TOPROL-XL (metoprolol succinate) · MELINTA THERAP
Toprol-XL (metoprolol succinate) is a beta₁-selective adrenoceptor blocking agent indicated for the treatment of hypertension, to lower blood pressure and thereby reduce the risk of fatal and non-fatal cardiovascular events, specifically strokes and myocardial infarctions. It is also indicated for the long-term treatment of angina pectoris and for the treatment of stable, symptomatic heart failure (NYHA Class II or III) of ischemic, hypertensive, or cardiomyopathic origin to reduce cardiovascular mortality and heart failure-related hospitalizations. It is typically utilized as part of a comprehensive cardiovascular risk management strategy including lipid control, diabetes management, and lifestyle modifications.
How TOPROL-XL Works
Metoprolol is a cardioselective beta₁-adrenergic receptor blocker. At therapeutic plasma concentrations, it preferentially inhibits beta₁-receptors located chiefly in cardiac muscle, resulting in a reduction in heart rate (sinus rate) and a decrease in AV nodal conduction. This selectivity is dose-dependent; at higher concentrations, metoprolol also inhibits beta₂-adrenoreceptors found in bronchial and vascular musculature. The drug lacks intrinsic sympathomimetic activity (ISA). Its antihypertensive effects are attributed to several mechanisms, including competitive antagonism of catecholamines leading to decreased cardiac output, reduced central sympathetic outflow, and suppression of renin secretion.
Details
- Status
- Prescription
- First Approved
- 1992-01-10
- Routes
- ORAL
- Dosage Forms
- TABLET, EXTENDED RELEASE
TOPROL-XL Approval History
What TOPROL-XL Treats
3 indicationsTOPROL-XL is approved for 3 conditions since its original approval in 1992. These indications span multiple therapeutic areas including oncology, immunology, and more.
TOPROL-XL Boxed Warning
ISCHEMIC HEART DISEASE: Following abrupt cessation of therapy with certain beta-blocking agents, exacerbations of angina pectoris and, in some cases, myocardial infarction have occurred. When discontinuing chronically administered metoprolol succinate extended-release tablets, particularly in patients with ischemic heart disease, the dosage should be gradually reduced over a period of 1 - 2 weeks and the patient should be carefully monitored. If angina markedly worsens or acute coronary insuffic...
WARNING: ISCHEMIC HEART DISEASE: Following abrupt cessation of therapy with certain beta-blocking agents, exacerbations of angina pectoris and, in some cases, myocardial infarction have occurred. When discontinuing chronically administered metoprolol succinate extended-release tablets, particularly in patients with ischemic heart disease, the dosage should be gradually reduced over a period of 1 - 2 weeks and the patient should be carefully monitored. If angina markedly worsens or acute coronary insufficiency develops, metoprolol succinate extended-release tablet administration should be reinstated promptly, at least temporarily, and other measures appropriate for the management of unstable angina should be taken. Warn patients against interruption or discontinuation of therapy without the physician’s advice. Because coronary artery disease is common and may be unrecognized, it may be prudent not to discontinue metoprolol succinate extended-release tablet therapy abruptly even in patients treated only for hypertension (5.1). WARNING: ISCHEMIC HEART DISEASE (See Full Prescribing Information for complete boxed warning) Following abrupt cessation of therapy with beta-blocking agents, exacerbations of angina pectoris and myocardial infarction have occurred. Warn patients against interruption or discontinuation of therapy without the physician’s advice. (5.1)
TOPROL-XL Competitive Set
ProThree rings of competition based on shared molecular targets and treated indications.
Direct competitors
Same target(s) AND same indication — head-to-head.
Indication competitors
Same indication, different mechanism — what else might this patient receive?
Filters applied: drops same-active-ingredient (505(b)(2) reformulations), route-mismatch (topical vs systemic), and cross-therapeutic-area matches in same-indication rings.
What's emerging in TOPROL-XL's indications
See all emerging drugs →Phase 3 candidates targeting molecules with no FDA-approved drug, in indications TOPROL-XL treats. First-in-class if their pivotal trials read out positive.
Drugs Similar to TOPROL-XL
3 of 20FDA-approved drugs for similar conditions. Compare mechanisms and indications to understand treatment alternatives.
Clinical Trial Registry
18 trials| Trial | Sponsor ID | Phase | Status | Title |
|---|---|---|---|---|
| NCT07490067 | HUM00266021 1R01HL178410-01 | Ph 4 | recruiting | Mechanistic Clinical Trial Comparing the Pharmacokinetics/Pharmacodynamics of Metoprolol in Heart Failure With Reduced Ejection Fraction Patients With Low vs. High Polygenic Score |
| NCT04434664 BLOCK HFpEF results posted | 833517 | Ph 4 | completed | BLOCKade of Calcium Channels and Beta Adrenergic Receptors for the Treatment of Hypertension in HFpEF |
| NCT05931276 BRAVO | 2026 | Ph 3 | recruiting | CSP #2026 - Beta Blocker Dialyzability on Cardiovascular Outcomes |
| NCT06964464 CARVTOP-ICD | STUDY00010093 PLACER-2023C3-33489 | Ph 4 | recruiting | Comparative Effectiveness of Carvedilol Versus Metoprolol Succinate in Heart Failure Patients With an Implantable Cardioverter Defibrillator |
| NCT03778554 DANBLOCK | 2018-002699-42 2018-002699-42 | Ph 4 | active not recruiting | Danish Trial of Beta Blocker Treatment After Myocardial Infarction Without Reduced Ejection Fraction |
| NCT05711810 | SARSCoVVaxPoison | Ph 4 | completed | Medicine-induced Cardiac Hemodialysis on COVID-19 |
| NCT01970501 GENETIC-AF results posted | BUC-CLIN-303 | Ph 2 | completed | Genetically Targeted Therapy for the Prevention of Symptomatic Atrial Fibrillation in Patients With Heart Failure |
| NCT05066633 MeDMD | NBK 154/1/2020 2020-004901-29 | Ph 3 | recruiting | The Efficacy and Safety of Metoprolol as add-on Treatment to Standard of Care in Preventing Cardiomyopathy in Patients With DMD |
| NCT03532802 TEMPO | 1-10-72-441-17 | Ph 2 | completed | The Effect of Metoprolol in Patients With Hypertrophic Obstructive Cardiomyopathy. |
| NCT02587351 results posted | 1512M81981 | Ph 3 | terminated | Beta-Blockers for the Prevention of Acute Exacerbations of Chronic Obstructive Pulmonary Disease |
| NCT01502787 results posted | STU 062011-072 | Ph 4 | completed | Comparison of Nebivolol and Metoprolol With Exercise and Angiotensin II in Hypertensive Patients |
| NCT01501929 results posted | Bystolic MD52 | Ph 4 | completed | Effects of Nebivolol on Skeletal Muscle During Exercise in Hypertensive Patients |
| NCT01041287 results posted | IRB00013262 BYD-MD-20 | Ph 4 | completed | Effect of Nebivolol on Oxidative Stress and Endothelial Progenitor Cells |
| NCT01499134 ENCOMPASS results posted | 11C.18 | Ph 3 | completed | Comparison of 2 Beta Blocker Drugs on Peripheral Arterial Disease in Patients With High Blood Pressure |
| NCT01676285 CARE Cirrhosis | 0010/11 | Ph 3 | completed | Metoprolol Succinate in Cardiac Remodeling Related to Cirrhosis |
| NCT01605370 Inapprop results posted | 11-007035 | Ph 4 | terminated | Can Nebivolol Reverse Inappropriate Left Ventricular Mass in Hypertensive Patients? |
| NCT01694797 | 642/09 | Ph 1 | completed | Bioequivalence Study for Metoprolol Succinate ER Tablets 50 mg Under Fasting Condition |
| NCT01673997 | P-643/09 | Ph 1 | completed | Bioequivalence Study of Metoprolol Succinate ER Tablets, 200 mg Under Fasting Conditions |
Active Pipeline
Ongoing clinical trials by development phase
Key Completed Trials
Completed studies with published results, ranked by significance
Trial Timeline
Full development history with FDA approval milestones
Understanding FDA Approval Types
| Count | Type | What it means |
|---|---|---|
| - | ORIG | Original approval - drug first enters market |
| - | SUPPL - Efficacy | New indication (new disease/condition approved) |
| - | SUPPL - Labeling | Label text changes (warnings, dosing updates) |
| - | SUPPL - Manufacturing | Production changes (new facility) |
| - | SUPPL - Chemistry | Formulation changes (new dosage strength) |
Green lines in the timeline show ORIG and Efficacy approvals - the clinically meaningful milestones.
TOPROL-XL FDA Label Details
Indications & Usage
FDA Label (PDF)Metoprolol Succinate is a beta 1 -selective adrenoceptor blocking agent. Metoprolol Succinate is indicated for the treatment of: Hypertension, to lower blood pressure. Lowering blood pressure reduces the risk of fatal and non-fatal cardiovascular events, primarily strokes and myocardial infarctions. Angina Pectoris. Heart Failure - for the treatment of stable, symptomatic (NYHA Class II or III) heart failure of ischemic, hypertensive, or cardiomyopathic origin. 1.1 Hypertension Metoprolol succinate is indicated for the treatment of hypertension, to lower blood pressure. Lowering blood pressure...
WARNING: ISCHEMIC HEART DISEASE: Following abrupt cessation of therapy with certain beta-blocking agents, exacerbations of angina pectoris and, in some cases, myocardial infarction have occurred. When discontinuing chronically administered metoprolol succinate extended-release tablets, particularly ...
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Data Sources
Data sourced from official FDA and NIH databases. Click links to verify on original sources.