Triamterene

Summary

Triamterene (CHEMBL585) is an approved small-molecule diuretic (ATC C03DB02); indicated across 13 conditions including cardiovascular disorder and nephrotic syndrome.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: C03DB02
• Indications: 13 conditions
• Clinical trials: 3
• Chemistry: 253.26 Da · C12H11N7

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL585
Name	Triamterene
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	5546
ChEBI	CHEBI:9671
ATC	C03DB02
Molecular formula	C12H11N7
Molecular weight	253.26
InChIKey	FNYLWPVRPXGIIP-UHFFFAOYSA-N

SMILES: C1=CC=C(C=C1)C2=NC3=C(N=C(N=C3N=C2N)N)N

IUPAC name: 6-phenylpteridine-2,4,7-triamine

ChEBI definition: Pteridine substituted at positions 2, 4 and 7 with amino groups and at position 6 with a phenyl group. A sodium channel blocker, it is used as a diuretic in the treatment of hypertension and oedema.

Pharmacological roles (ChEBI): diuretic, sodium channel blocker.

Also known as: Dyrenium, Dytac, NSC-639359, NSC-77625, SK&F 8542, SK&F-8542, SK-8542, Triamterene, Triamterene component of dyazide, Triamterene component of maxzide, Triamtereno, SID11111878

Patent coverage: 5,895 distinct patent families (21,663 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 21,659 (100%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
	ENaCαβγ		5.3

Broader ChEMBL bioactivity targets: 42 (assay-derived). Sample: Tyrosyl-DNA phosphodiesterase 1, Pyruvate kinase PKM, Lysine-specific demethylase 4E, Nuclear receptor ROR-gamma, Survival motor neuron protein, Prelamin-A/C, Inositol monophosphatase 1, Ferritin light chain, 15-hydroxyprostaglandin dehydrogenase [NAD(+)], Geminin.

Bioactivity

ChEMBL activities: 41 potent at pChembl ≥ 5 of 100 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
P08482	8.66	Potency	2.2	nM	CHEMBL_ACT_4807372
MAPK1	7.6	Potency	25.1	nM	CHEMBL_ACT_4533402
LMNA	7.35	Potency	44.7	nM	CHEMBL_ACT_3662417
TSHR	6.9	Potency	125.9	nM	CHEMBL_ACT_3924972
NFKB1	6.65	Potency	223.9	nM	CHEMBL_ACT_3672011
NFKB1	6.65	Potency	223.9	nM	CHEMBL_ACT_4585293
HPGD	6.15	Potency	707.9	nM	CHEMBL_ACT_4807633
KDM4E	5.95	Potency	1122	nM	CHEMBL_ACT_3740220
HSD17B10	5.9	Potency	1259	nM	CHEMBL_ACT_3688138
HPGD	5.6	Potency	2512	nM	CHEMBL_ACT_4788845
ALDH1A1	5.5	Potency	3162	nM	CHEMBL_ACT_4126087
ALDH1A1	5.5	Potency	3162	nM	CHEMBL_ACT_4168623
HSD17B10	5.5	Potency	3162	nM	CHEMBL_ACT_4833585
HSD17B10	5.5	Potency	3162	nM	CHEMBL_ACT_4849326
HSD17B10	5.5	Potency	3162	nM	CHEMBL_ACT_4849344
HSD17B10	5.5	Potency	3162	nM	CHEMBL_ACT_4853562
Q01782	5.47	Ki	3400	nM	CHEMBL_ACT_2979208
CASP1	5.44	IC50	3663	nM	CHEMBL_ACT_7786837
P25779	5.4	Potency	3981	nM	CHEMBL_ACT_3984613
HPGD	5.4	Potency	3981	nM	CHEMBL_ACT_4808782
JAK2	5.34	IC50	4613	nM	CHEMBL_ACT_4811512
HSD17B10	5.3	Potency	5012	nM	CHEMBL_ACT_3708668
KDM4E	5.3	Potency	5012	nM	CHEMBL_ACT_3723487
P15917	5.3	Potency	5012	nM	CHEMBL_ACT_4651813
CYP1A2	5.3	AC50	5012	nM	CHEMBL_ACT_6051298
P0A6C1	5.25	Potency	5623	nM	CHEMBL_ACT_4069613
SMN1	5.2	Potency	6310	nM	CHEMBL_ACT_3892628
CTSG	5.13	IC50	7413	nM	CHEMBL_ACT_7786839
HSD17B10	5.1	Potency	7943	nM	CHEMBL_ACT_3686655
KDM4E	5.1	Potency	7943	nM	CHEMBL_ACT_3711065

Target pathways

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

Indications & clinical

Indications

13 indications (8 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
cardiovascular disorder	4	MONDO:0004995	EFO:0000319
nephrotic syndrome	4	MONDO:0005377	EFO:0004255
congestive heart failure	4	MONDO:0005009	EFO:0000373
cirrhosis of liver	4	MONDO:0005155	EFO:0001422
hypertensive disorder	4	MONDO:0005044	EFO:0000537
hyperaldosteronism	4	MONDO:0003009	EFO:0009452
preeclampsia	4	MONDO:0005081	EFO:0000668
atherosclerosis	3	MONDO:0005311	EFO:0003914
coronary artery disorder	3	MONDO:0005010	EFO:0001645
type 2 diabetes mellitus	3	MONDO:0005148	MONDO:0005148

3 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 3.

Phase distribution

Phase	Trials
PHASE4	1
PHASE3	1
Not specified	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT02522650	PHASE4	UNKNOWN	A Crossover Pilot Study of the Effect of Amiloride on Proteinuria
NCT00000525	PHASE3	COMPLETED	Diuretics, Hypertension, and Arrhythmias Clinical Trial
NCT05125237	Not specified	COMPLETED	Data Analysis for Drug Repurposing for Effective Alzheimer’s Medicines (DREAM)- Amiloride vs Triamterene

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.

Related molecules

Related molecules

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