Peringatan Keamanan

No systemic signs of overdose are expected following topical application of Anzupgo due to the minimal systemic absorption of delgocitinib.L51589 There is no information regarding the LD50 of delgocitinib.

Delgocitinib

DB16133

small molecule investigational

Deskripsi

Delgocitinib is a pan-Janus kinase (JAK) inhibitor. After the first global approval in Japan,A264693 delgocitinib was also approved by the European Commission on September 23, 2024.L51913 It works to reduce the inflammatory response in inflammatory skin disorders.A264703

Struktur Molekul 2D

Berat 310.361
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Following repeated topical application of delgocitinib cream, the average half-life of delgocitinib was estimated to be 20.3 hours.[L51589]
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

The pharmacokinetics of delgocitinib cream were evaluated in a study involving 15 adult patients 22 to 69 years of age with moderate to severe CHE. Patients applied on average 0.87 g of delgocitinib 20 mg/g cream to the affected areas of the hands and wrists twice a day for 8 days.L51589 The geometric mean (GSD) maximum plasma concentration (Cmax) and area under the concentrationcurve from time 0 to 12 hours (AUC0-12) on Day 8 was 0.46 ng/mL (1.74) and 3.7 ng x h/mL (1.74), respectively. Steady state was reached by Day 8. The systemic exposure (AUC and Cmax) between Day 1 and Day 8 were similar. Following twice daily application of delgocitinib 20 mg/g cream in DELTA 2, the geometric mean plasma concentration observed 2-6 hours after application at Day 113 was 48% lower than that at Day 8 (0.11 ng/mL and 0.21 ng/mL, respectively). The relative bioavailability of delgocitinib following topical application is approximately 0.6% compared to administration via oral tablets.L51589

Metabolisme

There is limited metabolism of delgocitinib.L51589

Rute Eliminasi

Delgocitinib is primarily eliminated by renal excretion as approximately 70-80% of the total dose after oral administration was found unchanged in the urine.L51589

Interaksi Obat

0 Data
Tidak ada data.

Target Protein

Tyrosine-protein kinase JAK1 JAK1
Tyrosine-protein kinase JAK2 JAK2
Tyrosine-protein kinase JAK3 JAK3
Non-receptor tyrosine-protein kinase TYK2 TYK2

Referensi & Sumber

Artikel (PubMed)
  • PMID: 32166597
    Dhillon S: Delgocitinib: First Approval. Drugs. 2020 Apr;80(6):609-615. doi: 10.1007/s40265-020-01291-2.
  • PMID: 35084738
    Worm M, Thyssen JP, Schliemann S, Bauer A, Shi VY, Ehst B, Tillmann S, Korn S, Resen K, Agner T: The pan-JAK inhibitor delgocitinib in a cream formulation demonstrates dose response in chronic hand eczema in a 16-week randomized phase IIb trial. Br J Dermatol. 2022 Jul;187(1):42-51. doi: 10.1111/bjd.21037. Epub 2022 Apr 19.
  • PMID: 32029304
    Nakagawa H, Nemoto O, Igarashi A, Saeki H, Kaino H, Nagata T: Delgocitinib ointment, a topical Janus kinase inhibitor, in adult patients with moderate to severe atopic dermatitis: A phase 3, randomized, double-blind, vehicle-controlled study and an open-label, long-term extension study. J Am Acad Dermatol. 2020 Apr;82(4):823-831. doi: 10.1016/j.jaad.2019.12.015. Epub 2020 Feb 3.
  • PMID: 26115905
    Amano W, Nakajima S, Kunugi H, Numata Y, Kitoh A, Egawa G, Dainichi T, Honda T, Otsuka A, Kimoto Y, Yamamoto Y, Tanimoto A, Matsushita M, Miyachi Y, Kabashima K: The Janus kinase inhibitor JTE-052 improves skin barrier function through suppressing signal transducer and activator of transcription 3 signaling. J Allergy Clin Immunol. 2015 Sep;136(3):667-677.e7. doi: 10.1016/j.jaci.2015.03.051. Epub 2015 Jun 24.

Contoh Produk & Brand

Produk: 0 • International brands: 0
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Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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