Ohtuvayre (ensifentrine)
Phosphodiesterase-4 (PDE4) inhibitors Inhalation Ampul For Nebulization (Ml)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Ensifentrine is a selective, dual phosphodiesterase 3 (PDE3) and phosphodiesterase 4 (PDE4) inhibitor.
Ensifentrine is a selective dual inhibitor of phosphodiesterase 3 (PDE3) and phosphodiesterase 4 (PDE4) with bronchodilator and anti-inflammatory effects. PDE3 hydrolyzes cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP) present in airway smooth muscle, which mediates bronchial tone. PDE4 hydrolyzes cAMP and is involved in inflammatory cell activation and migration and cystic fibrosis transmembrane conductance regulator stimulation in bronchial epithelial cells.
Dual inhibition of PDE3 and PDE4 has demonstrated more synergistic effects when compared to inhibition of PDE3 or PDE4 alone on contraction of airway smooth muscle and suppression of the inflammatory response.
Following twice-daily dosing of ensifentrine, steady state was attained by Day 3. Population pharmacokinetic analysis predicts that accumulation of ensifentrine may be higher in patients with COPD compared to healthy subjects. Peak plasma concentrations and AUC are predicted to be 1.3- and 1.4-fold in healthy patients compared to 1.4- and 1.5-fold in patients with COPD.
Ensifentrine exposure was associated with high inter-subject variability.
Following administration of ensifentrine in healthy patients and those with COPD, peak plasma concentrations were attained approximately 0.6 to 1.5 hours after dosing. Clinical studies have demonstrated that the majority of the inhaled dose (approximately 90%) is delivered to the lung and absorbed. Ensifentrine is 90% bound to plasma protein.
Ensifentrine is metabolized by oxidation, conjugation, CYP2C9, and CYP2D6, and is largely identified as unchanged drug in plasma. The majority of drug is excreted in feces; urinary elimination is negligible (<0.3% of the dose). The elimination half life ranges from 10.6 to 12.6 hours.
USES: This medication is used to treat and control symptoms (wheezing and shortness of breath) caused by ongoing lung disease (chronic obstructive pulmonary disease-COPD which includes bronchitis and emphysema). Ensifentrine works by reducing the swelling of the airways and the muscles around the airways so you can breathe more easily. Controlling symptoms of breathing problems can decrease time lost from work or school.
This medication must be used regularly to be effective. It does not work right away and should not be used to relieve sudden shortness of breath or wheezing. If sudden breathing problems occur, use your quick-relief inhaler (such as albuterol, also called salbutamol in some countries) as prescribed.
Generic name: ensifentrine
Pronunciation: (EN-si-FEN-treen)
Drug class: Phosphodiesterase-4 (PDE4) inhibitors
Therapeutic class: Respiratory Therapy Agents
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Ohtuvayre
Indications
The following indications are listed for Ohtuvayre:
- Chronic Obstructive Pulmonary Disease
Dosing
No dosing information is available for this tab.
Administer ensifentrine by oral inhalation via a standard jet nebulizer using a mouthpiece connected to an air compressor. Ensifentrine should not be injected or swallowed.
Administer the drug twice daily, once in the morning and once in the evening.
Ensifentrine is available as a sterile, yellow to pale yellow, aqueous suspension in 3 mg/2.5 mL unit-dose ampules. Store the unit-dose ampules in the protective foil pouch at controlled room temperature (20-25degreesC). Protect from light and excessive heat and do not freeze.
Remove ensifentrine unit-dose ampule from foil pouch immediately before use and shake vigorously to ensure complete resuspension of the active ingredient. Squeeze and completely empty contents of the ampule into the nebulizer cap for administration by oral inhalation; discard ampule with any remaining content. Do not mix ensifentrine with other drugs or add to solutions containing other drugs.
| Drug label | Dosing type | Instructions |
|---|---|---|
| Ohtuvayre 3 Mg/2.5Ml Inhal Sus | Maintenance | Inhale 2.5 milliliters (3 mg) by nebulization route 2 times per day in the morning and evening. |
No dosing information is available for this tab.
Drug interactions
In vitro studies indicate that ensifentrine is metabolized predominantly by cytochrome P-450 (CYP) isoenzyme CYP2C9 and to a lesser extent by CYP2D6.
In vitro studies indicate that ensifentrine does not inhibit CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, or CYP3A4.
In vitro studies indicate that ensifentrine does not inhibit breast cancer resistance protein (BCRP), P-glycoprotein (P-gp), organic anion transporting polypeptides 1B1 (OATP1B1), OATP1B3, organic anion transporter 1 (OAT1), OAT3, organic cation transporter 2 (OCT2), multidrug and toxin extrusion protein (MATE1), or MATE2-K.
In vitro studies indicate that ensifentrine is a substrate of breast cancer resistance protein (BCRP) and is not a substrate of P-gp, OATP1B1, or OATP1B3.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
*Known hypersensitivity to ensifentrine or any component of the product.
There are no contraindication contraindications for this drug.
- Depression
- Suicidal ideation
- Child-pugh class B hepatic impairment
- Child-pugh class C hepatic impairment
- Disease of liver
Adverse reactions
The most common adverse reactions (incidence greater and equal to 1% and more common than placebo) reported with ensifentrine in clinical studies include back pain, hypertension, urinary tract infection, and diarrhea.
There are no severe adverse reactions for this drug.
More Frequent
- Back pain
- Diarrhea
- Hypertension
- Urinary tract infection
Precautions
No enhanced messaging available.
Safety and efficacy of ensifentrine have not been established in pediatric patients.
There are no available data on ensifentrine use in pregnant women to evaluate for a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes.
In animal studies, ensifentrine exposures at 30 times the maximum recommended human daily inhalation dose in male rats for the 10 weeks prior to mating with untreated female rates resulted in increased pre- and post-implantation loss and decreased live embryos. Following administration in pregnant rabbits and rats, no adverse developmental effects were observed during organogenesis at exposures up to 9 to 79 times the maximum recommended human daily inhalation dose, respectively. In pregnant rats, no adverse developmental effects were observed from organogenesis through lactation at exposures up to 79 times the maximum recommended human inhalation dose.
It is not known whether ensifentrine is distributed into human milk. Effects of the drug on breast-fed infants or milk production are also not known. There are no data from animal studies on the presence of ensifentrine in milk.
The manufacturer makes no dosage recommendations for geriatric patients.
In the ENHANCE trials, among patients randomized to receive ensifentrine, 534 (55%) and 84 (9%) were 65 years of age or older and 75 years of age or older, respectively. No differences in safety or efficacy have been observed between these geriatric and younger patients. However, greater sensitivity to ensifentrine in older patients cannot be ruled out.
ICD codes
| Code | Type | Description |
|---|---|---|
| Chronic obstructive pulmonary disease | ||
| J44 | ICD10CM | Other chronic obstructive pulmonary disease |
| J44.8 | ICD10CM | Other specified chronic obstructive pulmonary disease |
| J44.89 | ICD10CM | Other specified chronic obstructive pulmonary disease |
| J44.9 | ICD10CM | Chronic obstructive pulmonary disease, unspecified |
ICD code information from First Databank (FDB).
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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