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Ranexa (RANOLAZINE)
Ranexa works by blocking the sodium channels in heart muscle cells to reduce the amount of calcium that enters the cells during heart contractions.
Ranexa (Ranolazine) is a small molecule anti-anginal medication originally developed by Gilead and currently owned by Menarini Intl. It targets the sodium channel protein type 5 subunit alpha to treat angina pectoris. Ranexa was FDA approved in 2006 and is now off-patent with 26 generic manufacturers. The medication has a half-life of 1.8 hours and bioavailability of 42%. Key safety considerations include its potential to prolong the QT interval.
At a glance
| Generic name | RANOLAZINE |
|---|---|
| Sponsor | Menarini Intl |
| Drug class | Anti-anginal [EPC] |
| Target | Sodium channel protein type 5 subunit alpha |
| Modality | Small molecule |
| Therapeutic area | Metabolic |
| Phase | FDA-approved |
| First approval | 2006 |
Mechanism of action
The mechanism of action of ranolazines antianginal effects has not been determined. Ranolazine has anti-ischemic and antianginal effects that do not depend upon reductions in heart rate or blood pressure. It does not affect the rate-pressure product, measure of myocardial work, at maximal exercise. Ranolazine at therapeutic levels can inhibit the cardiac late sodium current (INa). However, the relationship of this inhibition to angina symptoms is uncertain.The QT prolongation effect of ranolazine on the surface electrocardiogram is the result of inhibition ofIKr, which prolongs the ventricular action potential.
Approved indications
- Angina pectoris
Common side effects
- Dizziness
- Headache
- Constipation
- Nausea
- Bradycardia
- Palpitations
- Tinnitus
- Vertigo
- Blurred vision
- Abdominal pain
- Dry mouth
- Vomiting
Drug interactions
- High Risk QT Prolonging Agents
- P-glycoprotein Substrates
- carbamazepine
- fluconazole
- phenobarbital
- rifabutin
- rifampicin
- rifapentine
- ritonavir
- saquinavir
- simvastatin
- sotalol
Key clinical trials
- Inhibition of Late Sodium Current (INa) to Prevent Coronary MICROvascular Dysfunction in Patients Presenting With ST-Elevation Myocardial Infarction and Multivessel Disease: INaMICRON Study (PHASE2,PHASE3)
- A Study of Ranolazine in ALS (PHASE2)
- Feasibility Trial for a Right Ventricular Failure Platform Trial (PHASE2)
- Bioequivalence Study of Ranolazine Extended-release Tablets in Healthy Chinese Subjects (PHASE1)
- Reduce Crohn's-Associated Diarrhea With Sodium Channel Therapy (PHASE2)
- Safety and Efficacy of Ranolazine for the Treatment of Amyotrophic Lateral Sclerosis (PHASE2)
- Ranolazine in Ischemic Cardiomyopathy (PHASE4)
- Impact of Ranolazine on Coronary Microcirculatory Resistance (NA)
Patents
| Patent | Expiry | Type |
|---|---|---|
| 11510878 | 2038-01-24 | Formulation |
| 12161761 | 2038-01-24 | Formulation |
| 10898444 | 2038-01-24 | Formulation |
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| FDA label | Mechanism, indications, dosing, boxed warnings, drug interactions |
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
| FDA Orange Book | Patents + exclusivity |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Ranexa CI brief — competitive landscape report
- Ranexa updates RSS · CI watch RSS
- Menarini Intl portfolio CI