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Ekterly (SEBETRALSTAT)

Kalvista · FDA-approved active Small molecule Quality 45/100

Ekterly works by blocking the plasma kallikrein enzyme, which is involved in the production of bradykinin, a key mediator of HAE symptoms.

Ekterly (sebetralstat) is a small molecule plasma kallikrein inhibitor developed by Kalvista, approved by the FDA in 2025 for the treatment of hereditary angioedema (HAE). It works by inhibiting the plasma kallikrein enzyme, which plays a key role in the pathogenesis of HAE. Ekterly is a patented medication with no generic manufacturers available. Key safety considerations include the need for further studies to determine its long-term effects. As a plasma kallikrein inhibitor, Ekterly has the potential to interact with other medications that affect blood clotting.

At a glance

Generic nameSEBETRALSTAT
SponsorKalvista
Drug classPlasma Kallikrein Inhibitor [EPC]
ModalitySmall molecule
Therapeutic areaOther
PhaseFDA-approved
First approval2025

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.

Approved indications

Common side effects

Drug interactions

Key clinical trials

Patents

PatentExpiryType

Primary sources

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SourceUsed for
FDA labelMechanism, indications, dosing, boxed warnings, drug interactions
ClinicalTrials.govTrial enrolment, design, endpoints, results
FDA Orange BookPatents + exclusivity

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