Ensifentrine

OHTUVAYRE

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Pronunciation: en-si-FEN-treen (OE-too-vair)

Ensifentrine ballicule: receptor binding, kinetics and half-life diagram — Mechanism of action: Ensifentrine ballicule

What it isNebulized dual PDE3 and PDE4 inhibitor; maintenance treatment of COPD.

Why this oneIts dual action combines airway smooth-muscle relaxation with a nonsteroidal anti-inflammatory effect.

What limits itTwice-daily nebulization adds only modest benefit to existing inhalers; headache and diarrhea can limit use.

Ensifentrine molecular structure (skeletal formula) — Molecular structure: Ensifentrine

FDA label

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FDA dosing	Population	Start	Target	Max
COPD (maintenance)	Adults	Inhaled via standard jet nebulizer: 3 mg (one unit-dose ampule) BID (morning and evening)	Same	Inhaled 3 mg BID

Renal Mild-moderate: no adjustment needed; severe: not evaluated

Hepatic Use with caution — systemic exposure increased 2.3-fold in moderate/severe hepatic impairment (no specific dose adjustment given)

Instructions

Administer by oral inhalation using a standard jet nebulizer with mouthpiece connected to an air compressor
Remove ampule from foil pouch only immediately before use; once pouch opened, discard unused ampules after 14 days
Shake ampule vigorously; squeeze entire contents into nebulizer cup; discard ampule with residual content
Do not mix with other drugs or add to solutions containing other drugs (compatibility not established)

Available strengths

susp 3 mg/2.5 mL

Cautions

Not for acute bronchospasm relief (not rescue therapy) — treat acute symptoms with an inhaled short-acting bronchodilator
Paradoxical bronchospasm (may be life-threatening) — treat with SABA, discontinue immediately, institute alternative therapy
Psychiatric adverse reactions incl. suicidality reported (suicide attempt and completed suicide in trials) — carefully weigh risks/benefits in patients with history of depression and/or suicidal thoughts or behavior

Adverse reactions

>=1% and more common than placebo: back pain, hypertension, urinary tract infection, diarrhea
Psychiatric: insomnia, anxiety, depression-related reactions

Pregnancy No human data; no adverse developmental effects in rats/rabbits at up to 79x/9x MRHDID exposure; male rat fertility effects (implantation loss, decreased live embryos) at 30x MRHDID

Lactation No human or animal milk data — weigh benefit/risk

Cost

Ensifentrine (OHTUVAYRE)

Strength		#/mo	generic $/unit	CostPlus
3 mg/2.5 mL	susp	per unit		not offered

NADAC is a voluntary CMS survey of what retail community pharmacies pay for the drugs they stock. Ensifentrine is dispensed outside retail pharmacies, so it rarely appears on surveyed invoices.

NO BOXED WARNINGS

Principal riskModest added benefit; nebulised twice daily

Classes and tags

Clinical profile

Therapeutic safety burden1 / 4

Overdose danger1 / 4

Weight-gain liability0 / 4

Sedation liability0 / 4

QT / Torsades0 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk2 / 4

Legacy pregnancy categoryN/A (post-2015 labeling)

Defining liabilityPsychiatric adverse reactions and paradoxical bronchospasm

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