Berotralstat

Pronunciation: BER-oh-TRAL-stat
Brand name: Orladeyo
Dosage form: capsules (150 mg, 110 mg)
Drug class: Hereditary angioedema agents

Medically reviewed by Melisa Puckey, BPharm. Last updated on Feb 24, 2025.

What is Berotralstat?

Berotralstat (Orladeyo) is a prescription medication used to reduce the frequency of hereditary angioedema (HAE) attacks in patients 12 years and older. It works by inhibiting plasma kallikrein, an enzyme that contributes to excessive bradykinin production, which leads to swelling and inflammation in HAE. It is not used for the treatment of acute HAE attacks.

Berotralstat capsule is taken once daily with food 

Berotralstat brand name is Orladeyo, by BioCryst Pharmaceuticals, Inc.

Berotralstat FDA approval was granted for the prevention of recurrent HAE attacks in patients 12 years and older on December 3, 2020, after positive results from Clinical Trial 1 (NCT3485911). The results from 24-week Trial 1 demonstrated that Berotralstat patients had:

• 30% reduction in HAE attack rate 110mg daily
• 44.2% reduction in HAE attack rate 150mg daily

How does berotralstat work?

In hereditary angioedema, excessive kallikrein activity results in high levels of bradykinin, causing blood vessel leakage and swelling. 

Berotralstat mechanism of action is a plasma kallikrein inhibitor that binds to plasma kallikrein, reducing its activity and helping to prevent angioedema attacks.

Berotralstat side effects

Common berotralstat side effects

Common side effects of berotralstat include:

• Abdominal pain (16%)
• Vomiting (12%)
• Diarrhea (12%)
• Heartburn (7%)
• Back pain (6%)

These common side effects occurred in patients taking berotralstat 110mg or 50 mg once daily in 24-week (Part 1) data from a 3-part, double-blind parallel-group, placebo-controlled clinical trial Trial 1 (NCT3485911).  

Serious Side Effects

QT prolongation (irregular heart rhythm) – may occur if more than one capsule is taken per day. Do not take more than one capsule a day.

Severe allergic reactions – seek emergency help if you experience:

• Hives
• Swelling of face, lips, or throat
• Difficulty breathing

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 FDA at 1-800-FDA-1088.

Related/similar drugs

Warnings & Precautions

• QT Prolongation Risk: 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 or Kidney Disease: Inform your doctor before taking Orladeyo.
• Not Approved for Children Under 12.

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.

Berotralstat dosage & administration

• Recommended Dosage: One 150 mg capsule taken once daily with food.
• Dose adjustments may be necessary for patients with moderate or severe liver impairment or with persistent gastrointestinal GI reactions
• Do not take more than one capsule per day, as it may lead to serious heart rhythm issues (QT prolongation).

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?

Berotralstat 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.

Berotralstat Package Insert 

HCPs and patients often use the Berotralstat Package Insert (Orladeyo) for more detailed information about this medicine. The Package Insert (PI) 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 Berotralstat Prescribing Information or FDA label.

Storage & Handling

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

Ingredients

Active ingredient: berotralstat dihydrochloride

Orladeyo Inactive ingredients: colloidal silicon dioxide, crospovidone, magnesium stearate, and pregelatinized starch

Manufacturer Information

Orladeyo BioCryst Pharmaceuticals, Inc. – Durham, NC 27703

Further information

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

Medical Disclaimer