Peringatan Keamanan

There is no information regarding the lethal dose 50 of ensifentrine. An overdosage of ensifentrine may lead to signs and symptoms such as headache, tachycardia, and palpitations. Treatment of overdosage consists of temporary interruption of ensifentrine along with appropriate symptomatic and/or supportive therapy.L50893

Ensifentrine

DB16157

small molecule approved investigational

Deskripsi

Ensifentrine is a first-in-class, selective dual inhibitor of the phosphodiesterase 3 (PDE3) and phosphodiesterase 4 (PDE4) enzymes.L50903 On June 26, 2024, the FDA announced the approval of an inhaled product of ensifentrine for the treatment of chronic obstructive pulmonary disease (COPD) in adults, which allows the drug to be directly delivered to the lungs.L50903 It works to induce bronchodilator and reduce inflammation in COPD.A263913

Struktur Molekul 2D

Berat 477.565
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) Following twice-daily administration for 6 days, terminal elimination half-life ranged from 10.6 to 12.6 hours in healthy subjects and subjects with COPD (1.5 mg to 12 mg twice daily).[L50893]
Volume Distribusi Apparent central and peripheral volume of distribution for ensifentrine in healthy subjects were 2700 L and 1820 L, respectively, as estimated in population PK analysis. In patients with COPD, apparent central and peripheral volumes were estimated as 8150 L and 5490 L, respectively.[L50893]
Klirens (Clearance) -

Absorpsi

Following inhaled administration of ensifentrine in healthy subjects and subjects with COPD, ensifentrine Cmax was attained around 0.6 to 1.5 hours after dosing. A randomized, two-period, cross-over study assessing systemic exposure following inhalation of two times the recommended dose of ensifentrine with and without charcoal block demonstrated that the majority of an inhaled dose (approximately 90%) is delivered to the lung from which it is absorbed.L50893 Population pharmacokinetic analysis indicates that relative bioavailability in subjects with COPD is approximately 35% lower when compared to healthy subjects. Exposure to ensifentrine was associated with high inter-subject variability.L50893

Metabolisme

Following administration of a single nebulized dose, 8 times the recommended dose of ensifentrine, unchanged ensifentrine was identified as the major drug-related component in human plasma, accounting for 96 and 99% of the drug-related material identified in Tmax and time normalized (0-24 h) plasma samples, respectively. The primary metabolic routes for ensifentrine are oxidative (hydroxylation, O-demethylation) followed by conjugation (e.g., glucuronidation). In vitro results indicate that, at physiologically relevant concentrations, ensifentrine was predominantly metabolized by CYP2C9 and to a lesser extent by CYP2D6.L50893

Rute Eliminasi

The majority of ensifentrine is excreted in feces. After a 3 mg nebulized dose, urinary elimination of unchanged ensifentrine was negligible (<0.3% of the dose).L50893

Interaksi Obat

1 Data
Isosorbide mononitrate Ensifentrine may increase the hypotensive activities of Isosorbide mononitrate.

Target Protein

Phosphodiesterase 3 PDE3A
Phosphodiesterase 4 PDE4A

Referensi & Sumber

Artikel (PubMed)
  • PMID: 33012706
    Turner MJ, Dauletbaev N, Lands LC, Hanrahan JW: The Phosphodiesterase Inhibitor Ensifentrine Reduces Production of Proinflammatory Mediators in Well Differentiated Bronchial Epithelial Cells by Inhibiting PDE4. J Pharmacol Exp Ther. 2020 Dec;375(3):414-429. doi: 10.1124/jpet.120.000080. Epub 2020 Oct 4.
  • PMID: 37364283
    Anzueto A, Barjaktarevic IZ, Siler TM, Rheault T, Bengtsson T, Rickard K, Sciurba F: Ensifentrine, a Novel Phosphodiesterase 3 and 4 Inhibitor for the Treatment of Chronic Obstructive Pulmonary Disease: Randomized, Double-Blind, Placebo-controlled, Multicenter Phase III Trials (the ENHANCE Trials). Am J Respir Crit Care Med. 2023 Aug 15;208(4):406-416. doi: 10.1164/rccm.202306-0944OC.
  • PMID: 37533771
    Donohue JF, Rheault T, MacDonald-Berko M, Bengtsson T, Rickard K: Ensifentrine as a Novel, Inhaled Treatment for Patients with COPD. Int J Chron Obstruct Pulmon Dis. 2023 Jul 28;18:1611-1622. doi: 10.2147/COPD.S413436. eCollection 2023.
  • PMID: 38188891
    Faruqi MA, Khan MMKS, Mannino DM: Perspectives on Ensifentrine and Its Therapeutic Potential in the Treatment of COPD: Evidence to Date. Int J Chron Obstruct Pulmon Dis. 2024 Jan 3;19:11-16. doi: 10.2147/COPD.S385811. eCollection 2024.

Contoh Produk & Brand

Produk: 1 • International brands: 0
Produk
  • Ohtuvayre
    Suspension • 3 mg/2.5mL • Respiratory (inhalation) • US • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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