INDICATION
ORLADEYO® (berotralstat) is a plasma kallikrein inhibitor indicated for prophylaxis to prevent
attacks of hereditary angioedema (HAE) in adults and pediatric patients 12 years and older.
Limitations of use
The safety and effectiveness of ORLADEYO for the treatment of acute HAE attacks have not
been established. ORLADEYO should not be used for the treatment of acute HAE attacks.
Additional doses or dosages of ORLADEYO higher than 150 mg once daily are not recommended
due to the potential for QT prolongation.
IMPORTANT SAFETY INFORMATION
An increase in QT prolongation was observed at dosages higher than the recommended 150 mg
once-daily dosage and was concentration dependent.
The most common adverse reactions (≥10% and higher than placebo) in patients receiving ORLADEYO
were abdominal pain, vomiting, diarrhea, back pain, and gastroesophageal reflux disease.
A reduced dosage of 110 mg taken orally once daily with food is recommended in patients with
moderate or severe hepatic impairment (Child-Pugh B or C) and in patients taking chronically
administered P-glycoprotein (P-gp) or breast cancer resistance protein (BCRP) inhibitors (eg,
cyclosporine).
Berotralstat is a substrate of P-gp and BCRP. P-gp inducers (eg, rifampin, St. John’s wort) may
decrease berotralstat plasma concentration, leading to reduced efficacy of ORLADEYO. The use of
P-gp inducers is not recommended with ORLADEYO.
ORLADEYO at a dose of 150 mg is a moderate inhibitor of CYP2D6 and CYP3A4. For concomitant
medications with a narrow therapeutic index that are predominantly metabolized by CYP2D6 or
CYP3A4, appropriate monitoring and dose titration is recommended. ORLADEYO at a dose of 300 mg
is a P-gp inhibitor. Appropriate monitoring and dose titration is recommended for P-gp
substrates (eg, digoxin) when coadministering with ORLADEYO.
The safety and effectiveness of ORLADEYO in pediatric patients <12 years of age have not been
established.
There are insufficient data available to inform drug-related risks with ORLADEYO use in
pregnancy. There are no data on the presence of berotralstat in human milk, its effects on the
breastfed infant, or its effects on milk production.
To report SUSPECTED ADVERSE REACTIONS, contact BioCryst Pharmaceuticals, Inc. at 1-833-633-2279 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.
Please see full
Prescribing Information.
