Pronunciation: or-luh-DAY-oh
Generic name: berotralstat [ BER-oh-TRAL-stat ]
Dosage form: capsules (150 mg, 110 mg)
Drug class: Hereditary angioedema agents

Medically reviewed by Melisa Puckey, BPharm. Last updated on Mar 19, 2025.

What is Orladeyo?

Orladeyo is a preventative treatment used for hereditary angioedema (HAE) to help reduce the angioedema attack rate in adults and children at least 12 years old. Orladeyo works by blocking a protein called kallikrein which results in a reduction of swelling and inflammation in hereditary angioedema. 

Orladeyo capsules are taken once daily.

Orladeyo is not used for treating a hereditary angioedema attack that has already begun.

Hereditary angioedema is a rare and potentially life-threatening genetic disorder that causes an attack of rapid swelling in the face, throat, arms, legs, or around the abdomen. 

Orladeyo FDA approval is for the prevention of hereditary angioedema (HAE) attacks in adults and pediatric patients 12 years and older. The FDA approval was granted on  December 3, 2020, to BioCryst Pharmaceuticals, Inc.

How does Orladeyo work?

In people with hereditary angioedema, overactive kallikrein increases levels of bradykinin, a protein that causes blood vessels to widen and leak. This leads to the swelling and inflammation of angioedema attacks. 

Orladeyo mechanism of action is binding to plasma kallikrein which decreases plasma kallikrein activity and controls excess bradykinin generation in patients with HAE.  By inhibiting kallikrein, Orladeyo reduces the frequency of angioedema attacks.

Orladeyo (berotralstat) is from a class of medicines called kallikrein inhibitors.

How well does Orladeyo work?

Orladeyo was shown to be effective in treating hereditary angioedema, with positive results from a 48 week Clinical trial APeX-2 (NCT03485911), which demonstrated that Orladeyo patients had a:

• 67% reduction in hereditary angioedema attack rate using 150mg daily
• 52% reduction in hereditary angioedema attack rate using 110mg daily

Orladeyo side effects

Common Orladeyo side effects may include stomach pain (16%), heartburn (7%), vomiting (12%), diarrhea (12%), or back pain (6%). These were the common side effects that occurred in 10% or more of Orladeyo patients in the  24-week (Part 1) clinical trial called Trial 1.  

Serious side effects

Allergic reaction. Get emergency medical help if you have signs of an allergic reaction to this medicine with symptoms of hives; difficulty breathing; and swelling of your face, lips, tongue, or throat.

QT prolongation. Taking more than one capsule a day may cause serious side effects of heart rhythm problems. QT prolongation is a heart rhythm problem that can happen in people who take more than one capsule a day. This condition can cause an abnormal heartbeat. Do not take more than one capsule a day.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

Related/similar drugs

Warnings

QT Prolongation Risk: An increase in QT prolongation can occur at dosages higher than the recommended 150 mg once daily dosage. Do not exceed 150 mg per day.

Before taking this medicine

Before taking Orladeyo for HAE make sure this medicine is safe for you, tell your doctor if you have ever had:

• Liver disease
• Kidney Disease (or if you are on dialysis)
• Heart rhythm problems.

Orladeyo is not approved for use by anyone younger than 12 years old.

Pregnancy

Tell your healthcare professional if you are pregnant or planning to become pregnant as it is not known if Orladeyo can harm your unborn baby. 

Breastfeeding 

Tell your healthcare professional if you are breastfeeding or planning to breastfeed as it is not known if Orladeyo passes into breast milk. Talk to your healthcare professional about the best way to feed your baby.

Orladeyo Dosing Information

Recommended Orladeyo dosage: One capsule (150 mg) taken orally once daily with food.

Dose adjustment for ongoing GI reactions: Gastrointestinal side effects can occur in some patients. If these side effects persist a reduce dose of 110mg once daily with food may be considered.

Dose adjustment for hepatic impairment:

• No adjustment is required for mild hepatic impairment (Child-Pugh Class A)
• For Patients with moderate or severe hepatic impairment (Child-Pugh B or C)  the recommended dose is one 110 mg capsule taken orally once daily with food

What happens if I miss a dose?

• Take as soon as you remember.
• Skip the missed dose if it is almost time for your next dose.
• Do not double up on doses.

What happens if I overdose?

• Call the Poison Help Line (1-800-222-1222) or seek emergency medical attention immediately.

What other drugs will affect this medicine?

Orladeyo may interact with other medications, including:

• P-gp inducers - avoid use with Orladeyo.
• CYP2D6, CYP3A4, or P-gp substrates - monitor closely or dose titrate narrow therapeutic index medications that are predominantly metabolized by CYP2D6, CYP3A4 or are P-gp substrates when co-administered with Orladeyo.

Inform your doctor about all medications, vitamins, and supplements you are taking. Not all possible interactions are listed here.

Orladeyo Package Insert 

HCPs and patients often use the Orladeyo Package Insert (PI) for more detailed information about this medicine. The Package Insert contains more comprehensive information on Indications and Usage, Dosage and Administration, Clinical Pharmacology, Clinical Studies, Drug Interaction, and more. Discuss any medical questions you have with your doctor or other health care provider. This is not all the information you need to know about this medicine for safe and effective use, and it does not take the place of talking to your doctor about your treatment.

The Package Insert is sometimes called Orladeyo Prescribing Information (PI) or FDA label.

Storage & Handling

• Store at room temperature (68ºF–77ºF / 20ºC–25ºC).
• Keep out of reach of children.

Manufacturer Information

Orladeyo manufacturer BioCryst Pharmaceuticals, Inc. – Durham, NC 27703

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Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

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