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Levalbuterol (R albuterol)
Levalbuterol is the active R-enantiomer of albuterol that selectively binds to and activates beta-2 adrenergic receptors on airway smooth muscle, causing bronchodilation.
Levalbuterol is the active R-enantiomer of albuterol that selectively binds to and activates beta-2 adrenergic receptors on airway smooth muscle, causing bronchodilation. Used for Acute bronchospasm in asthma and COPD, Prevention of exercise-induced bronchospasm.
At a glance
| Generic name | Levalbuterol (R albuterol) |
|---|---|
| Also known as | Xopenex |
| Sponsor | Children's Hospital of Philadelphia |
| Drug class | Beta-2 adrenergic agonist (short-acting) |
| Target | Beta-2 adrenergic receptor |
| Modality | Small molecule |
| Therapeutic area | Respiratory |
| Phase | FDA-approved |
Mechanism of action
Levalbuterol is the pharmacologically active isomer of the racemic mixture albuterol. By selectively activating beta-2 adrenergic receptors, it triggers smooth muscle relaxation in the airways, leading to rapid bronchodilation. The R-enantiomer is approximately 50-fold more potent at the beta-2 receptor than the S-enantiomer, potentially allowing for lower doses and reduced systemic side effects compared to racemic albuterol.
Approved indications
- Acute bronchospasm in asthma and COPD
- Prevention of exercise-induced bronchospasm
Common side effects
- Tremor
- Nervousness
- Headache
- Palpitations
- Tachycardia
- Muscle cramps
Key clinical trials
- 5 Versus 10 Units of Insulin in Hyperkalemia Management (PHASE4)
- Individualizing Treatment for Asthma in Primary Care (Full Study) (PHASE4)
- Bronchoprovocation Study to Demonstrate the Pharmacodynamic Bioequivalence of Albuterol Sulfate HFA Inhalation Aerosol (E.Q. 90 mcg of Albuterol Base/Inh) of Macleods Pharmaceuticals Ltd (PHASE3)
- Bioequivalence With Clinical Endpoint Study of Fluticasone Propionate 100 mcg and Salmeterol 50 mcg Inhalation Powder/Respirent Pharmaceuticals vs. ADVAIR DISKUS® 100/50 mcg Inhalation Powder/GSK in Patients With Asthma (PHASE3)
- Pooled Analysis FP_SX_250_50
- A Clinical Trial for Examining the Therapeutic Equivalence Between Fluticasone Propionate 100 mcg and Salmeterol 50 mcg Inhalation Powder/Respirent Pharmaceuticals vs. ADVAIR DISKUS® 100/50 mcg Inhalation Powder/GSK in Patients With Asthma (PHASE3)
- Lung Pharmacokinetics (PK) in Epithelial Lining Fluid (ELF) (NA)
- The Cardiopulmonary Effect of Inhaled Beta-2-agonists on Adult Patients Born With Ventricular Septum Defects. (PHASE4)
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 |
|---|---|
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Levalbuterol (R albuterol) CI brief — competitive landscape report
- Levalbuterol (R albuterol) updates RSS · CI watch RSS
- Children's Hospital of Philadelphia portfolio CI