Oteracil

DB03209

small molecule approved

Deskripsi

Oteracil is an adjunct to antineoplastic therapy, used to reduce the toxic side effects associated with chemotherapy. Approved by the European Medicines Agency (EMA) in March 2011, Oteracil is available in combination with DB09257 and DB09256 within the commercially available product "Teysuno". The main active ingredient in Teysuno is DB09256, a pro-drug of DB00544 (5-FU), which is a cytotoxic anti-metabolite drug that acts on rapidly dividing cancer cells. By mimicking a class of compounds called "pyrimidines" that are essential components of RNA and DNA, 5-FU is able to insert itself into strands of DNA and RNA, thereby halting the replication process necessary for continued cancer growth.

Oteracil's main role within Teysuno is to reduce the activity of 5-FU within normal gastrointestinal mucosa, and therefore reduce's gastrointestinal toxicity L933. It functions by blocking the enzyme orotate phosphoribosyltransferase (OPRT), which is involved in the production of 5-FU.

Struktur Molekul 2D

Berat 157.0843
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Following a single dose of Teysuno, T1/2 values ranged from 6.7 to 11.3 hours for tegafur, from 3.1 to 4.1 hours for gimeracil, and from 1.8 to 9.5 hours for oteracil [L933].
Volume Distribusi Although no intravenous data are available for Teysuno in humans, the volume of distribution could be roughly estimated from the apparent volume of distribution and urinary excretion data as 16 l/m2, 17 l/m2, and 23 l/m2 for tegafur, gimeracil and oteracil, respectively [L933].
Klirens (Clearance) -

Absorpsi

After administration of a single dose of 50 mg Teysuno (expressed as tegafur content), median Tmax for Teysuno components tegafur, gimeracil, and oteracil was 0.5, 1.0, and 2.0 hours, respectively L933.

Metabolisme

Based on the results of in vitro studies, a part of oteracil is non-enzymatically degraded to 5-azauracil (5-AZU) by gastric fluid, and is then converted to cyanuric acid (CA) in the digestive tract. Only a small amount of oteracil is metabolised in the liver because of its low permeability L933.

Rute Eliminasi

Following a single dose of Teysuno, approximately 3.8% to 4.2% of administered tegafur, 65% to 72% of administered gimeracil, and 3.5% to 3.9% of administered oteracil were excreted unchanged in the urine L933.

Interaksi Makanan

1 Data
  • 1. Take separate from meals. Oteracil should be separated from meals by at least one hour before and after eating.

Interaksi Obat

1 Data
Allopurinol The therapeutic efficacy of Oteracil can be decreased when used in combination with Allopurinol.

Referensi & Sumber

Contoh Produk & Brand

Produk: 5 • International brands: 0
Produk
  • Teysuno
    Capsule • - • Oral • EU • Approved
  • Teysuno
    Capsule • - • Oral • EU • Approved
  • Teysuno
    Capsule • - • Oral • EU • Approved
  • Teysuno
    Capsule • - • Oral • EU • Approved
  • Teysuno
    Capsule • - • Oral • EU • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
© 2025 Digital Pharmacy Research - Universitas Esa Unggul