Dantrolene

Summary

Dantrolene (CHEMBL1201288) is an approved small molecule (ATC M03CA01) targeting RYR1 and RYR3; indicated across 4 conditions including injury and ventricular tachycardia.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: M03CA01
• Targets: 2 (RYR1, RYR3)
• Indications: 4 conditions
• Clinical trials: 9
• Chemistry: 314.25 Da · C14H10N4O5

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1201288
Name	Dantrolene
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	6914273
ATC	M03CA01
Molecular formula	C14H10N4O5
Molecular weight	314.25
InChIKey	OZOMQRBLCMDCEG-VIZOYTHASA-N

SMILES: C1C(=O)NC(=O)N1/N=C/C2=CC=C(O2)C3=CC=C(C=C3)[N+](=O)[O-]

IUPAC name: 1-[(E)-[5-(4-nitrophenyl)furan-2-yl]methylideneamino]imidazolidine-2,4-dione

Also known as: BAS-305, BAS-3050, BAS-3050F, Bebenil, Dantrolene, Dantroleno, F-368, Mebenil, NSC-227402, NSC-26404, O-methylbenzanilide, O-toluanilide

Parent form; salt/anhydrous children: CHEMBL928, CHEMBL2067986

Patent coverage: 2,710 distinct patent families (10,182 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 10,175 (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
RYR1	RyR1	Antagonist		1%	P21817
RYR3	RyR3	Antagonist		0%	Q15413

Broader ChEMBL bioactivity targets: 6 (assay-derived). Sample: Microtubule-associated protein tau, Prelamin-A/C, 4’-phosphopantetheinyl transferase ffp, CDGSH iron-sulfur domain-containing protein 1, Adenosine receptor A1, Bile salt export pump.

Bioactivity

ChEMBL activities: 3 potent at pChembl ≥ 5 of 8 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
CISD1	5.68	Ki	2065	nM	CHEMBL_ACT_16766195
LMNA	5.2	Potency	6310	nM	CHEMBL_ACT_3636654
MAPT	5	Potency	10000	nM	CHEMBL_ACT_4026844

Target pathways

Aggregated over 2 target gene(s): RYR1, RYR3.

Top Reactome pathways

6 total, by targets touching each:

Pathway	Targets	Genes
Stimuli-sensing channels	2	RYR1, RYR3
Transport of small molecules	2	RYR1, RYR3
Muscle contraction	2	RYR1, RYR3
Cardiac conduction	2	RYR1, RYR3
Ion homeostasis	2	RYR1, RYR3
Ion channel transport	2	RYR1, RYR3

Dominant GO biological processes

GO term	Targets
calcium ion transport	2
striated muscle contraction	2
release of sequestered calcium ion into cytosol by sarcoplasmic reticulum	2
release of sequestered calcium ion into cytosol	2
protein homotetramerization	2
cellular response to calcium ion	2
cellular response to caffeine	2
monoatomic ion transport	2
intracellular calcium ion homeostasis	2
calcium-mediated signaling	2
monoatomic ion transmembrane transport	2
transmembrane transport	2
calcium ion transmembrane transport	2
response to hypoxia	1
outflow tract morphogenesis	1

Indications & clinical

Indications

4 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
injury	2	MONDO:0021178	EFO:0000546
ventricular tachycardia	2	MONDO:0005477	EFO:0005306
multiple sclerosis	1	MONDO:0005301	MONDO:0005301

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

Clinical trials

Total trials: 9.

Phase distribution

Phase	Trials
PHASE2/PHASE3	3
PHASE1/PHASE2	3
PHASE2	3

Top trials by phase / activity

NCT	Phase	Status	Title
NCT06966843	PHASE2/PHASE3	NOT_YET_RECRUITING	Dantrolene in Statin-induced Myopathy
NCT00796900	PHASE2/PHASE3	TERMINATED	Dantrolene for Treatment of Hyperthermia in Subarachnoidal Hemorrhage (SAH)
NCT04134845	PHASE2/PHASE3	COMPLETED	A Clinical Trial Utilizing Dantrolene in Patients With Ventricular Arrhythmias.
NCT03109288	PHASE1/PHASE2	RECRUITING	Targeting Residual Activity By Precision, Biomarker-Guided Combination Therapies of Multiple Sclerosis (TRAP-MS)
NCT00964548	PHASE1/PHASE2	COMPLETED	Safety Study of Dantrolene to Treat Cerebral Vasospasm After Subarachnoid Hemorrhage
NCT01024972	PHASE1/PHASE2	COMPLETED	Safety Study of Dantrolene in Subarachnoid Hemorrhage
NCT01950520	PHASE2	COMPLETED	Study of Human Non-Shivering Thermogenesis and Basal Metabolic Rate
NCT02513095	PHASE2	COMPLETED	Efficacy and Safety of Ryanodex® (EGL-4104) as Adjuvant Treatment in Subjects With Exertional Heat Stroke (EHS)
NCT03762109	PHASE2	COMPLETED	The Use of Dantrolene to Improve Analgesia in Posterior Lumbar Surgery

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

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.

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

Molecule	Source	Status	Shared targets
Oxolinic Acid	PubChem	Approved	RYR3