Ranolazine

Summary

Ranolazine (CHEMBL1404) is an approved small molecule (ATC C01EB18); indicated across 17 conditions including cardiovascular disorder and atrial fibrillation.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: C01EB18
• Indications: 17 conditions
• Clinical trials: 81
• Chemistry: 427.5 Da · C24H33N3O4

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1404
Name	Ranolazine
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	56959
ChEBI	CHEBI:87690
ATC	C01EB18
Molecular formula	C24H33N3O4
Molecular weight	427.5
InChIKey	XKLMZUWKNUAPSZ-UHFFFAOYSA-N

SMILES: CC1=C(C(=CC=C1)C)NC(=O)CN2CCN(CC2)CC(COC3=CC=CC=C3OC)O

IUPAC name: N-(2,6-dimethylphenyl)-2-[4-[2-hydroxy-3-(2-methoxyphenoxy)propyl]piperazin-1-yl]acetamide

ChEBI definition: An aromatic amide obtained by formal condensation of the carboxy group of 2-{4-[2-hydroxy-3-(2-methoxyphenoxy)propyl]piperazin-1-yl}acetic acid with the amino group of 2,6-dimethylaniline.

Also known as: Aspruzyo, Aspruzyo sprinkle, CVT-303, NSC-759100, Ran d, Ranexa, Ranexa (previously latixa), Ranolazina, Ranolazine, ranolazine, SID26749060, SID90340842

Parent form; salt/anhydrous children: CHEMBL537649, CHEMBL1526084

Patent coverage: 3,180 distinct patent families (9,372 SureChEMBL compound mentions), from 2 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: 10 (assay-derived). Sample: 5-hydroxytryptamine receptor 2B, Alpha-2A adrenergic receptor, Alpha-2C adrenergic receptor, Alpha-2B adrenergic receptor, Sodium channel protein type 5 subunit alpha, Beta-2 adrenergic receptor, Beta-1 adrenergic receptor, Alpha-1A adrenergic receptor, D(3) dopamine receptor, Voltage-gated inwardly rectifying potassium channel KCNH2.

Bioactivity

ChEMBL activities: 8 potent at pChembl ≥ 5 of 15 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
ADRA2C	5.85	AC50	1400	nM	CHEMBL_ACT_25147871
ADRA1A	5.77	AC50	1700	nM	CHEMBL_ACT_25218067
ADRB2	5.24	AC50	5700	nM	CHEMBL_ACT_25122864
SCN5A	5.17	IC50	6700	nM	CHEMBL_ACT_16911065
SCN5A	5.16	IC50	7000	nM	CHEMBL_ACT_23165476
KCNH2	5.14	AC50	7198	nM	CHEMBL_ACT_25117860
ADRB1	5.11	AC50	7800	nM	CHEMBL_ACT_25121770
ADRA2A	5.11	AC50	7700	nM	CHEMBL_ACT_25219889

Target pathways

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

Indications & clinical

Indications

17 indications (2 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
atrial fibrillation	3	MONDO:0004981	EFO:0000275
myocardial ischemia	3	MONDO:0024644	EFO:1001375
coronary artery disorder	3	MONDO:0005010	EFO:0001645
type 2 diabetes mellitus	3	MONDO:0005148	MONDO:0005148
dilated cardiomyopathy	2	MONDO:0005021	EFO:0000407
acute coronary syndrome	2	MONDO:0005542	EFO:0005672
irritable bowel syndrome	2	MONDO:0005052	EFO:0000555
vascular disorder	2	MONDO:0005385	EFO:0004264
diastolic heart failure	2	MONDO:0006727	EFO:1000899
Crohn disease	2	MONDO:0005011	EFO:0000384
amyotrophic lateral sclerosis	2	MONDO:0004976	MONDO:0004976
pulmonary arterial hypertension	1	MONDO:0015924	EFO:0001361
kidney disorder	1	MONDO:0005240	EFO:0003086
myotonic syndrome	1	MONDO:0016120	MONDO:0008195

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

Clinical trials

Total trials: 81.

Phase distribution

Phase	Trials
PHASE4	26
PHASE2	19
PHASE3	13
Not specified	11
PHASE1	9
PHASE2/PHASE3	3

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00644332	PHASE4	COMPLETED	An Open-label, Multi-center Study Evaluating the Validity, Reliability, and Responsiveness of a New Female-specific Angina Questionnaire in Women With Chronic Angina Treated With Ranolazine Extended-release Tablets (CVT 3041)
NCT00657514	PHASE4	WITHDRAWN	Ranolazine Versus Placebo Effects on Exercise Tolerance in Patients With Heart Disease and Peripheral Arterial Disease
NCT00832572	PHASE4	TERMINATED	Study of Ranexa in Patients With Coronary Artery Disease and Painful Polyneuropathy
NCT01221272	PHASE4	COMPLETED	Effect of Ranolazine on Myocardial Perfusion Assessed by Serial Quantitative Exercise SPECT Imaging
NCT01304095	PHASE4	UNKNOWN	Ranolazine, Ethnicity and the Metabolic Syndrome
NCT01334203	PHASE4	WITHDRAWN	A Study on the Effects of Ranolazine on Exercise Duration in Subjects With Chronic Stable Angina and Coronary Artery Disease (CAD) With Type 2 Diabetes Mellitus (T2DM)
NCT01345188	PHASE4	COMPLETED	Ranolazine in Ischemic Cardiomyopathy
NCT01425359	PHASE4	COMPLETED	Type 2 Diabetes Evaluation of Ranolazine in Subjects With Chronic Stable Angina
NCT01435174	PHASE4	COMPLETED	Pharmacokinetics of Single-Dose Oral Ranolazine in Hemodialysis Patients
NCT01490255	PHASE4	UNKNOWN	Pharmacodynamic Effects of Ranolazine Versus Amlodipine on Platelet Reactivity
NCT01491061	PHASE4	UNKNOWN	Ranolazine Loading to Prevent PCI-induced Myocardial Injury
NCT01495520	PHASE4	UNKNOWN	Ranolazine for Improving Symptoms of Palpitations
NCT01558830	PHASE4	UNKNOWN	Safety of Amiodarone and Ranolazine Together in Patients With Angina
NCT01721967	PHASE4	COMPLETED	Ranolazine for the Treatment of Chest Pain in HCM Patients
NCT01839110	PHASE4	COMPLETED	Targeting the Right Ventricle in Pulmonary Hypertension
NCT01948310	PHASE4	COMPLETED	Effects of Ranolazine and Exercise on Daily Physical Activity Trial
NCT01996618	PHASE4	UNKNOWN	Study to Reduce Symptoms of Premature Beats With Ranolazine
NCT02052011	PHASE4	COMPLETED	Ranolazine and Microvascular Angina by PET in the Emergency Department
NCT02133352	PHASE4	COMPLETED	Study of Ranolazine in the Treatment of Pulmonary Hypertension Associated With Diastolic Left Ventricular Dysfunction
NCT02156336	PHASE4	TERMINATED	Ranolazine for Diabetic Peripheral Neuropathic Pain (DPNP)
NCT02252406	PHASE4	COMPLETED	Impact of Ranolazine in Blood Markers in Women With Angina and Metabolic Syndrome
NCT02423265	PHASE4	WITHDRAWN	Efficacy of Ranolazine in Patients With Chronic Total Occlusions of Coronary Arteries
NCT02687269	PHASE4	WITHDRAWN	Ranolazine a Potential New Therapeutic Application
NCT02829034	PHASE4	COMPLETED	Targeting Right Ventricle in Pulmonary Hypertension Gilead
NCT03044964	PHASE4	UNKNOWN	Effect of Ranolazine on Activity Level in Patients With Angina After FFR Based Deferred Intervention (REPTAR)
NCT03486561	PHASE4	UNKNOWN	Management of Ischemic Heart Disease With Angiwell-XR (Ranolazine)
NCT07380919	PHASE2/PHASE3	RECRUITING	Inhibition of Late Sodium Current (INa) to Prevent Coronary MICROvascular Dysfunction in Patients Presenting With ST-Elevation Myocardial Infarction and Multivessel Disease: INaMICRON Study
NCT00091429	PHASE3	COMPLETED	Ranolazine SR in Patients With Chronic Angina Who Remain Symptomatic Despite Maximal Treatment With Amlodipine
NCT00099788	PHASE3	COMPLETED	Metabolic Efficiency With Ranolazine for Less Ischemia in Non-ST Elevation Acute Coronary Syndromes
NCT00998218	PHASE3	COMPLETED	Effect of Ranolazine on Arrhythmias and Microvolt T- Wave Alternans (MVTWA) Patients With LV Dysfunction
NCT01174173	PHASE3	COMPLETED	Ranolazine and Pulmonary Hypertension
NCT01215253	PHASE3	COMPLETED	Ranolazine Implantable Cardioverter-Defibrillator Trial
NCT01349491	PHASE3	TERMINATED	Ranolazine for the Prevention of Atrial Fibrillation After Electrical Cardioversion
NCT01352416	PHASE3	TERMINATED	Suppression Of Atrial Fibrillation With Ranolazine After Cardiac Surgery
NCT01442038	PHASE3	COMPLETED	Ranolazine for Incomplete Vessel Revascularization Post-Percutaneous Coronary Intervention (PCI)
NCT01472185	PHASE3	COMPLETED	Ranolazine Monotherapy in Subjects With Type 2 Diabetes Mellitus
NCT01494987	PHASE3	COMPLETED	Ranolazine When Added to Glimepiride in Subjects With Type 2 Diabetes Mellitus
NCT01555164	PHASE3	COMPLETED	A Phase 3 Study of Ranolazine in Subjects With Type 2 Diabetes Who Are Inadequately Controlled on Metformin Alone
NCT01754259	PHASE3	COMPLETED	Effects of Ranolazine on Coronary Flow Reserve in Symptomatic Diabetic Patients and CAD
NCT01797484	PHASE2/PHASE3	COMPLETED	Reduction of Ischemic Myocardium With Ranolazine-Treatment in Patients With Acute Myocardial Ischemia

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).