Molnupiravir

DB15661

small molecule investigational

Deskripsi

Molnupiravir (EIDD-2801, MK-4482) is the isopropylester prodrug of N4-hydroxycytidine.A193014,A193026 With improved oral bioavailability in non-human primates, it is hydrolyzed in vivo, and distributes into tissues where it becomes the active 5’-triphosphate form.A193026 The active drug incorporates into the genome of RNA viruses, leading to an accumulation of mutations known as viral error catastrophe.A193029 Recent studies have shown molnupiravir inhibits replication of human and bat coronaviruses, including SARS-CoV-2, in mice and human airway epithelial cells.A193014 A remdesivir resistant mutant mouse hepatitis virus has also been shown to have increased sensitivity to N4-hydroxycytidine.A193014

Molnupiravir was granted approval by the UK's Medicines and Health products Regulatory Agency (MHRA) on 4 November 2021 to prevent severe outcomes such as hospitalization and death due to COVID-19 in adults.L39050 Molnupiravir was also granted emergency use authorization by the FDA on December 23, 2021; however, it is not yet fully approved.L39588

Struktur Molekul 2D

Berat 329.309
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The half life of the active metabolite, N4-hydroxycytidine, is 3.3 hours.[L39055]
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

After an 800 mg oral dose of molnupiravir every 12 hours, the active compound (N4-hydroxycytidine) reaches a Cmax of 2970 ng/mL, with a Tmax of 1.5 hours, and an AUC0-12h of 8360 h\*ng/mL.L39055

Metabolisme

Molnupiravir is hydrolyzed to N4-hydroxycytidine, which distributes into tissues.A193026 Once inside cells, N4-hydroxycytidine is phosphorylated to the 5'-triphosphate form.A193026

Rute Eliminasi

?3% of an oral molnupiravir dose is eliminated in the urine as the active metabolite N4-hydroxycytidine.L39055

Interaksi Makanan

1 Data
  • 1. Take with or without food. A high fat meal reduces the maximum concentration of the active metabolite by 35% and does not significantly affect the area under the curve.

Interaksi Obat

0 Data
Tidak ada data.

Referensi & Sumber

Artikel (PubMed)
  • PMID: -
    T. P. Sheahan et al.: An orally bioavailable broad-spectrum antiviral inhibits SARS-CoV-2 in human airway epithelial cell cultures and multiple coronaviruses in mice. Sci. Transl. Med..
  • PMID: 31645453
    Toots M, Yoon JJ, Cox RM, Hart M, Sticher ZM, Makhsous N, Plesker R, Barrena AH, Reddy PG, Mitchell DG, Shean RC, Bluemling GR, Kolykhalov AA, Greninger AL, Natchus MG, Painter GR, Plemper RK: Characterization of orally efficacious influenza drug with high resistance barrier in ferrets and human airway epithelia. Sci Transl Med. 2019 Oct 23;11(515). pii: 11/515/eaax5866. doi: 10.1126/scitranslmed.aax5866.
  • PMID: 31910262
    Hampton T: New Flu Antiviral Candidate May Thwart Drug Resistance. JAMA. 2020 Jan 7;323(1):17. doi: 10.1001/jama.2019.20225.

Contoh Produk & Brand

Produk: 2 • International brands: 0
Produk
  • Lagevrio
    Capsule • 200 mg/1 • Oral • US
  • Lagevrio
    Capsule • 200 mg/1 • Oral • US

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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