Suramin

Summary

Suramin (CHEMBL265502) is a phase-3 clinical-stage small-molecule antinematodal drug targeting P2RY1, P2RY2, and P2RY6; indicated across 1 condition including non-small cell lung carcinoma.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Targets: 11 (P2RY1, P2RY2, P2RY6…)
• Indications: 1 condition
• Clinical trials: 17
• Chemistry: 1297.3 Da · C51H40N6O23S6

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL265502
Name	Suramin
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	5361
ChEBI	CHEBI:45906
Molecular formula	C51H40N6O23S6
Molecular weight	1297.3
InChIKey	FIAFUQMPZJWCLV-UHFFFAOYSA-N

SMILES: CC1=C(C=C(C=C1)C(=O)NC2=C3C(=CC(=CC3=C(C=C2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O)NC(=O)C4=CC(=CC=C4)NC(=O)NC5=CC=CC(=C5)C(=O)NC6=C(C=CC(=C6)C(=O)NC7=C8C(=CC(=CC8=C(C=C7)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O)C

IUPAC name: 8-[[4-methyl-3-[[3-[[3-[[2-methyl-5-[(4,6,8-trisulfonaphthalen-1-yl)carbamoyl]phenyl]carbamoyl]phenyl]carbamoylamino]benzoyl]amino]benzoyl]amino]naphthalene-1,3,5-trisulfonic acid

ChEBI definition: A member of the class of phenylureas that is urea in which each of the amino groups has been substituted by a 3-({2-methyl-5-[(4,6,8-trisulfo-1-naphthyl)carbamoyl]phenyl}carbamoyl)phenyl group. An activator of both the rabbit skeletal muscle RyR1 and sheep cardiac RyR2 isoform ryanodine receptor channels, it has been used for the treatment of human African trypanosomiasis for over 100 years.

Pharmacological roles (ChEBI): antinematodal drug, trypanocidal drug, ryanodine receptor agonist, GABA-gated chloride channel antagonist, GABA antagonist, apoptosis inhibitor, antineoplastic agent, angiogenesis inhibitor, purinergic receptor P2 antagonist, EC 2.7.11.13 (protein kinase C) inhibitor.

Also known as: Farma, FARMA-939, Fourneau, Metaret, Naganol, NSC-34936, Suramin, Suramine, suramine, suramin, Urea derivative, SID11114098

Parent form; salt/anhydrous children: CHEMBL413376

Patent coverage: 9,346 distinct patent families (36,848 SureChEMBL compound mentions), from 5 matched compound structure(s). One matched structure accounts for 36,649 (99%) 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
P2RY1	P2Y1 receptor	Antagonist	5.3	0%	P47900
P2RY2	P2Y2 receptor	Antagonist	4.3	1%	P41231
P2RY6	P2Y6 receptor	Antagonist	4	3.2%	Q15077
P2RY11	P2Y11 receptor	Antagonist	6	0%	Q96G91
P2RY13	P2Y13 receptor	Antagonist	5.6	0%	Q9BPV8
P2RX1	P2X1	Antagonist	6	0.3%	P51575
P2RX2	P2X2	Antagonist	4.98	2%	Q9UBL9
P2RX3	P2X3	Antagonist	4.83	1.6%	P56373
P2RX5	P2X5	Antagonist	5.4	0%	Q93086
RYR1	RyR1			1%	P21817
RYR2	RyR2			0.3%	Q92736

Broader ChEMBL bioactivity targets: 65 (assay-derived). Sample: Pyruvate kinase PKLR, Tyrosyl-DNA phosphodiesterase 1, Pyruvate kinase PKM, Microtubule-associated protein tau, Ubiquitin carboxyl-terminal hydrolase 2, ATP-dependent DNA helicase Q1, Inositol monophosphatase 1, 4’-phosphopantetheinyl transferase ffp, Histone-lysine N-methyltransferase 2A, Chromobox protein homolog 7, Bis(5’-adenosyl)-triphosphatase, Estrogen receptor, Menin/Histone-lysine N-methyltransferase MLL, Protein kinase C (PKC), P2X purinoceptor 1, P2X purinoceptor 4, P2X purinoceptor 2, 5-hydroxytryptamine receptor 1A, NAD-dependent protein deacylase sirtuin-5, mitochondrial, NAD-dependent protein lipoamidase sirtuin-4, mitochondrial.

Bioactivity

ChEMBL activities: 90 potent at pChembl ≥ 5 of 168 total. Top 100 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
TIMP3	8.72	Kd	1.9	nM	CHEMBL_ACT_25485231
SIRT1	7.57	IC50	27	nM	CHEMBL_ACT_22474669
SIRT1	7.46	IC50	35	nM	CHEMBL_ACT_22474672
ENPP3	7.4	Ki	40	nM	CHEMBL_ACT_24812539
P2RY11	6.95	Ki	112.2	nM	CHEMBL_ACT_1610537
ENPP1	6.58	Ki	260	nM	CHEMBL_ACT_16610260
ENPP1	6.58	Ki	260	nM	CHEMBL_ACT_18740695
P0DTD1	6.58	IC50	260	nM	CHEMBL_ACT_24980858
P0DTD1	6.58	IC50	260	nM	CHEMBL_ACT_25615959
P0DTD1	6.58	IC50	260	nM	CHEMBL_ACT_25848675
ENPP1	6.58	Ki	260	nM	CHEMBL_ACT_25874398
SIRT1	6.53	IC50	297	nM	CHEMBL_ACT_24824595
SIRT1	6.52	IC50	300	nM	CHEMBL_ACT_12178810
SIRT1	6.52	IC50	300	nM	CHEMBL_ACT_12705802
SIRT1	6.52	IC50	300	nM	CHEMBL_ACT_14926555
P2RY11	6.52	Ki	302	nM	CHEMBL_ACT_1610542
SIRT1	6.22	IC50	600	nM	CHEMBL_ACT_3069121
AGO2	6.16	IC50	690	nM	CHEMBL_ACT_25003402
P29990	6.12	Ki	750	nM	CHEMBL_ACT_19440555
P29990	6.12	Ki	750	nM	CHEMBL_ACT_19440562
ENPP1	6.11	Ki	780	nM	CHEMBL_ACT_18740696
ENPP3	6.05	IC50	890	nM	CHEMBL_ACT_22793228
ENPP3	6.05	IC50	890	nM	CHEMBL_ACT_23184367
ENPP3	6.05	IC50	900	nM	CHEMBL_ACT_25503763
P47824	6	IC50	1000	nM	CHEMBL_ACT_20648662
P47824	6	EC50	1000	nM	CHEMBL_ACT_32704
ENPP1	5.99	Ki	1030	nM	CHEMBL_ACT_18740698
ENPP1	5.97	Ki	1070	nM	CHEMBL_ACT_18740697
SIRT2	5.96	IC50	1100	nM	CHEMBL_ACT_12178808
PKLR	5.96	Ki	1100	nM	CHEMBL_ACT_24971769
SIRT2	5.94	IC50	1150	nM	CHEMBL_ACT_24824596
SIRT2	5.92	IC50	1200	nM	CHEMBL_ACT_12705799
ENPP3	5.9	IC50	1270	nM	CHEMBL_ACT_18308873
ENPP3	5.9	IC50	1270	nM	CHEMBL_ACT_18791970
ENPP3	5.9	IC50	1270	nM	CHEMBL_ACT_18885361
ENPP3	5.9	IC50	1270	nM	CHEMBL_ACT_18995170
NR1I2	5.89	EC50	1300	nM	CHEMBL_ACT_15465507
PTPN1	5.85	IC50	1420	nM	CHEMBL_ACT_18562060
KDR	5.81	AC50	1551	nM	CHEMBL_ACT_25168371
PRKDC	5.77	IC50	1700	nM	CHEMBL_ACT_1005123
SIRT5	5.7	IC50	2000	nM	CHEMBL_ACT_15186290
GABRA1	5.7	AC50	2010	nM	CHEMBL_ACT_25202843
SIRT4	5.7	IC50	2000	nM	CHEMBL_ACT_25966057
SIRT2	5.66	IC50	2200	nM	CHEMBL_ACT_22474674
PKLR	5.66	IC50	2200	nM	CHEMBL_ACT_24971766
RECQL	5.6	Potency	2512	nM	CHEMBL_ACT_5056288
SIRT1	5.58	IC50	2600	nM	CHEMBL_ACT_12147569
SIRT1	5.58	IC50	2620	nM	CHEMBL_ACT_17645700
SIRT5	5.56	IC50	2730	nM	CHEMBL_ACT_22474686
SIRT1	5.55	IC50	2800	nM	CHEMBL_ACT_10861324
SIRT1	5.55	IC50	2800	nM	CHEMBL_ACT_15645354
SIRT1	5.55	IC50	2800	nM	CHEMBL_ACT_18251088
PTPN1	5.54	IC50	2900	nM	CHEMBL_ACT_18401062
O15648	5.52	IC50	3000	nM	CHEMBL_ACT_13897649
SIRT5	5.52	IC50	3000	nM	CHEMBL_ACT_15186291
P2RX3	5.52	EC50	3000	nM	CHEMBL_ACT_32706
P97697	5.5	Potency	3162	nM	CHEMBL_ACT_4412007
USP2	5.48	Potency	3288	nM	CHEMBL_ACT_5052250
Q9EPX4	5.4	EC50	4000	nM	CHEMBL_ACT_32703
P51578	5.4	EC50	4000	nM	CHEMBL_ACT_32709
P49653	5.4	IC50	4000	nM	CHEMBL_ACT_5208498
ENTPD3	5.37	IC50	4310	nM	CHEMBL_ACT_18308915
P2RX1	5.37	IC50	4300	nM	CHEMBL_ACT_18416680
P2RX1	5.37	IC50	4270	nM	CHEMBL_ACT_19474502
ENTPD3	5.37	IC50	4300	nM	CHEMBL_ACT_22481997
TDP1	5.35	Potency	4467	nM	CHEMBL_ACT_3931870
P47824	5.33	IC50	4680	nM	CHEMBL_ACT_19474506
P2RX4	5.33	IC50	4730	nM	CHEMBL_ACT_24821344
TDP1	5.3	IC50	5000	nM	CHEMBL_ACT_19439593
TDP1	5.3	IC50	5000	nM	CHEMBL_ACT_19439603
PRMT1	5.27	IC50	5330	nM	CHEMBL_ACT_3515267
SIRT2	5.26	IC50	5444	nM	CHEMBL_ACT_24420906
P2RX4	5.25	IC50	5640	nM	CHEMBL_ACT_24801356
SIRT1	5.17	IC50	6700	nM	CHEMBL_ACT_19236671
MEN1	5.15	Potency	7080	nM	CHEMBL_ACT_4589528
HSPD1	5.14	IC50	7200	nM	CHEMBL_ACT_19209397
ENPP1	5.11	IC50	7770	nM	CHEMBL_ACT_22793218
ENPP1	5.11	IC50	7770	nM	CHEMBL_ACT_23184356
ENPP1	5.11	IC50	7770	nM	CHEMBL_ACT_25503757
HSD17B10	5.1	Potency	7943	nM	CHEMBL_ACT_3689483
CBX7	5.09	IC50	8100	nM	CHEMBL_ACT_18341262
ADORA3	5.07	AC50	8565	nM	CHEMBL_ACT_25198872
ENPP1	5.06	IC50	8670	nM	CHEMBL_ACT_18308859
ENPP1	5.06	IC50	8670	nM	CHEMBL_ACT_18740700
ENPP1	5.06	IC50	8670	nM	CHEMBL_ACT_18791991
ENPP1	5.06	IC50	8670	nM	CHEMBL_ACT_18885360
ENPP1	5.06	IC50	8670	nM	CHEMBL_ACT_18995123
HTR1A	5.04	AC50	9130	nM	CHEMBL_ACT_25165217
P0A6F5	5.01	Kd	9800	nM	CHEMBL_ACT_19209259
PKM	5	Ki	10000	nM	CHEMBL_ACT_24971767

Target pathways

Aggregated over 11 target gene(s): P2RY1, P2RY2, P2RY6, P2RY11, P2RY13, P2RX1, P2RX2, P2RX3, P2RX5, RYR1, RYR2.

Top Reactome pathways

16 total, by targets touching each:

Pathway	Targets	Genes
P2Y receptors	5	P2RY1, P2RY11, P2RY13, P2RY2, P2RY6
Elevation of cytosolic Ca2+ levels	4	P2RX1, P2RX2, P2RX3, P2RX5
G alpha (q) signalling events	4	P2RY1, P2RY11, P2RY2, P2RY6
Platelet homeostasis	4	P2RX1, P2RX2, P2RX3, P2RX5
Stimuli-sensing channels	2	RYR1, RYR2
Transport of small molecules	2	RYR1, RYR2
Muscle contraction	2	RYR1, RYR2
Cardiac conduction	2	RYR1, RYR2
Ion homeostasis	2	RYR1, RYR2
Ion channel transport	2	RYR1, RYR2
G alpha (s) signalling events	1	P2RY11
ADP signalling through P2Y purinoceptor 1	1	P2RY1
G alpha (i) signalling events	1	P2RY13
Surfactant metabolism	1	P2RY2
Neutrophil degranulation	1	P2RX1
High laminar flow shear stress activates signaling by PIEZO1 and PECAM1:CDH5:KDR in endothelial cells	1	P2RY2

Dominant GO biological processes

GO term	Targets
signal transduction	8
monoatomic ion transport	7
calcium ion transmembrane transport	6
monoatomic ion transmembrane transport	6
G protein-coupled receptor signaling pathway	5
G protein-coupled purinergic nucleotide receptor signaling pathway	5
phospholipase C-activating G protein-coupled receptor signaling pathway	4
establishment of localization in cell	4
cellular response to ATP	4
calcium-mediated signaling	4
response to ATP	4
purinergic nucleotide receptor signaling pathway	4
excitatory postsynaptic potential	4
monoatomic cation transmembrane transport	4
response to hypoxia	4

Indications & clinical

Indications

1 disease in clinical trials (phase 1–3, investigational — not approved indications). Highest ChEMBL trial phase per disease; a non-cancer approved use is occasionally logged at phase 3 here.

Disease (in trials)	Phase	MONDO	EFO
non-small cell lung carcinoma	2	MONDO:0005233	EFO:0003060

Clinical trials

Total trials: 17.

Phase distribution

Phase	Trials
PHASE2	8
PHASE1	4
PHASE1/PHASE2	3
PHASE3	2

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00002723	PHASE3	COMPLETED	Low, Intermediate, or High Dose Suramin in Treating Patients With Hormone-Refractory Prostate Cancer
NCT00002881	PHASE3	COMPLETED	Flutamide, Suramin, and Hydrocortisone in Treating Patients With Prostate Cancer
NCT00001266	PHASE2	COMPLETED	A Phase II Trial of Leuprolide + Flutamide + Suramin in Untreated Poor Prognosis Prostate Carcinoma
NCT00002639	PHASE2	COMPLETED	Suramin in Treating Patients With Recurrent Primary Brain Tumors
NCT00002652	PHASE2	COMPLETED	Suramin in Treating Patients With Refractory or Relapsed Multiple Myeloma or Castleman’s Disease
NCT00002921	PHASE2	TERMINATED	S9427, Suramin in Treating Patients With Stage III or Stage IV Adrenocortical Cancer Incurable by Surgery
NCT00004073	PHASE2	COMPLETED	Suramin Plus Radiation Therapy in Treating Patients With Newly Diagnosed Glioblastoma Multiforme
NCT00006929	PHASE2	COMPLETED	Suramin, Paclitaxel, and Carboplatin in Treating Patients With Stage IIIB or Stage IV Non-small Cell Lung Cancer
NCT00054028	PHASE1/PHASE2	COMPLETED	Suramin and Paclitaxel in Treating Women With Stage IIIB-IV Breast Cancer
NCT00083109	PHASE1/PHASE2	COMPLETED	Fluorouracil and Low-Dose Suramin as Chemosensitization in Treating Patients With Metastatic Renal Cell (Kidney) Cancer
NCT01671332	PHASE2	COMPLETED	Docetaxel +/- Suramin in 2nd Line Advanced Non-Small Cell Lung Cancer
NCT02508259	PHASE1/PHASE2	COMPLETED	University of California, San Diego (UCSD) Suramin Autism Treatment-1 (SAT1) Trial
NCT04496596	PHASE2	UNKNOWN	Study of Suramin in Subjects With Furosemide-Resistant AKI
NCT00001381	PHASE1	COMPLETED	A Phase I Trial Using Suramin to Treat Superficial Transitional Cell Carcinoma of the Bladder
NCT00003038	PHASE1	COMPLETED	Combination Chemotherapy With Suramin Plus Doxorubicin in Treating Patients With Advanced Solid Tumors
NCT00006476	PHASE1	COMPLETED	Suramin in Treating Patients With Recurrent Bladder Cancer
NCT00066768	PHASE1	COMPLETED	Suramin and Either Docetaxel or Gemcitabine in Treating Patients With Stage IIIB or Stage IV Platinum-Refractory Non-Small Cell Lung Cancer

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

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

22 molecules share ≥1 primary target. Top 22 by shared-target count:

Molecule	Source	Status	Shared targets
ADENOSINE TRIPHOSPHATE	ChEMBL	Phase 2	P2RX1, P2RX3, P2RY1, P2RY11, P2RY2
ADENOSINE	ChEMBL + PubChem	Phase 4 (approved)	P2RY1, P2RY11, P2RY2
CANGRELOR	ChEMBL + PubChem	Phase 4 (approved)	P2RX1, P2RY13
DIQUAFOSOL	ChEMBL	Phase 4 (approved)	P2RY2, P2RY6
DIQUAFOSOL TETRASODIUM	ChEMBL	Phase 4 (approved)	P2RY2, P2RY6
GEFAPIXANT	ChEMBL	Phase 4 (approved)	P2RX2, P2RX3
DENUFOSOL	ChEMBL	Phase 3	P2RY2, P2RY6
PYRIDOXAL	ChEMBL	Phase 3	P2RX1, P2RX2
URIDINE TRIPHOSPHATE	ChEMBL	Phase 3	P2RY2, P2RY6
ELIAPIXANT	ChEMBL	Phase 2	P2RX2, P2RX3
TICAGRELOR	ChEMBL + PubChem	Phase 4 (approved)	P2RY13
PROGESTERONE	ChEMBL	Phase 4 (approved)	P2RX3
DENUFOSOL TETRASODIUM	ChEMBL	Phase 3	P2RY2
ALADORIAN	ChEMBL	Phase 2	RYR2
SALFLUVERINE	ChEMBL	Phase 2	P2RX1
Belzutifan	PubChem	Approved	P2RY1
Caffeine	PubChem	Approved	RYR2
Carbachol	PubChem	Approved	P2RY2
Dantrolene	PubChem	Approved	RYR2
Indomethacin	PubChem	Approved	P2RY2
Oxolinic Acid	PubChem	Approved	RYR2
theophylline	PubChem	Approved	P2RX3