Sebetralstat

Sebetralstat
Clinical data
Trade namesEkterly
Other namesKVD-900, KVD900
License data
Routes of
administration
By mouth
ATC code
Legal status
Legal status
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
FormulaC26H26FN5O4
Molar mass491.523 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, sold under the brand name Ekterly, is a medication used for the treatment of hereditary angioedema.[1] Sebetralstat is a plasma kallikrein inhibitor.[1]

Sebetralstat was approved for medical use in the United States in July 2025.[1][2]

Medical uses

Sebetralstat is indicated for the treatment of acute attacks of hereditary angioedema.[1]

Pharmacology

Sebetralstat is a plasma kallikrein inhibitor that contains the unusual 2-pyridone heterocycle.[3]

Society and culture

Sebetralstat was approved for medical use in the United States in July 2025.[1] The US Food and Drug Administration granted the application for sebetralstat orphan drug designation.[4]

Names

Sebetralstat is the international nonproprietary name.[5]

Sebetralstat is sold under the brand name Ekterly.[1]

References

  1. ^ a b c d e f g "Ekterly- sebetralstat tablet". DailyMed. 7 July 2025. Retrieved 9 July 2025.
  2. ^ "KalVista Pharmaceuticals Announces FDA Approval of Ekterly (sebetralstat), First and Only Oral On-demand Treatment for Hereditary Angioedema" (Press release). Kalvista. 7 July 2025. Retrieved 9 July 2025 – via Business Wire.
  3. ^ Davie RL, Edwards HJ, Evans DM, Hodgson ST, Stocks MJ, Smith AJ, et al. (October 2022). "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". Journal of Medicinal Chemistry. 65 (20): 13629–13644. doi:10.1021/acs.jmedchem.2c00921. PMC 9620001. PMID 36251573.
  4. ^ "Sebetralstat Orphan Drug Designations and Approvals". U.S. Food and Drug Administration (FDA). Retrieved 9 July 2025.
  5. ^ World Health Organization (2022). "International nonproprietary names for pharmaceutical substances (INN): recommended INN: list 87". WHO Drug Information. 36 (1). hdl:10665/352794.
  • "Sebetralstat (Code - C184930)". EVS Explore.
  • Clinical trial number NCT05259917 for "A Phase III, Crossover Trial Evaluating the Efficacy and Safety of KVD900 (Sebetralstat) for On-Demand Treatment of Angioedema Attacks in Adolescent and Adult Patients With Hereditary Angioedema (HAE)" at ClinicalTrials.gov