Last reviewed 2026-04-20 · How we verify

Yupelri (REVEFENACIN)

Yupelri works by blocking the action of a chemical called acetylcholine, which stimulates the muscles in the airways, leading to bronchodilation.

At a glance

Mechanism of action

Revefenacin is long-acting muscarinic antagonist, which is often referred to as an anticholinergic. It has similar affinity to the subtypes of muscarinic receptors M1 to M5. In the airways, it exhibits pharmacological effects through inhibition of M3 receptor at the smooth muscle leading to bronchodilation. The competitive and reversible nature of antagonism was shown with human and animal origin receptors and isolated organ preparations. In preclinical in vitro as well as in vivo models, prevention of methacholine- and acetylcholine-induced bronchoconstrictive effects was dose-dependent and lasted longer than 24 hours. The clinical relevance of these findings is unknown. The bronchodilation following inhalation of revefenacin is predominantly site-specific effect.

Approved indications

• Chronic obstructive lung disease

Common side effects

• Cough
• Nasopharyngitis
• Upper respiratory tract infection
• Headache
• Back pain
• Hypertension
• Dizziness
• Oropharyngeal pain
• Bronchitis

Key clinical trials

• Compare the Effects of Nebulizer Versus Inhaler Based Therapy for COPD Using Long-acting Bronchodilators (PHASE4)
• Revefenacin in Acute Respiratory Insufficiency in COPD (PHASE2)
• Phase 4 COPD and Suboptimal Inspiratory Flow Rate (PHASE4)
• Revefenacin in Chinese Subjects With Moderate to Very Severe Chronic Obstructive Pulmonary Disease(COPD) (PHASE3)
• Feasibility, Safety and Efficacy of Nebulized Long-Acting Bronchodilators (Formoterol and Revefenacin) vs. Short-Acting Bronchodilators (Albuterol and Ipratropium) in Hospitalized Patients With AECOPD (PHASE4)
• Fasting Bioavailability Study of Mylan's Revefenacin Inhalation Solution (PHASE1)
• A 42-day Parallel Group Safety Study of Revefenacin and Formoterol, Administered in Sequence and as a Combination, in Participants With COPD (PHASE3)
• Pharmacokinetics of TD-4208 in Patients With Severe Renal Impairment (PHASE1)

Patents

Primary sources

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