Kalbitor

What is Kalbitor?

Kalbitor is a prescription medicine used to treat sudden attacks of hereditary angioedema (HAE) in people 12 years of age and older. Kalbitor is not a cure for HAE.

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

Description

KALBITOR (ecallantide) is a human plasma kallikrein inhibitor for injection for subcutaneous use. Ecallantide is a 60-amino-acid protein produced in Pichia pastoris yeast cells by recombinant DNA technology.

KALBITOR is a clear and colorless, sterile, and nonpyrogenic solution. Each vial contains 10 mg ecallantide as the active ingredient, and the following inactive ingredients: 0.76 mg disodium hydrogen orthophosphate (dihydrate), 0.2 mg monopotassium phosphate, 0.2 mg potassium chloride, and 8 mg sodium chloride in water for injection, USP. KALBITOR is preservative free, with a pH of approximately 7.0. A 30 mg dose is supplied as 3 vials each containing 1 mL of 10 mg/mL KALBITOR. Vials are intended for single use.

Mechanism of Action

Hereditary angioedema (HAE) is a rare genetic disorder caused by mutations to C1-esterase-inhibitor (C1-INH) located on Chromosome 11q and inherited as an autosomal dominant trait. HAE is characterized by low levels of C1-INH activity and low levels of C4. C1-INH functions to regulate the activation of the complement and intrinsic coagulation (contact system pathway) and is a major endogenous inhibitor of plasma kallikrein. The kallikrein-kinin system is a complex proteolytic cascade involved in the initiation of both inflammatory and coagulation pathways.

One critical aspect of this pathway is the conversion of High Molecular Weight (HMW) kininogen to bradykinin by the protease plasma kallikrein. In HAE, normal regulation of plasma kallikrein activity and the classical complement cascade is therefore not present. During attacks, unregulated activity of plasma kallikrein results in excessive bradykinin generation. Bradykinin is a vasodilator which is thought by some to be responsible for the characteristic HAE symptoms of localized swelling, inflammation, and pain.

KALBITOR is a potent (Ki = 25 pM), selective, reversible inhibitor of plasma kallikrein. KALBITOR binds to plasma kallikrein and blocks its binding site, inhibiting the conversion of HMW kininogen to bradykinin. By directly inhibiting plasma kallikrein, KALBITOR reduces the conversion of HMW kininogen to bradykinin and thereby treats symptoms of the disease during acute episodic attacks of HAE.

What is the most important information I should know about Kalbitor?

Serious allergic reactions may happen in some people who receive Kalbitor. These allergic reactions can be life-threatening and usually happen within 1 hour after receiving Kalbitor.

• Kalbitor should be given to you by a doctor or nurse in a healthcare setting where serious allergic reactions and hereditary angioedema (HAE) can be treated.
• Symptoms of a serious allergic reaction to Kalbitor can be similar to the symptoms of HAE, the condition that you are being treated for. Your doctor or nurse should watch you for any signs of a serious allergic reaction after treatment with Kalbitor.
• Tell your doctor or nurse right away if you have any of these symptoms of a serious allergic reaction during or after treatment with Kalbitor:
  • wheezing, shortness of breath, cough, chest tightness, or trouble breathing
  • dizziness, fainting, fast or weak heartbeat, or feeling nervous
  • reddening of the face, itching, hives, or feeling warm
  • swelling of the throat or tongue, throat tightness, hoarse voice, or trouble swallowing
  • runny nose, nasal congestion, or sneezing

Who should not use Kalbitor?

Do not receive Kalbitor if you are allergic to Kalbitor.

What should I tell my healthcare provider before using Kalbitor?

Before receiving Kalbitor, tell your doctor if you:

• have ever had an allergic reaction to Kalbitor. See “Who should not take Kalbitor?”.
• are pregnant or plan to become pregnant. It is not known if Kalbitor will harm your unborn baby.
• are breast-feeding or plan to breast-feed. It is not known if Kalbitor passes into your breast milk.

Tell your doctor about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements.

Know the medicines you take. Keep a list of them to show to your doctor and pharmacist when you get a new medicine.

How should I use Kalbitor?

For each dose, you will receive 3 injections just under the skin (subcutaneous or SC injections) of your abdomen, thigh, or upper arm.

What are the possible side effects of Kalbitor?

Kalbitor can cause serious allergic reactions. See “What is the most important information I should know about Kalbitor?”

Common side effects of Kalbitor include:

• headache
• nausea
• diarrhea
• fever
• injection site reactions, such as redness, rash, swelling, itching, or bruising
• stuffy nose

Call your doctor for 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 Kalbitor

Medicines are sometimes prescribed for purposes other than those listed in a Medication Guide. This Medication Guide gives you the most important information about Kalbitor. If you would like more information, talk with your doctor. You can ask your pharmacist or doctor for information about Kalbitor that is written for health professionals.

What are the ingredients in Kalbitor?

Active Ingredient: ecallantide

Inactive ingredients: disodium hydrogen orthophosphate (dihydrate), monopotassium phosphate, potassi

Label

PRINCIPAL DISPLAY PANEL – 10 MG/ML VIAL CARTON

• ATTENTION: Dispense the enclosed
  Medication Guide to each patient.
  NDC# 47783-101-01
• KALBITOR®
• ecallantide
• 10 mg/mL
  Injection
  For Subcutaneous Use Only
  Single Use; Discard Unused Portion
  Net Quantity: 3 Vials
• Rx Only