Berotralstat
Hereditary angioedema agents
Hereditary angioedema agents
An oral small-molecule plasma kallikrein inhibitor taken daily to prevent hereditary angioedema attacks.
Quick facts
- Group
- Hereditary angioedema agents
- Target
- Plasma kallikrein (serine protease)
- Key effects
- Abdominal pain · Heartburn · Back pain
- Monitor
- Attack diary · ECG when there are QT risk factors
- ATC
- B06AC06
No doses: the clinician sets them by the current guideline.
Mechanism of action
The figure shows berotralstat in the active site of the human plasma kallikrein protease domain.
Berotralstat is a small molecule that fits into the active site of plasma kallikrein. The enzyme cannot cleave high-molecular-weight kininogen, so less bradykinin is produced. Taken every day, it lowers the number of attacks.
- Berotralstat enters the active site of plasma kallikrein
- Kininogen is no longer cut into bradykinin
- Daily intake keeps attacks less frequent
Indications
- Prevention of hereditary angioedema attacks Urticaria and angioedema →
Adverse effects
Common
- Abdominal pain, nausea, vomiting, diarrhoea
- Heartburn (reflux), gas or bloating
- Back pain
- Headache, tiredness, rash
Contraindications
- Hypersensitivity to berotralstat
- Caution with a history of long QT, and in liver or kidney disease
Key interactions
- P-glycoprotein or BCRP inhibitors (for example ciclosporin)
- Raise berotralstat levels; the label lowers the dose
- Other drugs that prolong the QT interval
- Add to the QT risk
What is monitored
- Attack diary
- ECG when there are QT risk factors
- Liver function in liver disease
Administration and safety
- Taken by mouth with a meal at about the same time each day
- Pellets are not chewed or crushed; they can be sprinkled on cool, non-acidic soft food and swallowed promptly
- It does not treat an acute attack
Pregnancy and breastfeeding
Pregnancy, plans for pregnancy or breastfeeding are discussed with the doctor; a pregnancy during treatment is reported at once.
Nursing care
- Review the medicine list for QT-prolonging drugs and P-gp inhibitors
- Teach to report palpitations, fainting or dizziness
- Check that an acute-attack plan is in place
- Explain that gut upset is common and usually passes
Pharmacokinetics
- Absorption
- Oral, once daily with a meal
Test yourself
Think of the answer, then tap the question to see it.
How is berotralstat given?
By mouth, once a day with food.
Which enzyme does it inhibit?
Plasma kallikrein.
Which ECG change is a concern at high exposure?
QT prolongation.
Connections
← Back to the class: Hereditary angioedema agents
Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.
Sources: Berotralstat: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2025); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026).
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Representative model, for educational purposes only.