Plasma Kallikrein InhibitorPrescription OnlyPregnancy Cat. Not classifiedFDA Yes
Ekterly
SEBETRALSTAT
1 INDICATIONS AND USAGE EKTERLY® is indicated for the treatment of acute attacks of hereditary angioedema (HAE) in adult and pediatric patients aged 12 years and older. EKTERLY ® is a plasma kallikrein inhibitor indicated for the treatment of acute attacks of hereditary angioedema (HAE) in adult and pediatric patients aged 12 years and older. ( 1 )
Medically reviewed by MedCentralHub Medical Review Board, Licensed Pharmacists & Physicians ·
Brand names:EKTERLY
Quick Reference
Medicine ClassPlasma Kallikrein Inhibitor
FDA ApprovedYes
PregnancyCategory Not classified
Quick Facts
- Active ingredient
- SEBETRALSTAT
- Medicine class
- Plasma Kallikrein Inhibitor
- Brand names
- EKTERLY
- Availability
- Prescription only (Rx)
- Pregnancy category
- Not classified
- Half-life
- half-life of sebetralstat ranged from 5
- FDA approved
- Yes
What Is Ekterly?
1 INDICATIONS AND USAGE EKTERLY® is indicated for the treatment of acute attacks of hereditary angioedema (HAE) in adult and pediatric patients aged 12 years and older. EKTERLY ® is a plasma kallikrein inhibitor indicated for the treatment of acute attacks of hereditary angioedema (HAE) in adult and pediatric patients aged 12 years and older. ( 1 )
Ekterly (SEBETRALSTAT) belongs to the Plasma Kallikrein Inhibitor class of medications. It was first approved by the FDA in Yes. This medication requires a prescription from a licensed healthcare provider.
Key Safety Information
- •Always follow the dose recommended by your healthcare professional. Taking more than prescribed increases the risk of side effects including serious complications.
- •Seek emergency care if you experience signs of an allergic reaction — hives, swelling, difficulty breathing, or rash. Stop the medication and call your doctor immediately.
- •Some medications can increase the risk of cardiovascular events. Tell your doctor if you have high blood pressure, a history of heart attack or stroke, or any pre-existing health condition.
- •Avoid or limit alcohol while taking Ekterly. Do not drink alcohol without first discussing it with your healthcare provider as it may increase adverse effects.
- •Take Ekterly with food or a full glass of water if stomach upset occurs. Stop use and talk to your doctor if you experience persistent stomach pain or GI symptoms.
- •Tell your doctor about all medications, supplements, and vitamins you take. Some combinations significantly increase the risk of harm.
This is a summary only. Always read the full prescribing information and consult your healthcare provider for personalized medical advice.
Uses & Indications
Ekterly is prescribed for the following conditions. Some uses are FDA-approved indications; others may be evidence-based off-label uses. Consult your healthcare provider for personalized guidance.
1 INDICATIONS AND USAGE EKTERLY® is indicated for the treatment of acute attacks of hereditary angioedema (HAE) in adult and pediatric patients aged 12 years and older.
EKTERLY ® is a plasma kallikrein inhibitor indicated for the treatment of acute attacks of hereditary angioedema (HAE) in adult and pediatric patients aged 12 years and older.
Dosage Guide
The following are general dosing guidelines only. Your actual dose should be determined by your healthcare provider based on your condition, renal/hepatic function, and other medications.
AD
Adult Dosage
2 DOSAGE AND ADMINISTRATION Recommended Dosage : one dose of 600 mg (2 tablets) taken orally at the earliest recognition of an HAE attack. ( 2.1 ) A second dose of 600 mg (2 tablets) may be taken 3 hours after the first dose if response is inadequate, or if symptoms worsen or recur. ( 2.1 ) Maximum Recommended Dosage: 1,200 mg in any 24-hour period. ( 2.1 ) See full prescribing information for dosage modification for concomitant use with CYP3A4 inhibitors and inducers. ( 2.2 ) See full prescribing information for recommended dosage for patients with hepatic impairment. ( 2.3 ) 2.1 Recommended Dosage The recommended dosage of EKTERLY is one dose of 600 mg (two tablets) orally at the earliest recognition of an acute HAE attack. A second dose of 600 mg (two tablets) may be taken at least 3 hours after the first dose if response is inadequate, or if symptoms worsen or recur. Maximum recommended dosage is 1,200 mg (four tablets) in any 24-hour period. 2.2 Dosage Modification for CYP3A4 Inhi
Available Forms
Available Strengths
Side Effects
Common
- 6 ADVERSE REACTIONS The most common adverse reaction (incidence ≥2%) is headache.
- ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact KalVista Pharmaceuticals, Inc.
- at 1-855-258-4782 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.
- 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.
- The safety of EKTERLY is based on data from a double-blind, randomized, placebo-controlled, three-way, crossover clinical trial (KONFIDENT) [see Clinical Studies ( 14 )] .
- In KONFIDENT, a total of 110 patients aged 12 years and older with HAE treated 264 attacks.
- In the safety population, 93 patients received EKTERLY 600 mg, 86 patients received EKTERLY 300 mg, and 83 patients received placebo.
Serious
Rare
Medicine Interactions
Always inform your healthcare provider and pharmacist about ALL medications you take, including prescriptions, OTC medicines, vitamins, and supplements.
MajorModerateMinor
Warnings & Contraindications
How Ekterly Works
12.1 Mechanism of Action Sebetralstat is a competitive, reversible inhibitor of plasma kallikrein. Plasma kallikrein is a serine protease that cleaves high molecular weight kininogen (HK) releasing bradykinin which increases vascular permeability through activation of bradykinin receptors causing edema. Sebetralstat inhibits the cleavage of HK and reduces production of bradykinin, thereby treating the clinical symptoms of an acute, episodic attack of HAE. Sebetralstat also inhibits the positive feedback mechanism of the kallikrein kinin system by plasma kallikrein, thereby reducing factor XIIa and additional plasma kallikrein generation.
Pharmacokinetics
Absorption
Absorption After a single oral dose of 600 mg sebetralstat, the median time to peak plasma concentration is approximately 1 hour
Half-Life
half-life of sebetralstat ranged from 5
Metabolism
Metabolism Sebetralstat is primarily metabolized by CYP3A4 and to a lesser extent by CYP2C8
Excretion
Excretion Following administration of a single oral dose of 600 mg radiolabeled sebetralstat to healthy male subjects, approximately 63% of the dose was recovered in feces (12
Pregnancy & Breastfeeding Safety
Not classified
Breastfeeding
Many medications pass into breast milk in varying amounts. Before using Ekterlywhile breastfeeding, discuss the benefits and risks with your healthcare provider or pharmacist — they can weigh your dose, your infant's age, and available lactation safety data to find the safest option for you and your baby.
Storage & Handling
Store at room temperature. Keep away from moisture and heat. Keep out of reach of children.
Frequently Asked Questions
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Complete adverse effect profile including common, serious, and rare reactions
Sources & References
- • FDA Prescribing Information — Official labeling and package insert for Ekterly
- • U.S. National Library of Medicine — MedlinePlus drug information
- • American Hospital Formulary Service (AHFS) — Clinical pharmacology monograph
- • PubMed / MEDLINE — View clinical studies
Last reviewed by MedCentralHub Medical Review Board · MedCentralHub Editorial Policy
Medical Disclaimer
The information on this page is for educational purposes only and is not intended as medical advice, diagnosis, or treatment. Always consult your doctor, pharmacist, or qualified healthcare provider before starting, stopping, or changing any medication.