Drug Monograph

Anoro Ellipta

umeclidinium / vilanterol

LAMA/LABA Dual Bronchodilator · Oral Inhalation (DPI — Ellipta)
Pharmacokinetic Profile
Half-Life
UMEC ~11 h (effective); VI ~11 h (effective)
Metabolism
UMEC: CYP2D6; VI: CYP3A4
Protein Binding
UMEC ~89%; VI ~94%
Bioavailability
Low systemic (inhaled route for both)
Volume of Distribution
UMEC 86 L (IV); VI 165 L (SS)
Clinical Information
Drug Class
LAMA + LABA (dual bronchodilator)
Available Doses
62.5/25 mcg per actuation (single strength)
Route
Oral inhalation (DPI — Ellipta inhaler)
Renal Adjustment
Not required
Hepatic Adjustment
No adjustment for moderate impairment; not studied in severe
Pregnancy
No adequate studies; use if benefits outweigh risk
Lactation
Unknown if excreted in human milk
Schedule / Legal
Prescription only (Rx); not scheduled
Generic Available
Yes (authorized generic, approved April 2025)
Asthma Use
NOT indicated — contraindicated as LABA without ICS
Rx

Indications

IndicationApproved PopulationTherapy TypeStatus
COPD — maintenance treatmentAdultsDual bronchodilator (LAMA + LABA)FDA Approved

Umeclidinium-vilanterol is indicated for the long-term, once-daily maintenance treatment of airflow obstruction in patients with COPD, including chronic bronchitis and emphysema. It improves symptoms and reduces the frequency of exacerbations through the additive bronchodilation provided by combining muscarinic blockade with beta-2 agonism. It does not contain an inhaled corticosteroid and is therefore not suitable for patients requiring anti-inflammatory airway therapy.

Critical Safety Note — NOT for Asthma

Anoro Ellipta is NOT indicated for the treatment of asthma. The safety and efficacy in asthma have not been established. Use of a LABA (vilanterol) without an inhaled corticosteroid in patients with asthma is associated with an increased risk of asthma-related death (LABA class effect). This contraindication is explicitly stated in the FDA-approved labelling.

Off-Label Uses

Asthma-COPD overlap (ACO) — as add-on to ICS: In practice, some clinicians prescribe Anoro Ellipta alongside a separate ICS inhaler for patients with features of both COPD and asthma. Evidence quality: Low. This use is not FDA-approved; dedicated ACO trials with this combination have not been conducted. Trelegy Ellipta (which adds fluticasone furoate) is a more appropriate single-inhaler option when ICS is also needed.

Dose

Dosing

Clinical ScenarioStarting DoseMaintenance DoseMaximum DoseNotes
COPD maintenance — initial dual bronchodilator therapy62.5/25 mcg, 1 inhalation once daily62.5/25 mcg, 1 inhalation once daily62.5/25 mcg once dailySingle strength only; do not exceed 1 inhalation/24 h
Use at the same time each day
COPD — step-up from LAMA or LABA monotherapy62.5/25 mcg, 1 inhalation once daily62.5/25 mcg, 1 inhalation once daily62.5/25 mcg once dailyDiscontinue separate LAMA and/or LABA inhalers when switching
Appropriate for patients with persistent symptoms on monotherapy
COPD — exacerbation-prone patients without eosinophilic phenotype62.5/25 mcg, 1 inhalation once daily62.5/25 mcg, 1 inhalation once daily62.5/25 mcg once dailyGOLD recommends LAMA/LABA over ICS/LABA for exacerbation prevention when eosinophils are low
If exacerbations persist or eosinophils ≥300 cells/µL, consider step-up to ICS/LAMA/LABA triple therapy
Clinical Pearl — Fixed Single Dose, Simple Inhaler

Anoro Ellipta is available in a single strength only (62.5/25 mcg) with no dose titration required. The Ellipta dry powder inhaler needs no shaking, no priming, and no breath-actuation coordination. The patient opens the cover (loading the dose), breathes in steadily and deeply, then closes. The inhaler has a dose counter and should be discarded after 30 doses or 6 weeks from opening the foil tray, whichever comes first. No mouth rinsing is needed (no ICS component), but patients should have a separate rescue inhaler (e.g., albuterol) for acute symptoms.

PK

Pharmacology

Mechanism of Action

Umeclidinium is a long-acting muscarinic antagonist (LAMA) with high affinity for the M1 through M5 receptor subtypes. Its therapeutic effect in COPD stems from competitive and reversible blockade of M3 muscarinic receptors on airway smooth muscle, preventing acetylcholine-mediated bronchoconstriction. The onset of bronchodilation begins within minutes of inhalation, and the duration extends beyond 24 hours, supporting once-daily dosing. The bronchodilation is predominantly a local site-specific effect in the airways.

Vilanterol is a selective, long-acting beta-2 adrenergic receptor agonist (LABA) that activates adenylyl cyclase in airway smooth muscle cells, increasing intracellular cyclic AMP and producing sustained relaxation of bronchial smooth muscle. Its duration of action exceeds 24 hours after a single inhaled dose. By combining muscarinic blockade (cholinergic pathway) with beta-2 stimulation (adrenergic pathway), Anoro Ellipta achieves additive bronchodilation greater than either agent alone, through two mechanistically distinct pathways.

ADME Profile

ParameterValueClinical Implication
AbsorptionUMEC: Tmax 5–15 min; negligible oral bioavailability. VI: rapid pulmonary absorption; negligible contribution from swallowed portionBronchodilation onset within minutes; systemic exposure is primarily from the lung-absorbed fraction
DistributionUMEC: Vd 86 L (IV), protein binding ~89%. VI: Vd 165 L (SS), protein binding ~94%Both distribute beyond plasma volume; moderate-to-high protein binding limits free systemic drug
MetabolismUMEC: primarily CYP2D6 (O-dealkylation, hydroxylation, conjugation); CYP2D6 poor metaboliser status does not clinically alter exposure. VI: CYP3A4 (O-dealkylation) to inactive metabolitesStrong CYP3A4 inhibitors increase vilanterol systemic exposure and cardiovascular effects; no dose adjustment needed for CYP2D6 polymorphisms
EliminationUMEC: t½ ~11 h (effective); faecal 58%, urinary 22%. VI: t½ ~11 h (effective); urinary 70%, faecal 30%Both support once-daily dosing; no dose adjustment needed for renal or moderate hepatic impairment
SE

Side Effects

1–10%Common (Four 6-Month Trials; ≥1% and > Placebo)
Adverse EffectIncidence (Anoro / Placebo)Clinical Note
Pharyngitis2% / <1%Most commonly reported adverse event; generally mild sore throat
Diarrhoea2% / 1%Usually mild and self-limiting; no dose adjustment needed
Pain in extremity2% / 1%Musculoskeletal complaint; not clearly dose-related
Sinusitis1% / <1%Comparable to rates seen with other inhaled bronchodilators
Lower respiratory tract infection1% / <1%No ICS component means no additional pneumonia risk vs LAMA/LABA class
Constipation1% / <1%Anticholinergic class effect from umeclidinium; advise adequate hydration and fibre intake
Muscle spasms1% / <1%LABA class effect; usually transient tremor or cramping
Neck pain1% / <1%Musculoskeletal; relationship to drug uncertain
Chest pain1% / <1%Non-cardiac in most cases; evaluate cardiovascular causes if persistent or severe

No adverse events reached the ≥10% (Very Common) threshold in clinical trials. Additional AEs from a 12-month safety trial (at the 125/25 mcg dose) included headache, back pain, cough, UTI, arthralgia, nausea, vertigo, abdominal pain, pleuritic pain, viral respiratory tract infection, toothache, and diabetes mellitus — all at ≥1% and more frequent than placebo.

SeriousSerious (Regardless of Frequency)
Adverse EffectEstimated FrequencyTypical OnsetRequired Action
Paradoxical bronchospasmRareImmediately after inhalationTreat with rescue SABA; permanently discontinue Anoro; switch to alternative
Anaphylaxis / angioedemaVery rare (postmarketing)Minutes to hours after doseEmergency treatment; permanent discontinuation; do not rechallenge
Acute narrow-angle glaucomaRare; LAMA class effectHours to daysEmergency ophthalmology referral; discontinue if confirmed
Urinary retentionUncommon; LAMA class effectDays to weeksDiscontinue if significant; urology referral; higher risk with BPH
Cardiac arrhythmias (atrial fibrillation, ventricular/supraventricular extrasystoles)Rare (postmarketing)VariableECG monitoring; discontinue if clinically significant; cardiology referral
Myocardial infarctionVery rare (postmarketing)VariableEmergency cardiac care; discontinue; MACE rate in IMPACT trial was 2.2/100 pt-yr for UMEC/VI arm
DiscontinuationDiscontinuation Rates
6-Month Efficacy Trials
Low overall comparable to placebo and active comparators
Top reasons: COPD exacerbation was the most common reason; no single adverse event predominated as a discontinuation driver
12-Month Safety Trial
Safety profile consistent with 6-month data
Key finding: No new safety signals at 12 months; no clinically significant changes in blood chemistry, haematology, or ECG
No ICS Component — Pneumonia Risk Advantage

Unlike ICS-containing triple therapy combinations, Anoro Ellipta does not carry the increased pneumonia risk associated with inhaled corticosteroids. In the IMPACT trial, the pneumonia incidence was 5% with umeclidinium-vilanterol compared with 8% in the ICS-containing triple therapy arm (Trelegy). This makes Anoro Ellipta a favourable option for COPD patients who do not have an eosinophilic phenotype or frequent exacerbations warranting ICS.

Int

Drug Interactions

Vilanterol is a CYP3A4 substrate, so strong CYP3A4 inhibitors are the most significant pharmacokinetic interaction. Umeclidinium interactions relate primarily to additive anticholinergic effects. Vilanterol also has pharmacodynamic interactions involving QTc prolongation, beta-blocker antagonism, and additive sympathomimetic effects.

MajorStrong CYP3A4 Inhibitors (e.g., ketoconazole, ritonavir, itraconazole, clarithromycin)
MechanismInhibition of CYP3A4-mediated vilanterol metabolism
EffectIncreased vilanterol systemic exposure; heightened cardiovascular beta-agonist effects
ManagementUse with caution; monitor for cardiovascular effects (tachycardia, QTc prolongation)
FDA PI
MajorOther Anticholinergics (e.g., tiotropium, ipratropium, aclidinium, glycopyrrolate)
MechanismAdditive anticholinergic burden from duplicate muscarinic antagonism
EffectIncreased risk of urinary retention, constipation, dry mouth, glaucoma exacerbation
ManagementAvoid co-administration; Anoro already contains a LAMA
FDA PI
MajorOther LABAs (e.g., salmeterol, formoterol, indacaterol, olodaterol)
MechanismDuplicate LABA pharmacology
EffectBeta-agonist overdose: tachycardia, arrhythmias, tremor, hypokalaemia; potentially fatal
ManagementAbsolutely contraindicated — never combine with another LABA-containing product
FDA PI
MajorNon-selective Beta-Blockers (e.g., propranolol, carvedilol)
MechanismAntagonism of vilanterol’s beta-2 bronchodilatory effect
EffectLoss of bronchodilation; risk of severe bronchospasm in COPD
ManagementUse cardioselective beta-1 blockers with caution if absolutely needed
FDA PI
ModerateMAO Inhibitors, Tricyclic Antidepressants, and QTc-Prolonging Drugs
MechanismPotentiation of vilanterol’s adrenergic cardiovascular effects; additive QTc prolongation
EffectHeightened cardiovascular stimulation, arrhythmia risk
ManagementUse with extreme caution; consider ECG monitoring; avoid use within 2 weeks of MAOI discontinuation
FDA PI
ModerateNon-Potassium-Sparing Diuretics
MechanismAdditive hypokalaemia from renal loss (diuretic) plus intracellular shift (vilanterol)
EffectECG changes, increased arrhythmia risk
ManagementMonitor serum potassium and ECG; supplement as needed
FDA PI
Mon

Monitoring

  • Lung Function (FEV1)Baseline, then every 3–6 months
    Routine
    Assess bronchodilator response. Improvement in trough FEV1 should be evident within 1–2 weeks. Declining values or increased rescue use may signal need for step-up to triple therapy.
  • COPD Exacerbation FrequencyEach visit
    Routine
    Track exacerbation history. If exacerbations persist despite LAMA/LABA therapy, assess blood eosinophils and consider adding an ICS (stepping up to triple therapy).
  • Ophthalmological SymptomsEach visit in at-risk patients
    Trigger-based
    LAMA class risk for narrow-angle glaucoma. Ask about eye pain, blurred vision, visual halos. Urgent referral if acute symptoms develop.
  • Urinary SymptomsEach visit in at-risk patients
    Trigger-based
    LAMA class effect: monitor for urinary retention in patients with prostatic hyperplasia or bladder-neck obstruction.
  • Cardiovascular StatusBaseline and as indicated
    Trigger-based
    Vilanterol can increase heart rate and blood pressure. Monitor patients with coronary insufficiency, arrhythmias, or hypertension. MACE rate was 2.2/100 patient-years in the IMPACT trial.
  • Serum PotassiumWhen concurrent diuretics or digoxin
    Trigger-based
    Beta-agonists can cause transient hypokalaemia via intracellular shift. In the 6-month COPD trials, no clinically significant treatment effect on potassium was observed at standard doses.
CI

Contraindications & Cautions

Absolute Contraindications

  • Asthma: Anoro Ellipta is NOT indicated for asthma. Use of LABA without ICS in asthma patients is associated with increased asthma-related death (LABA class effect). The PI explicitly contraindicates use of vilanterol without an ICS in patients with asthma.
  • Severe hypersensitivity to milk proteins — the Ellipta inhaler contains lactose monohydrate with milk proteins.
  • Known hypersensitivity to umeclidinium, vilanterol, or any excipient.

Relative Contraindications (Specialist Input Recommended)

  • Narrow-angle glaucoma: Umeclidinium may precipitate or worsen acute angle-closure glaucoma.
  • Prostatic hyperplasia or bladder-neck obstruction: Anticholinergic effects may worsen urinary retention.
  • Severe cardiovascular disease: Coronary insufficiency, arrhythmias, or hypertension may be exacerbated by vilanterol’s beta-adrenergic effects.

Use with Caution

  • Convulsive disorders: Beta-agonists can lower seizure threshold.
  • Thyrotoxicosis: Vilanterol may exacerbate symptoms.
  • Diabetes mellitus / ketoacidosis: Beta-agonists can cause transient hyperglycaemia.
  • Severe hepatic impairment: Not studied; UMEC exposure may increase.
FDA Class-Wide Regulatory Warning LABA Use in Asthma — Risk of Asthma-Related Death

LABA monotherapy (without ICS) is associated with an increased risk of asthma-related death. The SMART trial showed a relative risk of 4.37 (95% CI: 1.25–15.34) for salmeterol monotherapy compared with placebo. This is a class effect of all LABAs, including vilanterol. Anoro Ellipta does not contain an ICS and is therefore explicitly contraindicated for asthma use. Available data do not suggest an increased risk of death with LABA use in COPD patients. For COPD patients who also have asthma features or require anti-inflammatory therapy, consider ICS-containing alternatives such as Trelegy Ellipta or Breo Ellipta.

Pt

Patient Counselling

Purpose of Therapy

Anoro Ellipta is a once-daily maintenance inhaler for COPD that combines two bronchodilators to keep airways open and reduce flare-ups. It is not a rescue inhaler and will not relieve sudden breathing difficulty. Patients must always carry a separate short-acting rescue inhaler. Anoro Ellipta is for COPD only and must never be used for asthma.

How to Take

Use Anoro once daily at the same time each day. Open the cover of the Ellipta inhaler fully until you hear a click (this loads the dose). Breathe out gently away from the inhaler, then place the mouthpiece in your mouth and breathe in steadily and deeply. Hold your breath for 3–4 seconds, then breathe out slowly. Close the cover. Unlike steroid-containing inhalers, mouth rinsing after each dose is not required. Discard the inhaler 6 weeks after opening the foil tray or when the dose counter reads 0, whichever comes first.

Not for Asthma
Tell patientThis medicine is only for COPD. It does not contain a steroid and should never be used for asthma, as this could increase the risk of serious asthma problems including death.
Call prescriberIf you have been diagnosed with asthma or suspect you may have asthma symptoms, inform your prescriber immediately so appropriate therapy can be arranged.
Eye Symptoms
Tell patientThe anticholinergic component can very rarely affect the eyes. Report any sudden eye pain, blurred vision, seeing halos around lights, or red eyes immediately.
Call prescriberSeek urgent care if sudden eye symptoms develop — this may indicate acute glaucoma requiring emergency treatment.
Urinary Difficulty
Tell patientSome patients (especially men with prostate enlargement) may experience difficulty passing urine or a feeling of incomplete bladder emptying.
Call prescriberIf you develop painful urination, weak stream, or inability to urinate.
Worsening COPD Symptoms
Tell patientIf your COPD symptoms worsen over time or you need your rescue inhaler more often, do not increase the dose of Anoro. This is a signal that your treatment regimen needs review.
Call prescriberContact your healthcare provider promptly if breathing worsens. Seek emergency care if your rescue inhaler does not relieve sudden breathlessness.
Heart-Related Side Effects
Tell patientVilanterol can occasionally cause a fast or pounding heartbeat, tremor, or chest discomfort. These are usually mild.
Call prescriberIf you experience persistent chest pain, rapid irregular heartbeat, or severe tremor.
Ref

Sources

Regulatory (PI / SmPC)
  1. Anoro Ellipta (umeclidinium and vilanterol) Prescribing Information. GlaxoSmithKline. Revised June 2025. DailyMedPrimary source for all dosing, contraindications, adverse reaction data, and pharmacokinetic parameters in this monograph.
  2. Anoro Ellipta FDA Label Archive. AccessData. FDA.govHistorical label revision documenting updated warnings and safety data including IMPACT trial cardiovascular outcomes.
Key Clinical Trials
  1. Decramer M, Anzueto A, Kerwin E, et al. Efficacy and safety of umeclidinium plus vilanterol versus tiotropium, vilanterol, or umeclidinium monotherapies over 24 weeks in patients with chronic obstructive pulmonary disease: results from two multicentre, blinded, randomised controlled trials. Lancet Respir Med. 2014;2(6):472-486. doi:10.1016/S2213-2600(14)70065-7Pivotal Trial 1 and Trial 2 demonstrating superiority of UMEC/VI over individual components and tiotropium in trough FEV1 improvement.
  2. Maleki-Yazdi MR, Kaelin T, Richard N, et al. Efficacy and safety of umeclidinium/vilanterol 62.5/25 mcg and tiotropium 18 mcg in chronic obstructive pulmonary disease: results of a 24-week, randomized, controlled trial. Respir Med. 2014;108(12):1752-1760. doi:10.1016/j.rmed.2014.10.002Head-to-head trial vs tiotropium showing non-inferior to superior trough FEV1 with UMEC/VI; contributed to the four 6-month trial pooled safety data.
  3. Lipson DA, Barnhart F, Brealey N, et al. Once-daily single-inhaler triple versus dual therapy in patients with COPD (IMPACT). N Engl J Med. 2018;378(18):1671-1680. doi:10.1056/NEJMoa171390152-week trial including UMEC/VI arm (n=2,070); source of MACE rate and pneumonia advantage data (5% vs 8% triple therapy).
  4. Feldman GJ, Sousa AR, Lipson DA, et al. Comparative efficacy of umeclidinium/vilanterol and tiotropium/olodaterol in symptomatic COPD: a randomized trial. Adv Ther. 2017;34(11):2518-2533. doi:10.1007/s12325-017-0626-4Head-to-head crossover trial vs STIOLTO showing superiority of UMEC/VI in trough FEV1 at 8 weeks.
Guidelines
  1. Global Initiative for Chronic Obstructive Lung Disease (GOLD). Global Strategy for Prevention, Diagnosis and Management of COPD, 2024 Report. goldcopd.orgPositions LAMA/LABA dual bronchodilator therapy as first-line for symptomatic COPD patients (Group B/E without high eosinophils).
Mechanistic / Basic Science
  1. Salmon M, Luttmann MA, Foley JJ, et al. Pharmacological characterization of GSK573719 (umeclidinium): a novel, long-acting, inhaled antagonist of the muscarinic cholinergic receptors for treatment of pulmonary diseases. J Pharmacol Exp Ther. 2013;345(2):260-270. doi:10.1124/jpet.112.202051Characterises umeclidinium’s prolonged M3 receptor antagonism and >24-hour bronchodilatory effect.
  2. Slack RJ, Barrett VJ, Morrison VS, et al. In vitro pharmacological characterization of vilanterol, a novel long-acting beta2-adrenoceptor agonist with 24-hour duration of action. J Pharmacol Exp Ther. 2013;344(1):218-230. doi:10.1124/jpet.112.198481Establishes vilanterol’s 24-hour duration of action and beta-2 receptor selectivity, supporting once-daily dosing.
  3. Cazzola M, Molimard M. The scientific rationale for combining long-acting beta2-agonists and muscarinic antagonists in COPD. Pulm Pharmacol Ther. 2010;23(4):257-267. doi:10.1016/j.pupt.2010.03.003Reviews the mechanistic rationale for LAMA/LABA combination, explaining additive bronchodilation through distinct cholinergic and adrenergic pathways.
Pharmacokinetics / Special Populations
  1. Mehta R, Engel M, Engel B, et al. Population pharmacokinetic analysis of umeclidinium and vilanterol in patients with chronic obstructive pulmonary disease. Clin Pharmacokinet. 2017;56(8):943-953. doi:10.1007/s40262-016-0486-yPopulation PK analysis confirming that age, race, gender, and CYP2D6 metaboliser status do not clinically alter UMEC or VI exposure.