Nimodipine

Summary

Nimodipine (CHEMBL1428) is an approved small-molecule antihypertensive agent (ATC C08CA06) targeting P2RX4, CACNA1S, and CACNA1C; indicated across 11 conditions including cardiovascular disorder and subarachnoid hemorrhage.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: C08CA06
• Targets: 7 (P2RX4, CACNA1S, CACNA1C…)
• Indications: 11 conditions
• Clinical trials: 32
• Chemistry: C21H26N2O7

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1428
Name	Nimodipine
Type	Small molecule
Max phase	4
ChEBI	CHEBI:7575
ATC	C08CA06
Molecular formula	C21H26N2O7
InChIKey	UIAGMCDKSXEBJQ-UHFFFAOYSA-N

SMILES: COCCOC(=O)C1=C(C)NC(C)=C(C(=O)OC(C)C)C1c1cccc([N+](=O)[O-])c1

ChEBI definition: A dihydropyridine that is 1,4-dihydropyridine which is substituted by methyl groups at positions 2 and 6, a (2-methoxyethoxy)carbonyl group at position 3, a m-nitrophenyl group at position 4, and an isopropoxycarbonyl group at position 5. An L-type calcium channel blocker, it acts particularly on cerebral circulation, and is used both orally and intravenously for the prevention and treatment of subarachnoid hemorrhage from ruptured intracranial aneurysm.

Pharmacological roles (ChEBI): antihypertensive agent, calcium channel blocker, vasodilator agent, cardiovascular drug.

Also known as: Admon, BAY E 9736, BAY-E-9736, Nemotan, Nimodipine, Nimodipine ap, Nimodipino, Nimotop, NSC-758476, Nymalize, Periplum, nimodipine

Patent coverage: 10,519 distinct patent families (32,587 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 32,536 (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
P2RX4	P2X4	Positive		1.2%	Q99571
CACNA1S	Cav1.1	Antagonist	6	0.2%	Q13698
CACNA1C	Cav1.2	Antagonist	6.8	0.1%	Q13936
CACNA1D	Cav1.3	Antagonist	6.6	0.3%	Q01668
CACNA1F	Cav1.4	Antagonist	6	0%	O60840
NR3C2	Mineralocorticoid receptor	Antagonist	6.8	0%	P08235
CFTR	CFTR	Potentiation		0.1%	P13569

Broader ChEMBL bioactivity targets: 35 (assay-derived). Sample: Transient receptor potential cation channel subfamily A member 1, Microtubule-associated protein tau, Prelamin-A/C, RecQ-like DNA helicase BLM, Ferritin light chain, Endonuclease 4, Peripheral myelin protein 22, 5-hydroxytryptamine receptor 2B, Voltage-dependent L-type calcium channel subunit alpha-1C, Sodium channel protein type 5 subunit alpha.

Bioactivity

ChEMBL activities: 33 potent at pChembl ≥ 5 of 50 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
LMNA	8.74	Potency	1.8	nM	CHEMBL_ACT_3625713
LMNA	8.35	Potency	4.5	nM	CHEMBL_ACT_3645334
P22002	7.74	AC50	18.3	nM	CHEMBL_ACT_25119636
CACNA2D1	7.53	IC50	29.8	nM	CHEMBL_ACT_24929469
CACNA1C	6.96	IC50	110	nM	CHEMBL_ACT_15373264
O35505	6.52	IC50	300	nM	CHEMBL_ACT_15373263
NR1I2	6.41	EC50	390	nM	CHEMBL_ACT_13362894
CACNA1C	6.38	AC50	420	nM	CHEMBL_ACT_25159098
NR1I2	6.18	AC50	661.8	nM	CHEMBL_ACT_25188215
Q8BLA8	6.1	EC50	800	nM	CHEMBL_ACT_3301112
NR1I2	6.04	AC50	907.6	nM	CHEMBL_ACT_25224367
CYP2C9	6	IC50	1000	nM	CHEMBL_ACT_7727087
PDE1C	5.91	IC50	1243	nM	CHEMBL_ACT_24929398
PDE1C	5.91	IC50	1243	nM	CHEMBL_ACT_25955581
CNR1	5.86	Ki	1371	nM	CHEMBL_ACT_7727062
NPSR1	5.8	Potency	1585	nM	CHEMBL_ACT_4944704
CYP2C9	5.77	IC50	1690	nM	CHEMBL_ACT_15450947
CNR1	5.76	IC50	1736	nM	CHEMBL_ACT_7727061
CYP3A4	5.75	IC50	1780	nM	CHEMBL_ACT_15450987
PDE1A	5.7	IC50	2000	nM	CHEMBL_ACT_25955598
CYP2C19	5.66	IC50	2170	nM	CHEMBL_ACT_15450927
SLC29A1	5.5	AC50	3200	nM	CHEMBL_ACT_25141593
CYP2J2	5.47	IC50	3380	nM	CHEMBL_ACT_15461594
CYP2C19	5.4	IC50	4000	nM	CHEMBL_ACT_7727085
ABCB11	5.35	AC50	4500	nM	CHEMBL_ACT_25127038
PDE4D	5.32	AC50	4800	nM	CHEMBL_ACT_25185383
SCN5A	5.22	AC50	6000	nM	CHEMBL_ACT_25158924
PDE4D	5.15	IC50	7150	nM	CHEMBL_ACT_24929481
CYP1A2	5.14	IC50	7200	nM	CHEMBL_ACT_15449398
NR3C1	5.07	AC50	8600	nM	CHEMBL_ACT_25175899

Target pathways

Aggregated over 7 target gene(s): P2RX4, CACNA1S, CACNA1C, CACNA1D, CACNA1F, NR3C2, CFTR.

Top Reactome pathways

39 total, by targets touching each:

Pathway	Targets	Genes
Developmental Biology	3	CACNA1C, CACNA1D, CACNA1S
NCAM signaling for neurite out-growth	3	CACNA1C, CACNA1D, CACNA1S
NCAM1 interactions	3	CACNA1C, CACNA1D, CACNA1S
Axon guidance	3	CACNA1C, CACNA1D, CACNA1S
Nervous system development	3	CACNA1C, CACNA1D, CACNA1S
Metabolism	2	CACNA1C, CACNA1D
Integration of energy metabolism	2	CACNA1C, CACNA1D
Adrenaline,noradrenaline inhibits insulin secretion	2	CACNA1C, CACNA1D
Regulation of insulin secretion	2	CACNA1C, CACNA1D
Elevation of cytosolic Ca2+ levels	1	P2RX4
Cellular responses to stress	1	NR3C2
SUMOylation	1	NR3C2
SUMO E3 ligases SUMOylate target proteins	1	NR3C2
HSP90 chaperone cycle for steroid hormone receptors (SHR) in the presence of ligand	1	NR3C2
ABC-family protein mediated transport	1	CFTR
Nuclear Receptor transcription pathway	1	NR3C2
Metabolism of proteins	1	NR3C2
Muscle contraction	1	CACNA1C
SUMOylation of intracellular receptors	1	NR3C2
Platelet homeostasis	1	P2RX4
Cardiac conduction	1	CACNA1C
Phase 0 - rapid depolarisation	1	CACNA1C
Phase 2 - plateau phase	1	CACNA1C
RHO GTPases regulate CFTR trafficking	1	CFTR
Defective CFTR causes cystic fibrosis	1	CFTR
Ub-specific processing proteases	1	CFTR
Post-translational protein modification	1	NR3C2
Cargo recognition for clathrin-mediated endocytosis	1	CFTR
Clathrin-mediated endocytosis	1	CFTR
Cellular responses to stimuli	1	NR3C2

Dominant GO biological processes

GO term	Targets
monoatomic ion transmembrane transport	6
monoatomic ion transport	6
calcium ion transmembrane transport	5
transmembrane transport	5
calcium ion transport	4
calcium ion import across plasma membrane	4
muscle contraction	3
signal transduction	2
positive regulation of calcium ion transport	2
regulation of metal ion transport	2
positive regulation of muscle contraction	2
system process	2
positive regulation of adenylate cyclase activity	2
cardiac muscle cell action potential involved in contraction	2
membrane depolarization during cardiac muscle cell action potential	2

Indications & clinical

Indications

11 indications (1 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
subarachnoid hemorrhage	3	MONDO:0005099	EFO:0000713
poisoning	3	MONDO:0029000	EFO:0008546
infertility disorder	2	MONDO:0005047	EFO:0000545
stroke disorder	2	MONDO:0005098	EFO:0000712
cocaine dependence	2	MONDO:0005186	EFO:0002610
acoustic neuroma	2	MONDO:0001569	HP:0009588
brain aneurysm	1	MONDO:0005291	EFO:0003870
cerebrovascular disorder	0	MONDO:0011057	EFO:0003763

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

Clinical trials

Total trials: 32.

Phase distribution

Phase	Trials
Not specified	8
PHASE2	7
PHASE4	5
PHASE1	5
PHASE3	3
EARLY_PHASE1	3
PHASE1/PHASE2	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00781326	PHASE4	TERMINATED	Effectiveness of Nimodipine Plus Antidepressant Medication in Treating Vascular Depression
NCT00814658	PHASE4	COMPLETED	The Use of Galantamine (Reminyl ER) in Patients With MIXed Dementia: Effects on Cognition and Quality of Life
NCT01220622	PHASE4	UNKNOWN	Efficacy and Safety Study of Nimodipine to Prevent Mild Cognitive Impairment After Acute Ischemic Strokes
NCT02248233	PHASE4	COMPLETED	Nimodipine for Treating Acute Massive Cerebral Infarction
NCT03150524	PHASE4	WITHDRAWN	RCVS: The Rational Approach to Diagnosis and Treatment
NCT07144956	PHASE3	NOT_YET_RECRUITING	Cilostazol With Nimodipine to Improve Outcome After Aneurysmal Subarachnoid Hemorrhage
NCT02790632	PHASE3	TERMINATED	Study of EG-1962 Compared to Standard of Care Oral Nimodipine in Adults With Aneurysmal Subarachnoid Hemorrhage
NCT03925025	PHASE3	COMPLETED	Effectiveness of Calcium Channel Blockade for OP and Carbamate Pesticide Poisoning
NCT06900998	PHASE2	NOT_YET_RECRUITING	Pilot Study: Effects of Nimodipine on Alcohol Drinking
NCT00000332	PHASE2	COMPLETED	High Dose Nimodipine Treatment Adjunct - 1
NCT01551368	PHASE2	TERMINATED	Use of a Calcium Channel Blocker to Prevent Premature Luteinizing Hormone Surges in Infertility Patients
NCT01893190	PHASE1/PHASE2	COMPLETED	Safety and Tolerability Study of EG-1962 in Aneurysmal Subarachnoid Hemorrhage
NCT02165644	PHASE2	WITHDRAWN	Carbonic Anhydrase Antagonism in Subarachnoid Hemorrhage
NCT04028596	PHASE2	COMPLETED	Measuring Blood Flow in the Brain After Epileptic Activity
NCT04100824	PHASE2	COMPLETED	Stellate Ganglion Block as Adjuvant Therapy to ca Channel Blocker
NCT05131867	PHASE2	COMPLETED	Management of Cerebral Vascular Spasm in Posttraumatic Subarachnoid Hemorrhage Using Combination Therapy
NCT00000280	PHASE1	COMPLETED	Glutaminergic Agents for Cocaine Abuse - 5
NCT00000738	PHASE1	COMPLETED	Randomized, Double-Blind, Placebo-Controlled Trial of Nimodipine for the Neurological Manifestations of HIV-1
NCT01835665	PHASE1	COMPLETED	Dose Finding Study of Nimodipine for the Treatment of Progranulin Insufficiency From GRN Gene Mutations
NCT02893826	PHASE1	TERMINATED	Safety/Pharmacokinetic Study Comparing Intracisternal EG-1962 to Standard of Care Enteral Nimodipine in Adults With aSAH
NCT05418348	PHASE1	COMPLETED	Relative Bioavailability of Intravenous GTX-104 Compared to Oral Nimodipine Capsules in Healthy Subjects
NCT04923659	EARLY_PHASE1	ACTIVE_NOT_RECRUITING	Pharmacological Mechanisms of Low-intensity Focused Ultrasound for Motor Cortex Neuroplasticity
NCT03671525	EARLY_PHASE1	COMPLETED	Cognitive Effects of Nimodipine in Patients With Schizophrenia
NCT03794843	EARLY_PHASE1	UNKNOWN	Bioavailability Comparison Study of Two Types of Nimodipine Injections in Healthy Volunteers
NCT06998368	Not specified	RECRUITING	A Causal Role for Voltage-gated Cav1.2 Calcium Channels in Mediating 5G FR1 Effects on Sleep-associated Brain Health in Humans
NCT07048522	Not specified	RECRUITING	Perioperative Intravenous Nimodipine Trial
NCT00004399	Not specified	COMPLETED	Randomized Study of Nimodipine Versus Magnesium Sulfate in the Prevention of Eclamptic Seizures in Patients With Severe Preeclampsia
NCT01672801	Not specified	COMPLETED	Nimodipine to Prevent LH Surge During Ovulation Induction: Blinded Placebo-controlled RCT
NCT02537080	Not specified	TERMINATED	The Effect of Nimodipine on the Postoperative Cognitive Dysfunction
NCT02991157	Not specified	COMPLETED	Noninvasive Assessment of Cerebral Oxygenation and Cardiac Function in Patients With Neurovascular Diseases
NCT04649398	Not specified	UNKNOWN	Cerebral Nimodipine Concentrations Following Oral, Intra-venous and Intra-arterial Administration
NCT04941846	Not specified	UNKNOWN	The Role of Deep Cerebral Vein Variation in Patients With Angiographic Negative Subarachnoid Hemorrhage

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.

157 molecules share ≥1 primary target. Top 60 by shared-target count:

Molecule	Source	Status	Shared targets
DULOXETINE	ChEMBL + PubChem	Phase 4 (approved)	CACNA1C, CACNA1D, CACNA1F, CACNA1S, P2RX4
PAROXETINE	ChEMBL + PubChem	Phase 4 (approved)	CACNA1C, CACNA1D, CACNA1F, CACNA1S, P2RX4
AMIODARONE	ChEMBL + PubChem	Phase 4 (approved)	CACNA1C, CACNA1D, CACNA1F, CACNA1S
AMITRIPTYLINE	ChEMBL + PubChem	Phase 4 (approved)	CACNA1C, CACNA1D, CACNA1F, CACNA1S
CHLORPROMAZINE	ChEMBL + PubChem	Phase 4 (approved)	CACNA1C, CACNA1D, CACNA1F, CACNA1S
CILOSTAZOL	ChEMBL + PubChem	Phase 4 (approved)	CACNA1C, CACNA1D, CACNA1F, CACNA1S
CLOZAPINE	ChEMBL + PubChem	Phase 4 (approved)	CACNA1C, CACNA1D, CACNA1F, CACNA1S
DIAZEPAM	ChEMBL + PubChem	Phase 4 (approved)	CACNA1C, CACNA1D, CACNA1F, CACNA1S
DILTIAZEM	ChEMBL + PubChem	Phase 4 (approved)	CACNA1C, CACNA1D, CACNA1F, CACNA1S
DOFETILIDE	ChEMBL + PubChem	Phase 4 (approved)	CACNA1C, CACNA1D, CACNA1F, CACNA1S
DONEPEZIL	ChEMBL + PubChem	Phase 4 (approved)	CACNA1C, CACNA1D, CACNA1F, CACNA1S
DROPERIDOL	ChEMBL + PubChem	Phase 4 (approved)	CACNA1C, CACNA1D, CACNA1F, CACNA1S
FLECAINIDE	ChEMBL + PubChem	Phase 4 (approved)	CACNA1C, CACNA1D, CACNA1F, CACNA1S
HALOPERIDOL	ChEMBL + PubChem	Phase 4 (approved)	CACNA1C, CACNA1D, CACNA1F, CACNA1S
IBUTILIDE	ChEMBL + PubChem	Phase 4 (approved)	CACNA1C, CACNA1D, CACNA1F, CACNA1S
IMIPRAMINE	ChEMBL + PubChem	Phase 4 (approved)	CACNA1C, CACNA1D, CACNA1F, CACNA1S
LAMIVUDINE	ChEMBL + PubChem	Phase 4 (approved)	CACNA1C, CACNA1D, CACNA1F, CACNA1S
LORATADINE	ChEMBL + PubChem	Phase 4 (approved)	CACNA1C, CACNA1D, CACNA1F, CACNA1S
METHADONE	ChEMBL + PubChem	Phase 4 (approved)	CACNA1C, CACNA1D, CACNA1F, CACNA1S
MEXILETINE	ChEMBL + PubChem	Phase 4 (approved)	CACNA1C, CACNA1D, CACNA1F, CACNA1S
MITOXANTRONE	ChEMBL + PubChem	Phase 4 (approved)	CACNA1C, CACNA1D, CACNA1F, CACNA1S
NIFEDIPINE	ChEMBL + PubChem	Phase 4 (approved)	CACNA1C, CACNA1D, CACNA1F, CACNA1S
NILOTINIB	ChEMBL + PubChem	Phase 4 (approved)	CACNA1C, CACNA1D, CACNA1F, CACNA1S
Nisoldipine	ChEMBL + PubChem	Phase 4 (approved)	CACNA1C, CACNA1D, CACNA1F, CACNA1S
PHENYTOIN	ChEMBL + PubChem	Phase 4 (approved)	CACNA1C, CACNA1D, CACNA1F, CACNA1S
PIMOZIDE	ChEMBL + PubChem	Phase 4 (approved)	CACNA1C, CACNA1D, CACNA1F, CACNA1S
QUINIDINE	ChEMBL + PubChem	Phase 4 (approved)	CACNA1C, CACNA1D, CACNA1F, CACNA1S
RISPERIDONE	ChEMBL + PubChem	Phase 4 (approved)	CACNA1C, CACNA1D, CACNA1F, CACNA1S
SAQUINAVIR	ChEMBL + PubChem	Phase 4 (approved)	CACNA1C, CACNA1D, CACNA1F, CACNA1S
SOLIFENACIN	ChEMBL + PubChem	Phase 4 (approved)	CACNA1C, CACNA1D, CACNA1F, CACNA1S
SUNITINIB	ChEMBL + PubChem	Phase 4 (approved)	CACNA1C, CACNA1D, CACNA1F, CACNA1S
THIORIDAZINE	ChEMBL + PubChem	Phase 4 (approved)	CACNA1C, CACNA1D, CACNA1F, CACNA1S
VERAPAMIL	ChEMBL + PubChem	Phase 4 (approved)	CACNA1C, CACNA1D, CACNA1F, CACNA1S
ASTEMIZOLE	ChEMBL	Phase 4 (approved)	CACNA1C, CACNA1D, CACNA1F, CACNA1S
BEPRIDIL	ChEMBL	Phase 4 (approved)	CACNA1C, CACNA1D, CACNA1F, CACNA1S
CISAPRIDE	ChEMBL	Phase 4 (approved)	CACNA1C, CACNA1D, CACNA1F, CACNA1S
DASATINIB	ChEMBL	Phase 4 (approved)	CACNA1C, CACNA1D, CACNA1F, CACNA1S
HALOFANTRINE	ChEMBL	Phase 4 (approved)	CACNA1C, CACNA1D, CACNA1F, CACNA1S
MIBEFRADIL	ChEMBL	Phase 4 (approved)	CACNA1C, CACNA1D, CACNA1F, CACNA1S
SERTINDOLE	ChEMBL	Phase 4 (approved)	CACNA1C, CACNA1D, CACNA1F, CACNA1S
SPARFLOXACIN	ChEMBL	Phase 4 (approved)	CACNA1C, CACNA1D, CACNA1F, CACNA1S
TACRINE	ChEMBL	Phase 4 (approved)	CACNA1C, CACNA1D, CACNA1F, CACNA1S
TERFENADINE	ChEMBL	Phase 4 (approved)	CACNA1C, CACNA1D, CACNA1F, CACNA1S
TERODILINE	ChEMBL	Phase 4 (approved)	CACNA1C, CACNA1D, CACNA1F, CACNA1S
AJMALINE	ChEMBL	Phase 3	CACNA1C, CACNA1D, CACNA1F, CACNA1S
NITRENDIPINE	ChEMBL	Phase 3	CACNA1C, CACNA1D, CACNA1F, CACNA1S
CIFENLINE	ChEMBL	Phase 2	CACNA1C, CACNA1D, CACNA1F, CACNA1S
GALLOPAMIL	ChEMBL	Phase 2	CACNA1C, CACNA1D, CACNA1F, CACNA1S
Belzutifan	PubChem	Approved	CACNA1C, CACNA1D, CACNA1F, CACNA1S
Moxifloxacin	PubChem	Approved	CACNA1C, CACNA1D, CACNA1F, CACNA1S
Paliperidone	PubChem	Approved	CACNA1C, CACNA1D, CACNA1F, CACNA1S
Ceftriaxone	PubChem	Approved	CACNA1D, CACNA1F, CACNA1S
Disopyramide	PubChem	Approved	CACNA1D, CACNA1F, CACNA1S
Linezolid	PubChem	Approved	CACNA1D, CACNA1F, CACNA1S
Melatonin	PubChem	Approved	CACNA1D, CACNA1F, CACNA1S
Metronidazole	PubChem	Approved	CACNA1D, CACNA1F, CACNA1S
Pemigatinib	PubChem	Approved	CACNA1D, CACNA1F, CACNA1S
Pentobarbital	PubChem	Approved	CACNA1D, CACNA1F, CACNA1S
Procainamide	PubChem	Approved	CACNA1D, CACNA1F, CACNA1S
Raltegravir	PubChem	Approved	CACNA1D, CACNA1F, CACNA1S