Berotralstat

Berotralstat is a prescription medication used for prevention of  hereditary angioedema attacks in adults and pediatric patients 12 years and older.

• Berotralstat is available under the following different brand names: Orladeyo

Common side effects of Berotralstat include:

• abdominal pain
• vomiting
• diarrhea
• back pain
• gastroesophageal reflux disease (GERD)

Serious side effects of Berotralstat include:

• hives
• difficulty breathing
• swelling of the face, lips, tongue, or throat
• abnormal heartbeat
• dizziness
• fainting

Rare side effects of Berotralstat include:

• none

Seek medical care or call 911 at once if you have the following serious side effects:

• Severe headache, confusion, slurred speech, arm or leg weakness, trouble walking, coordination loss, unsteady, very stiff muscles, high fever, profuse sweating, or tremors
• Serious eye symptoms such as sudden vision loss, blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights
• Serious heart symptoms include fast, irregular, or pounding heartbeats; fluttering in the chest; shortness of breath; sudden dizziness, lightheadedness, or passing out

This is not a complete list of side effects and other serious side effects or health problems that may occur because of the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may report side effects or health problems to FDA at 1-800-FDA-1088.

Adult and pediatric dosage

Capsule

• 110 mg
• 150 mg

Hereditary angioedema

Adult dosage

• 150 mg orally once a day

Pediatric dosage

• Children younger than 12 years: Safety and efficacy not established
• Children 12 years and older: 150 mg orally once a day

Dosage Considerations – Should be Given as Follows:

• See “Dosages”

If your medical doctor is using this medicine to treat your pain, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, healthcare provider, or pharmacist first.

• Berotralstat has severe interactions with the following drug:
  • lonafarnib
• Berotralstat has serious interactions with the following drugs:
  • carbamazepine
  • fosphenytoin
  • lorlatinib
  • phenobarbital
  • phenytoin
  • primidone
  • rifampin
  • St John's wort
  • tepotinib
  • tipranavir
  • vinblastine
• Berotralstat has moderate interactions with at least 179 other drugs.
• Berotralstat has minor interactions with the following drug:
  • verapamil

This information does not contain all possible interactions or adverse effects. Visit the RxList Drug Interaction Checker for any drug interactions. Therefore, before using this product, tell your doctor or pharmacist about all the products you use. Keep a list of all your medications with you and share this information with your doctor and pharmacist. Check with your healthcare professional or doctor for additional medical advice, health questions, or concerns.

Contraindications

• None

Effects of drug abuse

• None

Short-Term Effects

• See “What Are Side Effects Associated with Using Berotralstat?”

Long-Term Effects

• See “What Are Side Effects Associated with Using Berotralstat?”

Cautions

• QT prolongation may occur at dosages above 150 mg/day; additional doses or doses above 150 mg/day are not recommended
• Drug interaction overview
  • Berotralstat is a P-gp and BCRP substrate, a P-gp inhibitor, a moderate CYP2D6 inhibitor, and a weak CYP2D6 and CYP2C19 inhibitor
  • P-gp or BCRP inhibitors
  • Reduce berotralstat dose when coadministered
  • Cyclosporine, a P-gp and BCRP inhibitor, increased berotralstat peak plasma concentration by 25%, AUC(0-last) by 55%, and AUC(0-inf) by 69%
  • P-gp inducers
    • Avoid coadministration
    • P-gp inducers (eg, Rifampin, St. John’s wort) may decrease berotralstat plasma concentration and efficacy
  • CYP2D6 or CYP3A4
    • Monitor or titrate substrate dose when coadministered with narrow therapeutic index drugs that are CYP2D6 or CYP3A substrates
    • Berotralstat moderately inhibits CYP2D6 or CYP3A4 at the recommended dose (ie, 150 mg)
  • P-gp substrates
    • Monitoring or dose titration is recommended for P-gp substrates (eg, Digoxin)
    • Berotralstat inhibits P-gp at higher than the recommended dose (ie, 300 mg)

Pregnancy and Lactation

• Data available regarding the drug’s use in pregnant women are insufficient to inform drug-associated risks
• Lactation
  • There is no data on the presence of in human milk, effects on breastfed infants, or milk production
  • Low levels of berotralstat were detected in the plasma of rat pups when orally administered to dams during the lactation period; berotralstat concentration in pup plasma was approximately 2% of maternal plasma
  • When a drug is present in animal milk, it is likely that the drug will be present in human milk