 50% in moderate, and 115% in severe liver impairment, so a dose adjustment is recommended for severe liver impairment. Mild or moderate kidney (renal) impairment does not meaningfully change its levels, but a dose adjustment is recommended for severe kidney impairment, and it has not been studied in people with end-stage kidney disease. Age, sex, race, and body weight do not have a meaningful effect on its levels, so no dose change is needed.

Yes. The generic name for Ubrelvy is ubrogepant. It is the active ingredient, and Ubrelvy is the brand name it is sold under in the United States. There is no generic version available, so the medicine is currently sold only as Ubrelvy.

Ubrogepant is one of several gepants used for migraine, and they differ mainly in whether they treat or prevent migraine. Ubrogepant (Ubrelvy) is used only for acute treatment. Rimegepant (Nurtec ODT) is used for both acute treatment and the prevention of episodic migraine. Atogepant (Qulipta) is used only for prevention, including episodic and chronic migraine, and is taken once daily.

Allergic reactions

Ubrogepant can cause serious allergic reactions (hypersensitivity), including anaphylaxis, trouble breathing, and swelling of the face or throat, as well as rash, hives, and itching. These can happen within minutes, hours, or even days of a dose. Stop taking it and get emergency medical help if you have any of these signs, and do not take ubrogepant again if you have ever had a serious allergic reaction to it.

High blood pressure (hypertension)

New or worsening high blood pressure (hypertension) has been reported with ubrogepant and other CGRP medicines, most often within the first 7 days of treatment, and some cases have needed blood pressure medicine or hospital care. Your blood pressure should be checked during treatment, and you should contact your doctor if it goes up.

Raynaud's phenomenon

Raynaud's phenomenon, a circulation problem in which the fingers or toes feel numb, cool, or painful and can change color from pale to blue to red, has been reported with ubrogepant and other CGRP medicines. Stop taking it and contact your doctor if these symptoms develop.

Do not take ubrogepant with strong CYP3A4 inhibitors, such as ketoconazole, clarithromycin, or itraconazole, because these medicines raise its levels in the body. Do not take it if you have ever had a serious allergic reaction (hypersensitivity) to ubrogepant or any of its ingredients.

Before taking ubrogepant, tell your doctor about all of your medical conditions, including if you have high blood pressure, circulation problems in your fingers or toes, liver problems, or kidney problems, and if you are pregnant, planning to become pregnant, or breastfeeding. Also tell your doctor about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements, because some can affect how it works.

Ubrogepant is processed by the liver enzyme CYP3A4 and is carried by two drug transporters (BCRP and P-gp), so medicines that block or speed up these can change how much ubrogepant is in the body. Ubrogepant itself is not expected to meaningfully change the levels of other medicines.

Strong CYP3A4 inhibitors, such as ketoconazole, itraconazole, and clarithromycin, can raise ubrogepant exposure by around 10-fold and should not be taken with ubrogepant. Moderate CYP3A4 inhibitors, including grapefruit juice, verapamil, cyclosporine, ciprofloxacin, fluconazole, and fluvoxamine, raise ubrogepant levels to a smaller degree (verapamil by about 3.5-fold), and with these you should not take a second dose within 24 hours (see the dosage section). A dose adjustment is also recommended with weak CYP3A4 inhibitors.

Strong CYP3A4 inducers, such as rifampin, phenytoin, barbiturates, and St. John's wort, lower ubrogepant exposure (rifampin by about 80%), which is expected to make ubrogepant stop working, so these should be avoided. A dose adjustment is recommended with moderate or weak CYP3A4 inducers.

Medicines that block the BCRP or P-gp transporters, such as quinidine, carvedilol, eltrombopag, and curcumin (turmeric), can also raise ubrogepant levels, so a dose adjustment is recommended with these.

Ubrogepant has not shown meaningful interactions with several commonly used medicines, including combined oral contraceptives (containing norgestimate and ethinyl estradiol), acetaminophen, naproxen, sumatriptan, esomeprazole, and the migraine preventives erenumab, galcanezumab, and atogepant.

This is not a complete list of interactions. Check all of your prescription and over-the-counter medicines, vitamins, and herbal supplements before starting ubrogepant.

The most common ubrogepant side effects are nausea and sleepiness (somnolence), and some people also report dry mouth. Serious reactions, including allergic reactions, high blood pressure, and Raynaud's phenomenon, are covered in the warnings section above. This is not a complete list of side effects, and others may occur.

The usual ubrogepant dose is 50 mg or 100 mg taken by mouth at the start of a migraine. If the migraine does not go away or it comes back, a second dose may be taken at least 2 hours after the first, up to a maximum of 200 mg in 24 hours. It can be taken with or without food. The safety of treating more than 8 migraines in 30 days is not known.

You should not take a second dose within 24 hours if you have had grapefruit or grapefruit juice, or if you take certain medicines, including:

• ciprofloxacin
• cyclosporine
• fluconazole
• fluvoxamine
• verapamil

There are no adequate studies of ubrogepant in pregnant women, and in animal studies high doses were linked to harm to the developing baby. Tell your doctor if you are pregnant or plan to become pregnant. There is a pregnancy registry for people who take it during pregnancy, which you can join by calling 1-833-277-0206 or visiting empresspregnancyregistry.com.

Only small amounts of ubrogepant pass into breast milk. Talk with your doctor if you are breastfeeding or plan to breastfeed.

Ubrogepant is made by AbbVie and is sold under the brand name Ubrelvy.

There is no generic version of ubrogepant, so its price follows the brand. For current pricing and savings options, see the Ubrelvy price guide (add internal link before publishing).