Berotralstat
Berotralstat is an oral plasma kallikrein inhibitor used for the preventive treatment of hereditary angioedema (HAE) in adults and pediatric patients. By inhibiting plasma kallikrein, it reduces the production of bradykinin, a vasodilator that causes the characteristic swelling attacks in HAE patients. This medication offers a once-daily oral option for long-term prophylaxis of HAE attacks.
Berotralstat is an oral medication that prevents hereditary angioedema attacks by inhibiting the enzyme that produces bradykinin.
Key facts at a glance
- ATC
- B06AC06
- RxNorm
- 2467540
- Generic
- Berotralstat
- Class
- atc-b06
- Brands
- Orladeyo
- Availability
- rx
- Lactation
- unknown
- Routes
- oral
- Forms
- capsule
- Regions
- US, EU, CN, JP
- Monitoring
- —
This page is for informational purposes only.
Do not use this information to diagnose yourself or to replace a physician's advice. Always consult a qualified healthcare provider before starting, stopping, or changing any medication. If you believe you are experiencing a medical emergency, call your local emergency number immediately.
Dosage and administration
- Usual dose
- 150mg once daily
- Maximum
- consult physician
- Frequency
- once daily
- Instructions
- Follow physician instructions
- Duration limits
- as prescribed
- Monitoring
- standard
- Usual dose
- 150mg once daily
- Maximum
- consult physician
- Frequency
- once daily
- Instructions
- Follow physician instructions
- Duration limits
- as prescribed
- Monitoring
- standard
- Usual dose
- 150mg once daily
- Maximum
- consult physician
- Frequency
- once daily
- Instructions
- Follow physician instructions
- Duration limits
- as prescribed
- Monitoring
- standard
Overdose information
Special Populations
12 groupspregnancy
first trimesteravoid if possible
use only if benefits outweigh potential risks to fetus; consider continuing only if maternal HAE control is essential
regular prenatal monitoring and ultrasound assessments
Use with caution and monitor for adverse effects.
pregnancy
second trimesteravoid if possible
use only if benefits outweigh potential risks; continued use requires careful benefit-risk assessment
regular prenatal monitoring
Use with caution and monitor for adverse effects.
pregnancy
third trimesteravoid if possible
use only if benefits outweigh potential risks; discuss with healthcare provider
regular fetal monitoring
Use with caution and monitor for adverse effects.
lactation
breastfeedinguse with caution
decision to discontinue breastfeeding or discontinue drug should consider benefit of breastfeeding for infant and benefit of drug for mother
monitor infant for any adverse effects
pediatric_age
adolescents 12 to 17no adjustment needed
approved for use in patients 12 years and older for HAE prophylaxis; standard adult dosing applies
standard clinical monitoring for efficacy and safety
geriatric
elderly over 65no specific adjustment needed
use with caution due to potential increased sensitivity; start at standard dose and monitor response
monitor renal and hepatic function periodically; monitor for adverse effects
Use with caution and monitor for adverse effects.
renal_impairment
mildno adjustment needed
no dose adjustment required for mild renal impairment
standard clinical monitoring
renal_impairment
moderateno adjustment needed
no dose adjustment required; use with standard caution
monitor renal function periodically
Use with caution and monitor for adverse effects.
renal_impairment
severeuse with caution
use with caution; limited clinical data available for severe renal impairment
closely monitor for adverse effects and renal function
Use with caution and monitor for adverse effects.
hepatic_impairment
mildno adjustment needed
no dose adjustment required for mild hepatic impairment
standard clinical monitoring
hepatic_impairment
moderateno adjustment needed
use with caution; limited clinical data in moderate hepatic impairment
monitor hepatic function periodically
Use with caution and monitor for adverse effects.
hepatic_impairment
severeuse with caution
use with caution; limited clinical data available for severe hepatic impairment
closely monitor hepatic function and for adverse effects
Use with caution and monitor for adverse effects.
Statistics and clinical data
FDA approval year
FDA approved Berotralstat for hereditary angioedema prophylaxis
Drug class
Berotralstat is a selective plasma kallikrein inhibitor
Indication
Preventing attacks of hereditary angioedema in adults and pediatric patients 12 years and older
Standard dose
Oral tablet taken once daily with or without food
Prophylactic treatment of hereditary angioedema (HAE) in adults and children aged 12 years and older. It is specifically indicated for patients with HAE type I or II who have attacks related to plasma kallikrein activity.
Berotralstat binds directly to plasma kallikrein, inhibiting its proteolytic activity. This prevents the enzyme from cleaving high-molecular-weight kininogen (HMWK) into cleaved HMWK and bradykinin, thereby reducing bradykinin levels that cause vascular leakage and angioedema swelling.
Berotralstat is taken orally once daily with food. Common side effects may include abdominal pain, diarrhea, and vomiting. Patients should inform their healthcare provider of all medications as drug interactions can occur. It is not used for acute HAE attacks and should be continued as prescribed even when feeling well.
Contraindications
Conditions and patient states where this medication should be avoided or used with caution.
Do not use (1)
Known allergy to this medication or its components
Use caution (1)
Consult healthcare provider for benefits vs risks assessment
Official drug label
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This information is for educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment.
This content is for general informational and educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the guidance of a qualified healthcare provider with any questions you have about a medical condition, and never disregard professional medical advice or delay seeking it because of something you read here.
If you think you may have a medical emergency, call your local emergency number or go to the nearest emergency department immediately.
Medically reviewed by WellAlly Editorial Team Last reviewed July 26, 2026. · Read our editorial policy