Orladeyo

What is Orladeyo?

Orladeyo is a prescription medicine used to prevent attacks of Hereditary Angioedema (HAE) in adults and children 12 years of age and older. Orladeyo is not used to treat an acute HAE attack.

Do not take more than one capsule of Orladeyo a day because extra doses can cause heart rhythm problems. It is not known if Orladeyo is safe and effective to treat an acute HAE attack.

It is not known if Orladeyo is safe and effective in children under 12 years of age.

Description

ORLADEYO (berotralstat) capsules is a plasma kallikrein inhibitor. Berotralstat is presented as the dihydrochloride salt with the chemical name 1-[3-(aminomethyl)phenyl]-N-(5-{(R)-(3-cyanophenyl)[(cyclopropylmethyl)amino]methyl}-2-fluorophenyl)-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide dihydrochloride. The chemical structure is:

Berotralstat dihydrochloride is a white to off-white powder that is soluble in water at pH ≤4. The molecular formula is C30H26F4N6O ∙ 2HCl and the molecular weight is 635.49 (dihydrochloride).

ORLADEYO is supplied as 150 mg (equivalent to 169.4 mg berotralstat dihydrochloride) and 110 mg (equivalent to 124.3 mg berotralstat dihydrochloride) hard gelatin capsules for oral administration. Each capsule contains the active ingredient berotralstat dihydrochloride and the inactive ingredients colloidal silicon dioxide, crospovidone, magnesium stearate, and pregelatinized starch.

Mechanism of Action

Berotralstat is a plasma kallikrein inhibitor that binds to plasma kallikrein and inhibits its proteolytic activity. Plasma kallikrein is a protease that cleaves high-molecular-weight-kininogen (HMWK) to generate cleaved HMWK (cHMWK) and bradykinin, a potent vasodilator that increases vascular permeability resulting in swelling and pain associated with HAE. In patients with HAE due to C1-inhibitor (C1-INH) deficiency or dysfunction, normal regulation of plasma kallikrein activity is not present, which leads to uncontrolled increases in plasma kallikrein activity and results in angioedema attacks. Berotralstat

What should I tell my healthcare provider before taking Orladeyo?

Before you take Orladeyo, tell your healthcare provider about all of your medical conditions, including if you:

• have liver problems or are on kidney dialysis.
• are pregnant or planning to become pregnant. It is not known if Orladeyo can harm your unborn baby.
• are breastfeeding or plan to breastfeed. It is not known if Orladeyo passes into your breastmilk. Talk to your healthcare provider about the best way to feed your baby while taking Orladeyo.

Tell your healthcare provider about all of the medicines you take, including other medicines for HAE, prescription and over-the-counter medicines, vitamins, and herbal supplements.
Taking Orladeyo with certain other medicines may affect the way other medicines work and other medicines may affect how Orladeyo works.
Know the medicines you take. Keep a list of them to show your healthcare provider and pharmacist when you get a new medicine.

How should I take Orladeyo?

• Take Orladeyo exactly as your healthcare provider tells you to take it.
• Take 1 capsule, by mouth, 1 time every day with food.

What are the possible side effects of Orladeyo?

Taking more than one capsule of Orladeyo a day may cause serious side effects, including:

• heart rhythm problems. A heart rhythm problem called QT prolongation can happen in people who take more than one capsule of Orladeyo a day. This condition can cause an abnormal heart beat. Do not take more than one capsule of Orladeyo a day.

The most common side effects of Orladeyo include:

• abdominal pain
• vomiting
• diarrhea
• back pain
• heartburn

Less common side effects include increases in liver function tests. Rarely, some patients had a brief, itchy rash.

These are not all of the possible side effects of Orladeyo. For more information, ask your healthcare provider or pharmacist.
Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

General information about the safe and effective use of Orladeyo

Medicines are sometimes prescribed for purposes other than those listed in a Patient Information leaflet. Do not use Orladeyo for a condition for which it was not prescribed. Do not give Orladeyo to other people, even if they have the same symptoms that you have. It may harm them. You can ask your pharmacist or healthcare provider for information about Orladeyo that is written for health professionals.

How should I store Orladeyo?

• Store Orladeyo at room temperature between 68ºF to 77ºF (20ºC to 25ºC).
• Each carton contains a tamper evident seal. Do not use Orladeyo if the tamper evident seal is broken or missing.

Keep Orladeyo and all medicines out of the reach of children.

What are the ingredients in Orladeyo?

Active ingredient: berotralstat dihydrochloride

Inactive ingredients: colloidal silicon dioxide, crospovidone, magnesium stearate, and pregelatinized starch

Label

PRINCIPAL DISPLAY PANEL – 150 MG CAPSULE BLISTER CARD SHELLPACK CARTON

• NDC 72769-101-01
  RX only
• orladeyo®
  (berotralstat) capsules 150 mg
• FOR ORAL USE ONLY
• 28 capsules
  Contains a 28-day supply
  4 shellpacks each containing a 7-capsule blister card
• bio cryst®

PRINCIPAL DISPLAY PANEL – 110 MG CAPSULE BLISTER CARD SHELLPACK CARTON

• NDC 72769-102-01
  RX only
• orladeyo®
  (berotralstat) capsules 110 mg
• FOR ORAL USE ONLY
• 28 capsules
  Contains a 28-day supply
  4 shellpacks each containing a 7-capsule blister card
• bio cryst®

SRC: NLM .