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ensifentrine

Inhaled PDE3/PDE4 dual inhibitor (bronchodilator + anti-inflammatory) · Bronchodilator

START
3 mg via jet nebuliser twice daily
TYPICAL MAX
6 mg/day
STOP IF
Paradoxical bronchospasm or hypersensitivity
WATCH
Inhaler technique (jet nebuliser only — not mesh); not for acute use
CDSCO approvedATC R03BX01
Dose laddermg/d
3per dose6max/day
Renal dose adjustmenteGFR mL/min/1.73m²
FULLNo dose adjustment at any eGFR90

KDIGO 2024 + manufacturer label

Pharmacokineticsplasma · t hours
15minONSET1hPEAK7h12hDURATION
ONSET
15min · absorption
PEAK
1h · Tmax
7h ·
DURATION
12h · BID
EXCRETION
Mainly faecal; minor renal
route + CYP
INTERACTIONS
none in our sources
PREGNANCY
Limited data; use only if benefit outweighs risk.
FDA category + note

Mechanism

Selective dual inhibitor of phosphodiesterase 3 (smooth-muscle bronchodilation) and phosphodiesterase 4 (anti-inflammatory) delivered by nebuliser — combines mechanism of both LABAs and anti-inflammatory inhalers in a single molecule.

Indications

Maintenance treatment of COPD

Dosing

Adult
3 mg via standard jet nebuliser twice daily (12 h apart).
Pediatric
Not established.
Renal adjustment
No adjustment (inhaled, low systemic exposure).
Hepatic adjustment
No adjustment.
Geriatric
No specific adjustment.
Max dose
6 mg/day (3 mg twice daily)

Pharmacokinetics

Onset
Bronchodilation within minutes; steady benefit over weeks
Peak effect
~1 h (after nebulisation)
Duration
~12 h (twice-daily)
Half-life
~7 h
Bioavailability
Low systemic; lung deposition delivers active drug
Protein binding
~95%
Metabolism
Hepatic (minimal CYP3A4)
Excretion
Mainly faecal; minor renal

Contraindications

  • Hypersensitivity
  • Acute bronchospasm (not for rescue use)

Side effects

Common
CoughNasopharyngitisHeadacheDiarrhoeaBack pain
Serious
  • Paradoxical bronchospasm (rare)
  • Severe hypersensitivity

Pregnancy & lactation

Pregnancy

Limited data; use only if benefit outweighs risk.

Lactation

Limited data; weigh benefit/risk.

Drug interactions

Anticholinergic Inhalers
Mild
Database

Complementary (intended)

Standard combination

Source: Kimi deep-research + Cla

Beta Agonists
Mild
Database

Complementary effects (intended)

Standard combination COPD therapy

Source: Kimi deep-research + Cla

Other Pde Inhibitors
Mild
Database

Mechanism overlap

Monitor tolerability

Source: Kimi deep-research + Cla

Strong Cyp3a4 Inhibitors
Mild
Database

Limited metabolism implications

Routine monitoring

Source: Kimi deep-research + Cla

Theophylline
Mild
Database

Both PDE-acting; minimal additive at inhaled doses

Routine monitoring

Source: Kimi deep-research + Cla

Related guidelines

Ask House about ensifentrine

Continue into a citation-backed clinical answer with the drug context already attached.

Sources: Goodman & Gilman 14e·Verified: 2026-05-20 · House clinical team·Cockpit curated: 2026-05-20