Peringatan Keamanan

There are no reports of overdose with bulevirtide. In the case of an overdose, monitor the patient and provide supportive treatment.^L30290

Bulevirtide

DB15248

biotech approved investigational

Deskripsi

Hepatitis D is considered the most severe type of viral hepatitis and leads to the rapid development of cirrhosis, severe decompensation of liver function, and an increased risk of mortality.A226340,L30235 Until recently, there have been extremely limited treatments available for Hepatitis D infection.^A226305

Bulevirtide, also known as Hepcludex, is a first-in-class entry inhibitor for the treatment of chronic Hepatitis D infection developed by MYR Pharmaceuticals, now part of Gilead. It was first approved for use in the EU on May 28, 2020; bulevirtide has been granted PRIME scheme eligibility and Orphan Drug Designation by the European Medicines Agency.^L30215 In the USA, bulevirtide has been granted Orphan Drug Designation and Breakthrough Therapy Designation.L30260,L30275 Due to potentially beneficial synergistic effects in treating chronic Hepatitis D, bulevirtide is also under investigation in clinical trial NCT03852433 (Phase 2b Study of Bulevirtide With Peginterferon Alfa-2a) in Patients With CHD. Completion of this clinical trial is anticipated in early 2023.^L30240

Struktur Molekul 2D

Struktur tidak tersedia

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) The half-life of bulevirtide ranges between 4 and 7 hours in healthy adults.[L30290]

Volume Distribusi The volume of distribution of bulevirtide is estimated to be lower than total body water.[L30290] In animals, bulevirtide distributes into the liver, gastrointestinal tract, kidney, and bladder.[L30215]

Klirens (Clearance) The clearance after of bulevirtide after subcutaneous administration (CL/F) in healthy volunteers ranged from 7.98 L/h (±2.02) to 62 L/h (±16.7), depending on the dose administered.[L30215] The clearance of bulevirtide decreases as the dose increases.[L30290]

Absorpsi

Human pharmacokinetic data for bulevirtide is limited in the literature. In rats, bulevirtide administered by subcutaneous injection is rapidly absorbed with a Cmax of 4 to 6 hours.^L30215 The estimated bioavailability is 85% in humans, and steady-state concentrations are expected to occur within weeks of initiating treatment.A226375,L30290 The AUC for bulevirtide after a 2mg subcutaneous dose was found to be approximately 46 ng/ml.h with a Tmax of 0.5 hours.^L30215

Metabolisme

To date, metabolism studies have not been conducted on bulevirtide. It is expected to be catabolized by peptidases to smaller peptides and amino acids, with no active metabolites.L30215,L30290

Rute Eliminasi

Elimination through target (NTCP) binding is expected to be the main route of elimination for bulevirtide. In healthy volunteers, bulevirtide was not found to be excreted in the urine.^L30290

Interaksi Obat

14 Data

Rubella virus vaccine	The therapeutic efficacy of Rubella virus vaccine can be decreased when used in combination with Bulevirtide.
Varicella zoster vaccine (live/attenuated)	The therapeutic efficacy of Varicella zoster vaccine (live/attenuated) can be decreased when used in combination with Bulevirtide.
Bacillus calmette-guerin substrain tice live antigen	The therapeutic efficacy of Bacillus calmette-guerin substrain tice live antigen can be decreased when used in combination with Bulevirtide.
Bacillus calmette-guerin substrain connaught live antigen	The therapeutic efficacy of Bacillus calmette-guerin substrain connaught live antigen can be decreased when used in combination with Bulevirtide.
Yellow fever vaccine	The therapeutic efficacy of Yellow fever vaccine can be decreased when used in combination with Bulevirtide.
Anthrax vaccine	The therapeutic efficacy of Anthrax vaccine can be decreased when used in combination with Bulevirtide.
Typhoid Vaccine Live	The therapeutic efficacy of Typhoid Vaccine Live can be decreased when used in combination with Bulevirtide.
BCG vaccine	The therapeutic efficacy of BCG vaccine can be decreased when used in combination with Bulevirtide.
Human adenovirus e serotype 4 strain cl-68578 antigen	The therapeutic efficacy of Human adenovirus e serotype 4 strain cl-68578 antigen can be decreased when used in combination with Bulevirtide.
Vibrio cholerae CVD 103-HgR strain live antigen	The therapeutic efficacy of Vibrio cholerae CVD 103-HgR strain live antigen can be decreased when used in combination with Bulevirtide.
Adenovirus type 7 vaccine live	The therapeutic efficacy of Adenovirus type 7 vaccine live can be decreased when used in combination with Bulevirtide.
Bacillus calmette-guerin substrain russian BCG-I live antigen	The therapeutic efficacy of Bacillus calmette-guerin substrain russian BCG-I live antigen can be decreased when used in combination with Bulevirtide.
Chikungunya vaccine (live, attenuated)	The therapeutic efficacy of Chikungunya vaccine (live, attenuated) can be decreased when used in combination with Bulevirtide.
Smallpox (Vaccinia) Vaccine, Live	The therapeutic efficacy of Smallpox (Vaccinia) Vaccine, Live can be decreased when used in combination with Bulevirtide.

Target Protein

Hepatic sodium/bile acid cotransporter SLC10A1

Referensi & Sumber

Artikel (PubMed)

PMID: 22161394
Abbas Z, Khan MA, Salih M, Jafri W: Interferon alpha for chronic hepatitis D. Cochrane Database Syst Rev. 2011 Dec 7;(12):CD006002. doi: 10.1002/14651858.CD006002.pub2.
PMID: 32926353
Kang C, Syed YY: Bulevirtide: First Approval. Drugs. 2020 Oct;80(15):1601-1605. doi: 10.1007/s40265-020-01400-1.
PMID: 26134842
Rizzetto M: Hepatitis D Virus: Introduction and Epidemiology. Cold Spring Harb Perspect Med. 2015 Jul 1;5(7):a021576. doi: 10.1101/cshperspect.a021576.
PMID: 31840863
Smolders EJ, Burger DM, Feld JJ, Kiser JJ: Review article: clinical pharmacology of current and investigational hepatitis B virus therapies. Aliment Pharmacol Ther. 2020 Jan;51(2):231-243. doi: 10.1111/apt.15581. Epub 2019 Dec 16.

Link

Contoh Produk & Brand

Produk: 1 • International brands: 2

Produk

Hepcludex

Injection, powder, for solution • 2 mg • Subcutaneous • EU • Approved

International Brands

Hepcludex
Myrcludex B

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.