This website is intended for US healthcare professionals.

Mechanism
of Action

Real EKTERLY patient

EKTERLY delivers rapid PKa inhibition within minutes1,2

  • Dysregulated PKa Arrow

    In patients with HAE, PKa
    becomes dysregulated3

  • Increased vascular permeability Arrow

    Overactive PKa activity leads to
    increased vascular permeability3

  • Excessive fluid

    Excessive fluid leaks into surrounding
    tissues, resulting in edema3

  • EKTERLY® (sebetralstat) inhibiting PKa

    EKTERLY inhibits PKa1,4

EKTERLY is rapidly
absorbed in the stomach
and duodenum5,6

  • Absorption occurs higher in the gastrointestinal tract than where abdominal attacks most
    frequently occur5,6

After oral administration, PKa suppression begins in as little as

30
minutes (phase 1 trial)7
15
minutes (phase 2 trial)2

Based on healthy volunteers (n=6) in a phase 1 trial and HAE patients (n=12) in a phase 2 trial2,4,7

HAE=hereditary angioedema; PKa=plasma kallikrein.

Real EKTERLY® (sebetralstat) patient Zach talking on the phone Real EKTERLY® (sebetralstat) patient Zach talking on the phone Real EKTERLY patient
UP NEXT:
Patient SupportRight arrow

References:
1. EKTERLY. Package insert. KalVista Pharmaceuticals, Inc. 2025. 2. Aygören-Pürsün E, Zanichelli A, Cohn DM, et al. An investigational oral plasma kallikrein inhibitor for on-demand treatment of hereditary angioedema: a two-part, randomised, double-blind, placebo-controlled, crossover phase 2 trial. Lancet. 2023;401(10375):458-469. doi:10.1016/S0140-6736(22)02406-0 3. Busse P, Kaplan A. Specific targeting of plasma kallikrein for treatment of hereditary angioedema: a revolutionary decade. J Allergy Clin Immunol Pract. 2022;10(3):716-722. doi:10.1016/j.jaip.2021.11.011 4. Duckworth EJ, Murugesan N, Li L, et al. Pharmacological suppression of the kallikrein kinin system with KVD900: an orally available plasma kallikrein inhibitor for the on-demand treatment of hereditary angioedema. Clin Exp Allergy. 2022;52(9):1059-1070. doi:10.1111/cea.14122 5. Davie RL, Edwards HJ, Evans DM, et al. Sebetralstat (KVD900): a potent and selective small molecule plasma kallikrein inhibitor featuring a novel P1 group as a potential oral on-demand treatment for hereditary angioedema. J Med Chem. 2022;65(20):13629-13644. doi:10.1021/acs.jmedchem.2c00921 6. De Backer AI, De Schepper AM, Vandevenne JE, Schoeters P, Michielsen P, Stevens WJ. CT of angioedema of the small bowel. AJR Am J Roentgenol. 2001;176(3):649-652. doi:10.2214/ajr.176.3.1760649 7. Maetzel A, Smith MD, Duckworth EJ, et al. KVD900, an oral on-demand treatment for hereditary angioedema: Phase 1 study results. J Allergy Clin Immunol. 2022;149(6):2034-2042. doi:10.1016/j.jaci.2021.10.038

INDICATION AND IMPORTANT SAFETY INFORMATION

INDICATION

EKTERLY® (sebetralstat) 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.

IMPORTANT SAFETY INFORMATION

Adverse reactions: The most commonly reported adverse reaction was headache (3.2%).

Drug interactions: EKTERLY is a substrate of CYP3A4. Concomitant use of EKTERLY with a strong CYP3A4 inhibitor increases sebetralstat exposure, which may increase the risk of sebetralstat adverse reactions. Avoid use of EKTERLY with strong CYP3A4 inhibitors and reduce the dose of EKTERLY to one dose of 300 mg (one tablet) with moderate CYP3A4 inhibitors. Concomitant use of EKTERLY with a strong or moderate CYP3A4 inducer decreases sebetralstat exposure, which may decrease efficacy. The use of EKTERLY with strong or moderate CYP3A4 inducers is not recommended.

Use in specific populations: Avoid use of EKTERLY in patients with severe hepatic impairment (Child-Pugh Class C). The recommended dosage of EKTERLY is one dose of 300 mg (one tablet) in patients with moderate hepatic impairment (Child-Pugh Class B).

There are no available data on EKTERLY in pregnant women to evaluate for a drug-associated risk of major birth defects, miscarriage, or other adverse maternal or fetal outcomes. There are no data on the presence of sebetralstat or its metabolite in human milk, the effects on the breastfed infant, or the effects on milk production.

The safety and effectiveness of EKTERLY in pediatric patients aged under 12 years of age have not been established.

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.

Please see full Prescribing Information.