Ranolazine

Anti-anginal — CARDIOVASCULAR SYSTEM

Key facts

Ranolazine is an ofp drug in the Anti-anginal class catalogued in DrugCentral. It was first approved by the FDA in 2006. Its mechanism of action is classified as Cytochrome P450 2D6 Inhibitors, Cytochrome P450 3A Inhibitors and Organic Cation Transporter 2 Inhibitors. DrugCentral lists 4 molecular targets, including SCN5A, SCN5A and KCNH2. Recorded indications include Angina pectoris.

• Approval status: ofp (first approved 2006 by the FDA).
• Drug class: Anti-anginal.
• Mechanism of action: Cytochrome P450 2D6 Inhibitors; Cytochrome P450 3A Inhibitors; Organic Cation Transporter 2 Inhibitors.
• Molecular targets: SCN5A, SCN5A, KCNH2 and ABCB1 (4 listed in DrugCentral).
• Indications: Angina pectoris.
• ATC code: C01EB18 (Other cardiac preparations).
• Molecular formula: C24H33N3O4; molecular weight 427.55 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (1)

• Angina pectoris

Contraindications (5)

• Cirrhosis of liver
• Congenital long QT syndrome
• Kidney disease
• Prolonged QT interval
• Torsades de pointes

Mechanism & targets

• Mechanism of action (MoA): Cytochrome P450 2D6 Inhibitors; Cytochrome P450 3A Inhibitors; Organic Cation Transporter 2 Inhibitors; P-Glycoprotein Inhibitors
• Established pharmacologic class: Anti-anginal

Molecular targets (4)

Target	Gene	Action	Activity
Sodium channel protein type 5 subunit alpha	SCN5A	blocker	IC50 5.17
Voltage-gated sodium channel Nav1.5 cardiac isoform	SCN5A	unknown	IC50 5.16
Potassium voltage-gated channel subfamily H member 2	KCNH2	unknown	IC50 4.92
Multidrug resistance protein 1	ABCB1	unknown	—

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
2006-01-27	FDA	—	GILEAD

ATC classification

ATC code	Therapeutic hierarchy
C01EB18	CARDIOVASCULAR SYSTEM › CARDIAC THERAPY › OTHER CARDIAC PREPARATIONS › Other cardiac preparations

Pharmacogenomics

Drug-label and guideline annotations from PharmGKB and CPIC.

• EMA label: CYP2D6 · Actionable PGx
• FDA label
• HCSC label: CYP2D6 · Informative PGx
• Swissmedic label: CYP2D6 · Actionable PGx

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Dizziness	239.6
Chest pain	220.4
Drug interaction	195.5
Bradycardia	178.8
Angina pectoris	167.5
Electrocardiogram QT prolonged	160.4
Syncope	145.4
Hypotension	131.2
Coronary artery disease	129.4
Stent placement	112.0
Death	90.1
Dyspnoea	82.8

Chemical structure

• Molecular formula: C₂₄H₃₃N₃O₄
• Molecular weight: 427.55 g/mol
• CAS number: —
• InChIKey: XKLMZUWKNUAPSZ-UHFFFAOYSA-N
• PubChem CID: 56959

COC1=C(OCC(O)CN2CCN(CC(=O)NC3=C(C)C=CC=C3C)CC2)C=CC=C1

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Ranolazine used for?

DrugCentral lists the following indications for Ranolazine: Angina pectoris.

How does Ranolazine work?

Ranolazine is classified as Cytochrome P450 2D6 Inhibitors, Cytochrome P450 3A Inhibitors and Organic Cation Transporter 2 Inhibitors; its molecular targets in DrugCentral include SCN5A (blocker), SCN5A, KCNH2 and ABCB1.

When was Ranolazine first approved?

Ranolazine was first approved by the FDA in 2006.

What drug class does Ranolazine belong to?

Ranolazine is in the Anti-anginal class.

What is the chemical formula of Ranolazine?

Ranolazine has the molecular formula C24H33N3O4 and a molecular weight of 427.55 g/mol.

Sources

• DrugCentral drug card 2359 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL1404 — compound record and bioactivity
• PubChem CID 56959 — chemical identifiers
• DrugBank DB00243 — drug record
• FDA UNII A6IEZ5M406 — substance identity
• DailyMed: FDA labels for Ranolazine — current prescribing information (label search)
• UniProt Q14524 (SCN5A) — target protein
• UniProt Q12809 (KCNH2) — target protein
• UniProt P08183 (ABCB1) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral
• PharmGKB / CPIC — pharmacogenomic label annotations

How this page is built: methodology · editorial policy & corrections.