Peringatan Keamanan

Data regarding overdoses of odevixibat are not readily available, due to the low systemic absorption of the drug.^L34793 If patients experience an overdose, initiate treatment with symptomatic and supportive measures.

Odevixibat

DB16261

small molecule approved investigational

Deskripsi

Odevixibat, or A4250, is an ileal sodium/bile acid cotransporter inhibitor indicated for the treatment of pruritus in patients older than 3 months, with progressive familial intrahepatic cholestasis (PFIC).A236808,L34793 Odevixibat is the first approved non-surgical treatment option for PFIC.^L34803 Previous therapies for PFIC included a bile acid sequestrant such as ursodeoxycholic acid.^A236808

Odevixibat was granted FDA and Health Canada approval on 20 July 2021 and 13 November 2023 respectively.L34793,L49535

Struktur Molekul 2D

Berat 740.93

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) A 7.2 mg oral dose of odevixibat has a mean half life of 2.36 hours in adults.[L34793]

Volume Distribusi The majority of adult and pediatric patients, given a therapeutic dose, do not have detectable plasma concentrations of odevixibat.[A236808,L34793] Therefore, a volume of distribution has not been calculated.[A236808,L34793]

Klirens (Clearance) The majority of adult and pediatric patients, given a therapeutic dose, do not have detectable plasma concentrations of odevixibat.[A236808,L34793] Therefore, the clearance has not been calculated.[A236808,L34793]

Absorpsi

A 7.2 mg single oral dose of odevixibat in adults reaches a C_max of 0.47 ng/mL, with an AUC_0-24h of 2.19 h\*ng/mL.^L34793 The majority of adult and pediatric patients, given a therapeutic dose, do not have detectable plasma concentrations of odevixibat.A236808,L34793

Metabolisme

Odevixibat is largely unmetabolized, however a small amount is metabolized in vitro by mono-hydroxylation.^L34793 The exact structure of the metabolite has not been characterized as a primary endpoint of the clinical trial was to characterize the structure of metabolites accounting for >10% of the dose in plasma, urine, or feces.^L34798 No metabolites have been identified at such a high concentration.^L34793

Rute Eliminasi

Odevixibat is 82.9% recovered in the feces and <0.002% recovered in the urine.^L34793 The dose recovered in the feces is 97% unchanged parent compound.^L34793

Interaksi Makanan

1 Data

1. Take with a high fat meal. The effect of food is not clinically significant.

Interaksi Obat

4 Data

Colestipol	The therapeutic efficacy of Odevixibat can be decreased when used in combination with Colestipol.
Sevelamer	The therapeutic efficacy of Odevixibat can be decreased when used in combination with Sevelamer.
Colesevelam	The therapeutic efficacy of Odevixibat can be decreased when used in combination with Colesevelam.
Cholestyramine	The therapeutic efficacy of Odevixibat can be decreased when used in combination with Cholestyramine.

Target Protein

Ileal sodium/bile acid cotransporter SLC10A2

Referensi & Sumber

Artikel (PubMed)

PMID: 26527417
Graffner H, Gillberg PG, Rikner L, Marschall HU: The ileal bile acid transporter inhibitor A4250 decreases serum bile acids by interrupting the enterohepatic circulation. Aliment Pharmacol Ther. 2016 Jan;43(2):303-10. doi: 10.1111/apt.13457. Epub 2015 Nov 2.
PMID: 19133130
Davit-Spraul A, Gonzales E, Baussan C, Jacquemin E: Progressive familial intrahepatic cholestasis. Orphanet J Rare Dis. 2009 Jan 8;4:1. doi: 10.1186/1750-1172-4-1.
PMID: 32601135
Slavetinsky C, Sturm E: Odevixibat and partial external biliary diversion showed equal improvement of cholestasis in a patient with progressive familial intrahepatic cholestasis. BMJ Case Rep. 2020 Jun 29;13(6). pii: 13/6/e234185. doi: 10.1136/bcr-2019-234185.
PMID: 30186169
Al-Dury S, Marschall HU: Ileal Bile Acid Transporter Inhibition for the Treatment of Chronic Constipation, Cholestatic Pruritus, and NASH. Front Pharmacol. 2018 Aug 21;9:931. doi: 10.3389/fphar.2018.00931. eCollection 2018.

Link

Contoh Produk & Brand

Produk: 16 • International brands: 1

Produk

Bylvay

Capsule, coated pellets • 200 ug/1 • Oral • US • Approved
Bylvay

Capsule, coated pellets • 400 ug/1 • Oral • US • Approved
Bylvay

Capsule, coated pellets • 600 ug/1 • Oral • US • Approved
Bylvay

Capsule, coated pellets • 1200 ug/1 • Oral • US • Approved
Bylvay

Capsule • 200 µg • Oral • EU • Approved
Bylvay

Capsule • 400 µg • Oral • EU • Approved
Bylvay

Capsule • 600 µg • Oral • EU • Approved
Bylvay

Capsule • 1200 µg • Oral • EU • Approved

Menampilkan 8 dari 16 produk.

International Brands

Bylvay — Albireo Pharma, Inc.

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.