Sebetralstat

Last updated

Sebetralstat
Sebetralstat2.svg
Clinical data
Trade names EKTERLY
Other namesKVD-900, KVD900, Sebetralstat
AHFS/Drugs.com Ekterly
License data
Routes of
administration 		By mouth, Oral
ATC code
Legal status
Legal status
  • AU:TBD
  • US: ℞-only
  • EU:TBD
  • ℞ (Prescription only)
Identifiers
  • N-[(3-fluoro-4-methoxypyridin-2-yl)methyl]-3-(methoxymethyl)-1-[[4-[(2-oxopyridin-1-yl)methyl]phenyl]methyl]pyrazole-4-carboxamide
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
Chemical and physical data
Formula C26H26FN5O4
Molar mass 491.523 g·mol−1
3D model (JSmol)
  • COCC1=NN(C=C1C(=O)NCC2=NC=CC(=C2F)OC)CC3=CC=C(C=C3)CN4C=CC=CC4=O
  • InChI=1S/C26H26FN5O4/c1-35-17-22-20(26(34)29-13-21-25(27)23(36-2)10-11-28-21)16-32(30-22)15-19-8-6-18(7-9-19)14-31-12-4-3-5-24(31)33/h3-12,16H,13-15,17H2,1-2H3,(H,29,34)
  • Key:KGMPDQIYDKKXRD-UHFFFAOYSA-N

Sebetralstat is an oral on-demand therapy to treat acute hereditary angioedema (HAE) attacks. It is designed to reduce the severity and duration of HAE attacks by inhibiting plasma kallikrein, an enzyme that plays a key role in swelling during HAE attacks. Sebetralstat is marketed under the brand name EKTERLY and was approved by the U.S. Food and Drug Administration (FDA) in July 2025 for use in adults and children aged 12 years of age and older. It represents the first orally administered treatment option for acute HAE attacks. [1] [2]

Contents

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 (BK), which increases vascular permeability through activation of BK receptors, causing edema. Sebetralstat inhibits the cleavage of HK to BK, preventing activation of the BK receptors and halting the progression of HAE attacks. Sebetralstat also inhibits the positive feedback mechanism of the kallikrein kinin system by plasma kallikrein, thereby reducing factor XIIa and additional plasma kallikrein generation. [1]

Sebetralstat is administered orally, allowing for people with HAE to treat attacks at attack recognition. [1]

Society and culture

Sebetralstat was approved in the US by the FDA in July 2025 for the on-demand treatment of hereditary angioedema in adults and children aged 12 years of age and older. Regulatory submissions for approval in the European Union (EU) and other regions are ongoing. The drug is marketed as EKTERLY by KalVista Pharmaceuticals. [2]

References

  1. 1 2 3 "EKTERLY United States Prescribing Information V1.0 Approved" (PDF). www.kalvista.com. 7 July 2025. Retrieved 23 July 2025.
  2. 1 2 "KalVista Pharmaceuticals Announces FDA Approval of EKTERLY® (sebetralstat), First and Only Oral On-demand Treatment for Hereditary Angioedema". www.kalvista.com. 7 July 2025. Retrieved 23 July 2025.
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