[Durgical](https://durgical.com/en/) › [DurgiPedia](https://durgical.com/en/durgipedia/) › [Pharmacology](https://durgical.com/en/pharmacology/) › [Hereditary angioedema agents](https://durgical.com/en/pharmacology/classes/hereditary-angioedema-agents/) › Berotralstat

# Berotralstat

## Hereditary angioedema agents?

Hereditary angioedema agents

An oral small-molecule plasma kallikrein inhibitor taken daily to prevent hereditary angioedema attacks.

Updated Nov 1, 2026

## Quick facts

**Group**
[Hereditary angioedema agents](https://durgical.com/en/pharmacology/classes/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.

On this page

- The basics Mechanism of action
- Indications
- Adverse effects
- Pharmacokinetics
- Memory aid

- Safety Contraindications
- Key interactions
- What is monitored
- Administration and safety
- Pregnancy and breastfeeding
- Nursing care

- Study Test yourself

- Connections Connections

## Mechanism of action

✂**Plasma kallikrein (serine protease)**Berotralstat

ⓘ The figure shows berotralstat in the active site of the human plasma kallikrein protease domain.

**Target in 3D:** Plasma kallikrein (serine protease). PDB structure 7N7X (RCSB PDB, public domain). [View the structure at RCSB PDB](https://www.rcsb.org/structure/7N7X) · Drag to rotate · pinch to zoom

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 →](https://durgical.com/en/conditions/urticaria-and-angioedema/)

## Adverse effects

### Common

- Abdominal pain, nausea, vomiting, diarrhoea
- Heartburn (reflux), gas or bloating
- Back pain
- Headache, tiredness, rash

### Serious (rare, important)

- QT prolongation at doses above the recommended one (fast or pounding heartbeat, fainting)

## 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

## Memory aid

«BERO by mouth»: the only pill in the group, a daily kallikrein blocker.

## 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.

[Add to my cards (3)](https://durgical.app/estudiar/?add=/en/pharmacology/berotralstat/)

[More Pharmacology questions →](https://durgical.com/en/practice/?f=pharmacology)

## Connections

## Related drugs 3

- [Lanadelumab](https://durgical.com/en/pharmacology/lanadelumab/)
- [C1 esterase inhibitor](https://durgical.com/en/pharmacology/c1-esterase-inhibitor/)
- [Icatibant](https://durgical.com/en/pharmacology/icatibant/)

## Related conditions 1

- [Urticaria and angioedema](https://durgical.com/en/conditions/urticaria-and-angioedema/)

[← Back to the class: Hereditary angioedema agents](https://durgical.com/en/pharmacology/classes/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](https://medlineplus.gov/druginfo/meds/a626011.html) (MedlinePlus (U.S. National Library of Medicine), 2025); [ATCDDD - ATC/DDD Index](https://atcddd.fhi.no/atc_ddd_index/?code=B06AC&showdescription=no) (WHO Collaborating Centre for Drug Statistics Methodology, 2026).

## **Spotted a mistake?** We are always improving for the community. Tell us what is wrong and our team will review it. Report a mistake

Representative model, for educational purposes only.

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Source: https://durgical.com/en/pharmacology/berotralstat/
License: CC BY 4.0 (https://creativecommons.org/licenses/by/4.0/). Cite as: DurgiPedia (durgical.com), https://durgical.com/en/pharmacology/berotralstat/
