Revefenacin

Revefenacin is a 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.

• YUPELRI is indicated for the maintenance treatment of patients with chronic obstructive pulmonary disease (COPD). YUPELRI is an anticholinergic indicated for the maintenance treatment of patients with chronic obstructive pulmonary disease (COPD) .ICD-10: J44.9

• YUPELRI is contraindicated in patients with hypersensitivity to revefenacin or any component of this product. YUPELRI is contraindicated in patients with hypersensitivity to revefenacin or any component of this product.contraindicated

The recommended dosage is 175 mcg YUPELRI (one 175 mcg unit‑dose vial) administered by oral inhalation once daily by nebulizer using a mouthpiece. Administration Overview YUPELRI should be administered by the orally inhaled route via a standard jet nebulizer connected to an air compressor (See Instructions for Use) . The safety and efficacy of YUPELRI have been established in clinical trials when administered using the PARI LC ® Sprint nebulizer with a mouthpiece and the PARI Trek ® S compressor. The safety and efficacy of YUPELRI delivered from non‑compressor based nebulizer systems have not been established. The YUPELRI unit-dose vial should only be removed from the foil pouch and opened IMMEDIATELY BEFORE USE. The vial and any residual content should be discarded after use. No dosage adjustment is required for geriatric patients, or patients with renal impairment [see Use in Specific Populations (8.5 , 8.7) and Clinical Pharmacology (12.3) ] . The drug compatibility (physical and chemical), efficacy, and safety of YUPELRI when mixed with other drugs in a nebulizer have not been established. For oral inhalation use only. Do not swallow YUPELRI. • One 175 mcg vial (3 mL) once daily. ( 2 ) • For use with a standard jet nebulizer with a mouthpiece connected to an air compressor. ( 2 )

• Do not initiate YUPELRI in acutely deteriorating COPD or to treat acute symptoms. ( 5.1 ) • If paradoxical bronchospasm occurs, discontinue YUPELRI and institute alternative therapy. ( 5.2 ) • Worsening of narrow-angle glaucoma may occur. Use with caution in patients with narrow-angle glaucoma and instruct patients to contact a healthcare provider immediately if symptoms occur. ( 5.3 ) • Worsening of urinary retention may occur. Use with caution in patients with prostatic hyperplasia or bladder-neck obstruction and instruct patients to contact a healthcare provider immediately if symptoms occur. ( 5.4 ) • Immediate hypersensitivity reactions may occur. If such a reaction occurs, therapy with YUPELRI should be stopped at once and alternative treatments should be considered. ( 5.5 ) 5.1 Deterioration of Disease and Acute Episodes YUPELRI should not be initiated in patients during acutely deteriorating or potentially life-threatening episodes of COPD. YUPELRI has not been studied in subjects with acutely deteriorating COPD. The initiation of YUPELRI in this setting is not appropriate. YUPELRI is intended as a once-daily maintenance treatment for COPD and should not be used for relief of acute symptoms, i.e. as rescue therapy for the treatment of acute episodes of bronchospasm, and extra doses should not be used for that purpose. Acute symptoms should be treated with an inhaled, short-acting beta 2 -agonist. COPD may deteriorate acutely over a period of hours or chronically over several days or longer.

The following clinically significant adverse reactions are described elsewhere in labeling: • Paradoxical bronchospasm [see Warnings and Precautions (5.2) ] • Worsening of narrow-angle glaucoma [see Warnings and Precautions (5.3) ] • Worsening of urinary retention [see Warnings and Precautions (5.4) ] • Immediate hypersensitivity reactions [ see Warnings and Precautions (5.5) ] Most common adverse reactions (incidence greater than or equal to 2% and more common than placebo) include cough, nasopharyngitis, upper respiratory tract infection, headache, and back pain. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Mylan at 1-877-446-3679 (1-877-4-INFO-RX) or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trial Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. The YUPELRI safety database included 2,285 subjects with COPD in two 12-week efficacy studies and one 52-week long-term safety study. A total of 730 subjects received treatment with YUPELRI 175 mcg once daily. The safety data described below are based on the two 12-week trials and the one 52-week trial. 12-Week Trials YUPELRI was studied in two 12-week replicate placebo-controlled trials in patients with moderate to very severe COPD (Trials 1 and 2). In these trials, 395 patients were treated with YUPELRI at the recommended dose of 175 mcg once daily.

Hepatic impairment: Avoid use of YUPELRI in patients with hepatic impairment. ( 8.6 , 12.3 ) 8.1 Pregnancy Risk Summary There are no adequate and well-controlled studies with YUPELRI in pregnant women. Women should be advised to contact their physician if they become pregnant while taking YUPELRI. In animal reproduction studies, subcutaneous administration of revefenacin to pregnant rats and rabbits during the period of organogenesis produced no evidence of fetal harm at respective exposures approximately 209 times the exposure at the maximum recommended human dose (MRHD) (on an area under the curve [AUC] basis) (see Data ) . The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2-4% and 15-20%, respectively. Data Animal Data In an embryo‑fetal development study in pregnant rats dosed during the period of organogenesis from gestation days 6 to 17, revefenacin was not teratogenic and did not affect fetal survival at exposures up to 209 times the MRHD (based upon summed AUCs for revefenacin and its active metabolite at maternal subcutaneous doses up to 500 mcg/kg/day).

Metabolism

Revefenacin pharmacokinetic parameters are presented as the mean [standard deviation (SD)] unless otherwise specified. Following repeat dosing of inhaled YUPELRI, steady-state was achieved within 7 days with <1.6‑fold accumulation.

An overdosage of YUPELRI may lead to anticholinergic signs and symptoms such as nausea, vomiting, dizziness, lightheadedness, blurred vision, increased intraocular pressure (causing pain, vision disturbances, or reddening of the eye), obstipation or difficulties in voiding. Treatment of overdosage consists of discontinuation of YUPELRI along with institution of appropriate symptomatic and/or supportive therapy.

• Nov 9, 2018NDANDA210598Mylan Ireland Ltd

1. 1Dyspnoea18024%
2. 2Cough506.8%
3. 3Fatigue506.8%
4. 4Headache496.6%
5. 5Death466.2%
6. 6Pneumonia435.8%
7. 7Chronic Obstructive Pulmonary Disease415.5%
8. 8Nausea405.4%
9. 9Drug Ineffective364.9%
10. 10Dizziness354.7%
11. 11Product Dose Omission Issue354.7%
12. 12Off Label Use334.5%
13. 13Asthenia304.1%
14. 14Diarrhoea304.1%
15. 15Chest Discomfort293.9%

The 10 most recently updated of 19 ClinicalTrials.gov registrations naming Revefenacin as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Compare the Effects of Nebulizer Versus Inhaler Based Therapy for COPD Using Long-acting Bronchodilators
  Recruiting · Phase 4 · Interventional · 72 enrolled · University of Tennessee Graduate School of Medicine
  NCT07133880updated 2025-08-27
• Revefenacin in Acute Respiratory Insufficiency in COPD
  Completed · Phase 2 · Interventional · 21 enrolled · University of California, Los Angeles
  NCT04315558updated 2025-08-13
• Phase 4 COPD and Suboptimal Inspiratory Flow Rate
  Completed · Phase 4 · Interventional · 404 enrolled · Theravance Biopharma
  NCT05165485updated 2024-12-20
• Revefenacin in Chinese Subjects With Moderate to Very Severe Chronic Obstructive Pulmonary Disease(COPD)
  Completed · Phase 3 · Interventional · 258 enrolled · Mylan Pharma UK Ltd.
  NCT05046795updated 2024-11-01
• Feasibility, Safety and Efficacy of Nebulized Long-Acting Bronchodilators (Formoterol and Revefenacin) vs. Short-Acting Bronchodilators (Albuterol and Ipratropium) in Hospitalized Patients With AECOPD
  Unknown · Phase 4 · Interventional · 60 enrolled · University of Tennessee Graduate School of Medicine
  NCT04655170updated 2022-11-15
• Fasting Bioavailability Study of Mylan's Revefenacin Inhalation Solution
  Completed · Phase 1 · Interventional · 24 enrolled · Mylan Pharma UK Ltd.
  NCT05207111updated 2022-04-04
• Revefenacin Peak Inspiratory Flow Rate (PIFR) Study in COPD
  Completed · Phase 3 · Interventional · 207 enrolled · Mylan Inc.
  NCT03095456updated 2022-02-24
• Efficacy Study of Nebulized TD-4208 for Chronic Obstructive Pulmonary Disease (COPD)
  Completed · Phase 3 · Interventional · 611 enrolled · Mylan Inc.
  NCT02512510updated 2022-02-24
• A 42-day Parallel Group Safety Study of Revefenacin and Formoterol, Administered in Sequence and as a Combination, in Participants With COPD
  Completed · Phase 3 · Interventional · 122 enrolled · Mylan Inc.
  NCT03573817updated 2022-02-24
• A 7-Day Cross-over Study of QD (Once Daily) and BID (Twice Daily) TD-4208 in Chronic Obstructive Pulmonary Disease (COPD)
  Completed · Phase 2 · Interventional · 64 enrolled · Mylan Inc.
  NCT02109172updated 2022-02-24

Frequently asked questions

How does Revefenacin work?

Revefenacin is a 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.

What is Revefenacin used for?

According to FDA labeling, Revefenacin carries indications including: YUPELRI is indicated for the maintenance treatment of patients with chronic obstructive pulmonary disease (COPD). YUPELRI is an anticholinergic indicated for the maintenance treatment of patients with chronic obstructive pulmonary disease (COPD) .. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Revefenacin?

Revefenacin is classified as Anticholinergics, Anticholinergic, Cholinergic Antagonists, Cholinergic Muscarinic Antagonists, Bronchodilation.

What are the brand names for Revefenacin?

Revefenacin is marketed under brand names including Yupelri.

What are the contraindications for Revefenacin?

Revefenacin labeling lists contraindications including: YUPELRI is contraindicated in patients with hypersensitivity to revefenacin or any component of this product. YUPELRI is contraindicated in patients with hypersensitivity to revefenacin or any component of this product.. Always consult the full prescribing information and a clinician.