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berotralstat

Plasma kallikrein inhibitor (HAE prophylaxis) · Hereditary Angioedema

START
150 mg PO once daily with food
TYPICAL MAX
150 mg/day (no added benefit, more QT risk above)
STOP IF
Significant QT prolongation or hepatotoxicity
WATCH
LFTs, ECG if QT-drug co-use; not for acute attacks
CDSCO approvedATC B06AC06
Renal dose adjustmenteGFR mL/min/1.73m²
FULLNo adjustment (mild–moderate)30AVOIDNot studied — avoid90

KDIGO 2024 + manufacturer label

Pharmacokineticsplasma · t hours
2hONSET5hPEAK3.9d1dDURATION
ONSET
2h · absorption
PEAK
5h · Tmax
3.9d ·
DURATION
1d · once-daily
EXCRETION
Mainly faecal; minor renal
route + CYP
INTERACTIONS
12 major
SEVERE in our sources
PREGNANCY
Limited data; use only if clearly needed.
FDA category + note
Top interactionssee all 12
  • AmprenavirSevereDatabaseDDInter
  • AvanafilSevereDatabaseDDInter
  • AzithromycinSevereDatabaseDDInter
  • BosutinibSevereDatabaseDDInter

Mechanism

Oral, selective inhibitor of plasma kallikrein, reducing bradykinin generation and thereby preventing hereditary angioedema attacks.

Indications

Routine prophylaxis to prevent hereditary angioedema (HAE) attacks (≥12 years)

Dosing

Adult
150 mg PO once daily with food.
Pediatric
≥12 y: 150 mg once daily (same as adult).
Renal adjustment
No adjustment for mild–moderate; not studied/avoid in severe (eGFR <30 / ESRD).
Hepatic adjustment
Moderate–severe impairment: not recommended (limited data).
Geriatric
No specific adjustment.
Max dose
150 mg/day (no benefit and more QT risk at higher doses)

Pharmacokinetics

Onset
Attack-rate reduction over weeks of prophylaxis
Peak effect
~5 h (Tmax)
Duration
~24 h (once-daily)
Half-life
~93 h
Bioavailability
Low-moderate; taken with food
Protein binding
~99%
Metabolism
Hepatic CYP2D6/CYP3A4; P-gp substrate/inhibitor
Excretion
Mainly faecal; minor renal

Contraindications

  • Hypersensitivity
  • Caution: QT prolongation at supratherapeutic doses; hepatic impairment

Side effects

Common
Abdominal painDiarrhoeaNausea/vomitingHeadacheBack painGERD
Serious
  • QT prolongation (supratherapeutic/with QT drugs)
  • Hypersensitivity
  • Transaminase elevation

Pregnancy & lactation

Pregnancy

Limited data; use only if clearly needed.

Lactation

Limited data; weigh benefit/risk.

Drug interactions

Amprenavir
Severe
Database

Drug interaction classified as: excretion

Source: DDInter

Avanafil
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Azithromycin
Severe
Database

Drug interaction classified as: absorption

Source: DDInter

Bosutinib
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Brexpiprazole
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Cabozantinib
Severe
Database

Drug interaction classified as: absorption

Source: DDInter

Capmatinib
Severe
Database

Drug interaction classified as: absorption

Source: DDInter

Carbamazepine
Severe
Database

Drug interaction classified as: excretion

Source: DDInter

Carvedilol
Severe
Database

Drug interaction classified as: absorption

Source: DDInter

Cefiderocol
Severe
Database

Drug interaction classified as: excretion

Source: DDInter

Ceritinib
Severe
Database

Drug interaction classified as: absorption

Source: DDInter

Cilostazol
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Related guidelines

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Sources: Goodman & Gilman 14e·Verified: 2026-05-20 · House clinical team·Cockpit curated: 2026-05-20