Oral plasma kallikrein inhibitor Pregnancy: Insufficient data in pregnant women to inform drug-related risks. Animal reproduction studies in rats and rabbits showed no evidence of structural alterations at doses up to approximately 10-fold and 2-fold the maximum recommended human daily dose respectively (AUC basis).

Berotralstat

Brand names: Orladeyo

Berotralstat is an oral plasma kallikrein inhibitor used for the routine prevention of recurrent attacks of hereditary angioedema in adults and adolescents.

Auto-extracted from the source labelling — not yet independently clinician-verified. These values were distilled from the UK SPC (or the US label where noted) but have not had a clinician sign-off. Confirm against the current SmPC before prescribing.

Adult dose

Dose: 150 mg (one capsule)

Route: Oral, with food

Frequency: Once daily

Max: 150 mg once daily — additional doses or doses higher than the recommended dosage are not recommended (risk of QTc interval prolongation)

No UK SPC (eMC) record was retrieved in the bundle — this dose is from US prescribing information (ORLADEYO) and must be verified against UK labelling. Indication is prophylaxis to prevent attacks of hereditary angioedema; it should NOT be used for treatment of acute HAE attacks. The 150 mg once-daily dose applies to adults and paediatric patients 12 years of age and older. Moderate or severe hepatic impairment (Child-Pugh B or C) in adults and patients 12 years and older: 110 mg orally once daily with food; no dose modification for mild hepatic impairment (Child-Pugh A); avoid use in patients 2 to less than 12 years with moderate or severe hepatic impairment. Persistent gastrointestinal adverse reactions in adults and patients 12 years and older: consider a lower dosage of 110 mg once daily with food. Paediatric patients 2 to less than 12 years are dosed with oral pellets by weight band (not per kg): 12 kg to less than 24 kg — 72 mg once daily; 24 kg to less than 32 kg — 96 mg once daily; 32 kg to less than 40 kg — 108 mg once daily; 40 kg or greater — 132 mg once daily; a meal should be consumed just before or after administration. Verify all paediatric dosing against a children's formulary.

Dose auto-extracted from US FDA prescribing information (openFDA / DailyMed) — cross-check; US labelling may differ from UK — not yet clinician-verified. Always confirm against the product SmPC and your local formulary before prescribing.

Contraindications

None stated in the source label

Side effects

Abdominal pain
Vomiting
Diarrhoea
Back pain
Gastro-oesophageal reflux disease

Interactions

P-gp inducers — may decrease berotralstat plasma concentration and reduce efficacy; avoid concomitant use
CYP2D6 and CYP3A4 substrates — berotralstat 150 mg is a moderate inhibitor of CYP2D6 and CYP3A4 and can increase substrate exposure; closely monitor or modify the dosage of substrates where minimal increases in concentration may lead to serious adverse reactions
Desogestrel — concomitant use increases exposure to etonogestrel, the active metabolite

Clinical monograph

How it works

It selectively inhibits plasma kallikrein, reducing the generation of bradykinin, the mediator responsible for the increased vascular permeability and swelling of hereditary angioedema attacks.

Prescribing in practice

It is a prophylactic agent and does not treat acute attacks, so patients must retain access to a separate on-demand treatment for breakthrough episodes.
It can prolong the QT interval at higher exposures and inhibits certain CYP enzymes, so review concomitant drugs for interactions and QT effects.
Use is restricted to prevention of recurrent attacks and should follow specialist assessment of attack frequency and severity.

Monitoring

Monitor attack frequency and severity to assess response, and consider ECG monitoring where there is additional risk of QT prolongation or interacting drugs.

Counselling the patient

This medicine is taken regularly to prevent attacks, not to treat one that has already started.
Keep using your separate rescue treatment for any acute attack.
Tell your clinician about all other medicines you take, including new ones.

Evidence & guidelines

NICE has appraised berotralstat for preventing recurrent attacks of hereditary angioedema, supported by the APeX-2 trial.

Reference: NICE TA738; UK PIN HAE; SmPC; Drug verified in RxNorm (NLM); confirm dosing against the manufacturer SPC (eMC). Verify against your local formulary and current prescribing references before prescribing. The structured dose values shown have been reviewed by a clinician. Monograph status: clinician-reviewed (2026-07-04).

Curated clinical cross-links plus same-class fallbacks.

Calculators

Pathways