Brasofensine

DB04857

small molecule investigational

Deskripsi

Brasofensine is an orally administered dopamine reuptake inhibitor being developed for the treatment of Parkinson's Disease. Phase I/II trials for brasofensine have been completed in the U.K. In November 2001, NeuroSearch confirmed that the drug's development was discontinued in favor of NS 2230.

Struktur Molekul 2D

Berat 327.25

Wujud solid

Peta Jejaring Molekuler

Obat Target Gen Interaksi Enzim Transporter Carrier

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

1. Pendahuluan & Konsep

Fitur visualisasi ini dikembangkan menggunakan pendekatan Graph Theory untuk memetakan hubungan polifarmasi dan molekuler. Entitas (Obat, Target, Gen) direpresentasikan sebagai Simpul (Nodes), sedangkan hubungan biologisnya sebagai Sisi (Edges).

2. Sumber Data (Validasi)

Data Obat: Diekstraksi dari elemen drugbank-id dan name pada skema XML DrugBank.
Target Protein: Diambil dari elemen targets/target yang memuat polipeptida sasaran.
Genetik: Disinkronisasi dari sub-elemen gene-name dan varian snp-effects.
Genetik: Jumlah titik node dibatasi pada maksimal 10 (Slice=10) interaksi untuk menghindari tumpukan data.

3. Algoritma Visualisasi

Tata letak grafik menggunakan algoritma Force-Directed Graph (Barnes-Hut). Model fisika ini menerapkan gaya tolak-menolak antar simpul (Gravitasi: -3000) agar tidak tumpang tindih, serta gaya pegas (Spring: 0.04) pada garis penghubung untuk fleksibilitas interaksi.

4. Legenda Visual

Obat Utama (Pusat Analisis)

Target Protein (Mekanisme)

Gen (Faktor Genetik)

Metode ini mendukung analisis Precision Medicine dan evaluasi risiko Drug-Drug Interaction (DDI).

Profil Farmakokinetik

Waktu Paruh (Half-Life) Plasma terminal elimination half-lives were ~2 hr in rats, ~4 hr in monkeys, but ~24 hr in humans.

Volume Distribusi -

Klirens (Clearance) -

Absorpsi

Brasofensine is rapidly absorbed after oral administration in rats and monkeys, with peak plasma concentrations occurring 0.5-1 hr, but 3-8 hr for brasofensine in humans.

Metabolisme

Brasofensine undergoes extensive first-pass metabolism following oral administration in humans, monkeys, and rats. It primarily underwent O- and N-demethylation and isomerization. Some of the desmethyl metabolites were further converted to glucuronides. These primary metabolites and glucuronides of demethyl brasofensine (M1 and M2) were major circulating metabolites in humans, and were also observed in rat and monkey plasma.

Rute Eliminasi

Data eliminasi belum tersedia.

Interaksi Obat

0 Data

Tidak ada data.

Target Protein

Sodium-dependent serotonin transporter SLC6A4

D(2) dopamine receptor DRD2

Referensi & Sumber

Artikel (PubMed)

PMID: 17908924
Zhu M, Whigan DB, Chang SY, Dockens RC: Disposition and metabolism of 14Cbrasofensine in rats, monkeys, and humans. Drug Metab Dispos. 2008 Jan;36(1):24-35. Epub 2007 Oct 1.
PMID: 15298067
Johnston TH, Brotchie JM: Drugs in development for Parkinson's disease. Curr Opin Investig Drugs. 2004 Jul;5(7):720-6.
PMID: 11847938
Frackiewicz EJ, Jhee SS, Shiovitz TM, Webster J, Topham C, Dockens RC, Whigan D, Salazar DE, Cutler NR: Brasofensine treatment for Parkinson's disease in combination with levodopa/carbidopa. Ann Pharmacother. 2002 Feb;36(2):225-30.

Contoh Produk & Brand

Produk: 0 • International brands: 0

Belum ada data produk/brand untuk obat ini pada database. Jalankan import DrugBank untuk mengisi field produk/brand.

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.