Sebetralstat

Plasma Kallikrein Inhibitor — BLOOD AND BLOOD FORMING ORGANS

Key facts

Sebetralstat is an onp drug in the Plasma Kallikrein Inhibitor class catalogued in DrugCentral. It was first approved by the FDA in 2025. Its mechanism of action is classified as Kallikrein Inhibitors. DrugCentral lists 1 molecular target, including KLKB1. Recorded indications include Hereditary angioneurotic edema.

• Approval status: onp (first approved 2025 by the FDA).
• Drug class: Plasma Kallikrein Inhibitor.
• Mechanism of action: Kallikrein Inhibitors.
• Molecular targets: KLKB1 (1 listed in DrugCentral).
• Indications: Hereditary angioneurotic edema.
• ATC code: B06AC08 (Drugs used in hereditary angioedema).
• Molecular formula: C26H26FN5O4; molecular weight 491.52 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (1)

• Hereditary angioneurotic edema

Mechanism & targets

• Mechanism of action (MoA): Kallikrein Inhibitors
• Established pharmacologic class: Plasma Kallikrein Inhibitor

Molecular targets (1)

Target	Gene	Action	Activity
Plasma kallikrein	KLKB1	inhibitor	Ki 5.52

Regulatory approvals (3)

Date	Agency	Marketed as	Applicant	Orphan
2025-12-22	PMDA	—	KalVista Pharmaceuticals Ltd.	Yes
2025-09-17	EMA	—	Kalvista Pharmaceuticals (Ireland) Limited	Yes
2025-07-03	FDA	—	KalVista Pharmaceuticals	Yes

ATC classification

ATC code	Therapeutic hierarchy
B06AC08	BLOOD AND BLOOD FORMING ORGANS › OTHER HEMATOLOGICAL AGENTS › OTHER HEMATOLOGICAL AGENTS › Drugs used in hereditary angioedema

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Hereditary angioedema	152.6

Chemical structure

Full physicochemical, ADMET and 3D-structure analysis of Sebetralstat is on its molecule page.

• Molecular formula: C₂₆H₂₆FN₅O₄
• Molecular weight: 491.52 g/mol
• CAS number: —
• InChIKey: KGMPDQIYDKKXRD-UHFFFAOYSA-N
• PubChem CID: 121365142

COCC1=NN(C=C1C(=O)NCC2=NC=CC(=C2F)OC)CC3=CC=C(C=C3)CN4C=CC=CC4=O

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Sebetralstat used for?

DrugCentral lists the following indications for Sebetralstat: Hereditary angioneurotic edema.

How does Sebetralstat work?

Sebetralstat is classified as Kallikrein Inhibitors; its molecular targets in DrugCentral include KLKB1 (inhibitor).

When was Sebetralstat first approved?

Sebetralstat was first approved by the FDA in 2025.

What drug class does Sebetralstat belong to?

Sebetralstat is in the Plasma Kallikrein Inhibitor class.

What is the chemical formula of Sebetralstat?

Sebetralstat has the molecular formula C26H26FN5O4 and a molecular weight of 491.52 g/mol.

Sources

• DrugCentral drug card 5779 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL5095248 — compound record and bioactivity
• PubChem CID 121365142 — chemical identifiers
• FDA UNII O5ZD2TU2B7 — substance identity
• DailyMed: FDA labels for Sebetralstat — current prescribing information (label search)
• UniProt P03952 (KLKB1) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral

How this page is built: methodology · editorial policy & corrections.