Tezosentan

Summary

Tezosentan (CHEMBL61780) is a phase-3 clinical-stage small molecule; indicated across 2 conditions including heart failure and pulmonary arterial hypertension.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Indications: 2 conditions
• Clinical trials: 5
• Chemistry: 605.6 Da · C27H27N9O6S

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL61780
Name	Tezosentan
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	151174
Molecular formula	C27H27N9O6S
Molecular weight	605.6
InChIKey	TUYWTLTWNJOZNY-UHFFFAOYSA-N

SMILES: CC(C)C1=CN=C(C=C1)S(=O)(=O)NC2=C(C(=NC(=N2)C3=CC(=NC=C3)C4=NNN=N4)OCCO)OC5=CC=CC=C5OC

IUPAC name: N-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-2-[2-(2H-tetrazol-5-yl)-4-pyridinyl]pyrimidin-4-yl]-5-propan-2-ylpyridine-2-sulfonamide

Also known as: ACT-050089, Ro-610612, Tezosentan, Veletri, TEZOSENTAN

Patent coverage: 1,756 distinct patent families (8,374 SureChEMBL compound mentions), from 3 matched compound structure(s). Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Broader ChEMBL bioactivity targets: 2 (assay-derived). Sample: Endothelin receptor type B, Endothelin-1 receptor.

Bioactivity

ChEMBL activities: 3 potent at pChembl ≥ 5 of 3 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
EDNRA	7.75	IC50	18	nM	CHEMBL_ACT_19405686
EDNRB	7.68	IC50	21	nM	CHEMBL_ACT_19405664
EDNRA	7.64	IC50	23	nM	CHEMBL_ACT_178403

Target pathways

No target-pathway data for this drug (no mapped target genes).

Indications & clinical

Indications

2 indications (0 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
heart failure	3	MONDO:0005252	EFO:0003144
pulmonary arterial hypertension	2	MONDO:0015924	EFO:0001361

Clinical trials

Total trials: 5.

Phase distribution

Phase	Trials
PHASE3	3
PHASE2	2

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00458276	PHASE3	TERMINATED	Study of the Efficacy and Safety of Tezosentan in Patients With Pre-operative Pulmonary Hypertension, Due to Left Heart Disease, Undergoing Open Heart Surgery
NCT00524433	PHASE3	COMPLETED	Tezosentan in the Treatment of Acute Heart Failure
NCT00525707	PHASE3	COMPLETED	Tezosentan in Acute Heart Failure
NCT01077297	PHASE2	TERMINATED	Tezosentan in Pulmonary Arterial Hypertension
NCT01094067	PHASE2	TERMINATED	Tezosentan in Patients With Pulmonary Arterial Hypertension

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Related molecules

Related molecules

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).