Aprocitentan

Endothelin Receptor Antagonist — CARDIOVASCULAR SYSTEM

Key facts

Aprocitentan is an onp drug in the Endothelin Receptor Antagonist class catalogued in DrugCentral. It was first approved by the FDA in 2024. Its mechanism of action is classified as Endothelin Receptor Antagonists. DrugCentral lists 2 molecular targets, including EDNRA and EDNRB. Recorded indications include Hypertension.

• Approval status: onp (first approved 2024 by the FDA).
• Drug class: Endothelin Receptor Antagonist.
• Mechanism of action: Endothelin Receptor Antagonists.
• Molecular targets: EDNRA and EDNRB (2 listed in DrugCentral).
• Indications: Hypertension.
• ATC code: C02KN01 (Other antihypertensives).
• Molecular formula: C16H14Br2N6O4S; molecular weight 546.20 g/mol.

Indications & contraindications

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

Indications (1)

• Hypertension

Contraindications (1)

• Pregnancy, function

Mechanism & targets

• Mechanism of action (MoA): Endothelin Receptor Antagonists
• Established pharmacologic class: Endothelin Receptor Antagonist

Molecular targets (2)

Target	Gene	Action	Activity
Endothelin-1 receptor	EDNRA	antagonist	IC50 8.47
Endothelin B receptor	EDNRB	antagonist	IC50 6.01

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
2024-03-19	FDA	—	Idorsia Pharmaceuticals US Inc.

ATC classification

ATC code	Therapeutic hierarchy
C02KN01	CARDIOVASCULAR SYSTEM › ANTIHYPERTENSIVES › OTHER ANTIHYPERTENSIVES › Other antihypertensives

Chemical structure

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

• Molecular formula: C₁₆H₁₄Br₂N₆O₄S
• Molecular weight: 546.20 g/mol
• CAS number: —
• InChIKey: DKULOVKANLVDEA-UHFFFAOYSA-N
• PubChem CID: 25099191

C1=CC(=CC=C1C2=C(N=CN=C2OCCOC3=NC=C(C=N3)Br)NS(=O)(=O)N)Br

Frequently asked questions

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

What is Aprocitentan used for?

DrugCentral lists the following indications for Aprocitentan: Hypertension.

How does Aprocitentan work?

Aprocitentan is classified as Endothelin Receptor Antagonists; its molecular targets in DrugCentral include EDNRA (antagonist) and EDNRB (antagonist).

When was Aprocitentan first approved?

Aprocitentan was first approved by the FDA in 2024.

What drug class does Aprocitentan belong to?

Aprocitentan is in the Endothelin Receptor Antagonist class.

What is the chemical formula of Aprocitentan?

Aprocitentan has the molecular formula C16H14Br2N6O4S and a molecular weight of 546.20 g/mol.

Sources

• DrugCentral drug card 5812 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL2165326 — compound record and bioactivity
• PubChem CID 25099191 — chemical identifiers
• DrugBank DB15059 — drug record
• FDA UNII MZI81HV01P — substance identity
• DailyMed: FDA labels for Aprocitentan — current prescribing information (label search)
• UniProt P25101 (EDNRA) — target protein
• UniProt P24530 (EDNRB) — target protein

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