Peringatan Keamanan

Toxicity studies showed no carcinogenic nor genotoxic potential related to asunaprevir. In the case of overdose, clinical studies reported no unexpected adverse events.L2293 Asunaprevir had no effects on fertility in preclinical studies. It has been shown that asunaprevir gets localized in the GI tract and liver and thus, increased hepatic transaminases were observed as well as changes in iron metabolism and decreased serum proteins. These effects are not progressive and asunaprevir was generally well tolerated.L2278

Asunaprevir

DB11586

small molecule approved investigational withdrawn

Deskripsi

Asunaprevir, also named BMS-650032, is a potent hepatitis C virus (HCV) NS3 protease inhibitor. It has been shown to have a very high efficacy in dual-combination regimens with daclatasvir in patients chronically infected with HCV genotype 1b.A32528 It was developed by Bristol-Myers Squibb Canada and approved by Health Canada on April 22, 2016. The commercialization of asunaprevir was cancelled one year later on October 16, 2017.L1113

Struktur Molekul 2D

Berat 748.286
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Clinical pharmacokinetic studies showed a mean terminal half-life of 15-20 hours.[A18434]
Volume Distribusi The registered volume of distribution at steady state is 194 L.[L2293]
Klirens (Clearance) Clinical pharmacokinetic studies showed a mean oral clearance of 302-491 L/h.[A18434]

Absorpsi

In preclinical studies, asunaprevir showed a high liver-to-plasma AUC ratio. It is rapidly absorbed within 30 minutes of administration.L2278 Clinical pharmacokinetic studies showed a Tmax of 2-4 hours.A18434 The pharmacokinetic profile act in a dose-proportional manner and in a dose of 100 mg the steady-state Cmax and AUC was 572 ng/ml and 1887 ng x h/mL. The absolute bioavailability is reported to be 9.3%. The absorption of asunaprevir is increased with food.L2293

Metabolisme

Asunaprevir is metabolized by the liver.A18434 The metabolism is mainly marked by oxidative reactions mediated by the activity of CYP3A.L2293 Asunaprevir seems to weakly induce its own metabolism and from the circulating dose, just about 5% of the administered dose is formed by metabolites.L2278 The metabolites of asunaprevir are formed after mono- and bis-oxidation, N-dealkylation, loss of isoquinoline ring and O-demethylation. All the metabolic reactions form about 15 metabolites and studies have reported that the main metabolic activity is performed by CYP3A4 and CYP3A5 with some minor activity from CYP2A6, CYP2B6, CYP2C9, CYP2C19 and CYP2D6.L2293

Rute Eliminasi

Asunaprevir is primarily eliminated via the feces.A18434 From the administered dose, 84% is excreted by feces mainly as metabolites and less than 1% of the dose is recovered as metabolites in the urine. The proportion of unchanged asunaprevir recovered in feces represents only 7.5% of the dose.L2293

Interaksi Makanan

3 Data
  • 1. Avoid St. John's Wort. This herb induces CYP3A metabolism and may reduce serum levels of asunaprevir. Co-administration of asunaprevir with St. John's Wort is contraindicated.
  • 2. Exercise caution with grapefruit products. Grapefruit inhibits CYP3A metabolism, which may increase the serum concentration of asunaprevir.
  • 3. Take with or without food.

Interaksi Obat

1025 Data
Afatinib The serum concentration of Afatinib can be increased when it is combined with Asunaprevir.
Bosutinib The serum concentration of Bosutinib can be increased when it is combined with Asunaprevir.
Brentuximab vedotin The serum concentration of Brentuximab vedotin can be increased when it is combined with Asunaprevir.
Colchicine The serum concentration of Colchicine can be increased when it is combined with Asunaprevir.
Edoxaban The serum concentration of Edoxaban can be increased when it is combined with Asunaprevir.
Ledipasvir The serum concentration of Ledipasvir can be increased when it is combined with Asunaprevir.
Naloxegol The serum concentration of Naloxegol can be increased when it is combined with Asunaprevir.
Pazopanib The serum concentration of Pazopanib can be increased when it is combined with Asunaprevir.
Prucalopride The serum concentration of Prucalopride can be increased when it is combined with Asunaprevir.
Silodosin The excretion of Silodosin can be decreased when combined with Asunaprevir.
Topotecan The serum concentration of Topotecan can be increased when it is combined with Asunaprevir.
Aripiprazole The metabolism of Aripiprazole can be increased when combined with Asunaprevir.
Aripiprazole lauroxil The metabolism of Aripiprazole lauroxil can be increased when combined with Asunaprevir.
Everolimus The serum concentration of Everolimus can be increased when it is combined with Asunaprevir.
Rifaximin The serum concentration of Rifaximin can be increased when it is combined with Asunaprevir.
Brexpiprazole The metabolism of Brexpiprazole can be decreased when combined with Asunaprevir.
Eliglustat The metabolism of Asunaprevir can be decreased when combined with Eliglustat.
Alprazolam The serum concentration of Alprazolam can be increased when it is combined with Asunaprevir.
Cisapride The serum concentration of Cisapride can be increased when it is combined with Asunaprevir.
Clarithromycin The serum concentration of Clarithromycin can be increased when it is combined with Asunaprevir.
Cyclophosphamide The serum concentration of the active metabolites of Cyclophosphamide can be increased when Cyclophosphamide is used in combination with Asunaprevir.
Atomoxetine The metabolism of Atomoxetine can be decreased when combined with Asunaprevir.
Ifosfamide The metabolism of Ifosfamide can be increased when combined with Asunaprevir.
Perampanel The metabolism of Perampanel can be increased when combined with Asunaprevir.
Warfarin The metabolism of Warfarin can be increased when combined with Asunaprevir.
Acenocoumarol The metabolism of Acenocoumarol can be increased when combined with Asunaprevir.
(R)-warfarin The metabolism of (R)-warfarin can be increased when combined with Asunaprevir.
R,S-Warfarin alcohol The metabolism of R,S-Warfarin alcohol can be increased when combined with Asunaprevir.
S,R-Warfarin alcohol The metabolism of S,R-Warfarin alcohol can be increased when combined with Asunaprevir.
(S)-Warfarin The metabolism of (S)-Warfarin can be increased when combined with Asunaprevir.
Mirabegron The serum concentration of Asunaprevir can be increased when it is combined with Mirabegron.
Eluxadoline The serum concentration of Eluxadoline can be increased when it is combined with Asunaprevir.
Vincristine The excretion of Vincristine can be decreased when combined with Asunaprevir.
Doxorubicin The serum concentration of Doxorubicin can be decreased when it is combined with Asunaprevir.
Garlic Garlic can cause a decrease in the absorption of Asunaprevir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Erlotinib The serum concentration of Erlotinib can be decreased when it is combined with Asunaprevir.
Tranylcypromine The metabolism of Asunaprevir can be decreased when combined with Tranylcypromine.
Cyclosporine The metabolism of Asunaprevir can be decreased when combined with Cyclosporine.
Sildenafil The metabolism of Sildenafil can be decreased when combined with Asunaprevir.
Eletriptan The metabolism of Eletriptan can be decreased when combined with Asunaprevir.
Theophylline The metabolism of Theophylline can be decreased when combined with Asunaprevir.
Zolpidem The metabolism of Zolpidem can be decreased when combined with Asunaprevir.
Imipramine The metabolism of Asunaprevir can be decreased when combined with Imipramine.
Buspirone The metabolism of Buspirone can be decreased when combined with Asunaprevir.
Darifenacin The metabolism of Asunaprevir can be decreased when combined with Darifenacin.
Nortriptyline The metabolism of Nortriptyline can be decreased when combined with Asunaprevir.
Clonidine The metabolism of Clonidine can be decreased when combined with Asunaprevir.
Astemizole The metabolism of Astemizole can be decreased when combined with Asunaprevir.
Simvastatin The metabolism of Simvastatin can be decreased when combined with Asunaprevir.
Trimipramine The metabolism of Trimipramine can be decreased when combined with Asunaprevir.
Pimozide The metabolism of Pimozide can be decreased when combined with Asunaprevir.
Doxepin The metabolism of Doxepin can be decreased when combined with Asunaprevir.
Quetiapine The metabolism of Quetiapine can be decreased when combined with Asunaprevir.
Clomipramine The metabolism of Clomipramine can be decreased when combined with Asunaprevir.
Ibrutinib The metabolism of Ibrutinib can be decreased when combined with Asunaprevir.
Ticlopidine The metabolism of Ticlopidine can be decreased when combined with Asunaprevir.
Sertraline The metabolism of Sertraline can be decreased when combined with Asunaprevir.
Desipramine The metabolism of Asunaprevir can be decreased when combined with Desipramine.
Dosulepin The metabolism of Asunaprevir can be decreased when combined with Dosulepin.
Lidocaine The metabolism of Lidocaine can be decreased when combined with Asunaprevir.
Acetaminophen The metabolism of Acetaminophen can be decreased when combined with Asunaprevir.
Gefitinib The metabolism of Gefitinib can be decreased when combined with Asunaprevir.
Methadone The metabolism of Methadone can be decreased when combined with Asunaprevir.
Quinine The metabolism of Asunaprevir can be decreased when combined with Quinine.
Duloxetine The metabolism of Asunaprevir can be decreased when combined with Duloxetine.
Chlorpromazine The metabolism of Asunaprevir can be decreased when combined with Chlorpromazine.
Doxazosin The metabolism of Doxazosin can be decreased when combined with Asunaprevir.
Chloroquine The metabolism of Asunaprevir can be decreased when combined with Chloroquine.
Tamoxifen The metabolism of Tamoxifen can be decreased when combined with Asunaprevir.
Buprenorphine The metabolism of Buprenorphine can be decreased when combined with Asunaprevir.
Azelastine The metabolism of Azelastine can be decreased when combined with Asunaprevir.
Selegiline The metabolism of Selegiline can be decreased when combined with Asunaprevir.
Promethazine The metabolism of Promethazine can be decreased when combined with Asunaprevir.
Primaquine The metabolism of Asunaprevir can be decreased when combined with Primaquine.
Carvedilol The metabolism of Carvedilol can be decreased when combined with Asunaprevir.
Bepridil The metabolism of Bepridil can be decreased when combined with Asunaprevir.
Paliperidone The metabolism of Paliperidone can be decreased when combined with Asunaprevir.
Yohimbine The metabolism of Yohimbine can be decreased when combined with Asunaprevir.
Tesmilifene The metabolism of Tesmilifene can be decreased when combined with Asunaprevir.
Benzyl alcohol The metabolism of Benzyl alcohol can be decreased when combined with Asunaprevir.
Ponatinib The metabolism of Ponatinib can be decreased when combined with Asunaprevir.
Rolapitant The metabolism of Asunaprevir can be decreased when combined with Rolapitant.
Letermovir The metabolism of Asunaprevir can be decreased when combined with Letermovir.
Rucaparib The metabolism of Rucaparib can be decreased when combined with Asunaprevir.
Enasidenib The metabolism of Enasidenib can be decreased when combined with Asunaprevir.
Fluvoxamine The metabolism of Asunaprevir can be decreased when combined with Fluvoxamine.
Imatinib The serum concentration of Asunaprevir can be increased when it is combined with Imatinib.
Abiraterone The metabolism of Asunaprevir can be decreased when combined with Abiraterone.
Nicardipine The metabolism of Asunaprevir can be decreased when combined with Nicardipine.
Sulfaphenazole The metabolism of Asunaprevir can be decreased when combined with Sulfaphenazole.
Bortezomib The metabolism of Bortezomib can be decreased when combined with Asunaprevir.
Cimetidine The metabolism of Asunaprevir can be decreased when combined with Cimetidine.
Manidipine The metabolism of Asunaprevir can be decreased when combined with Manidipine.
Triclabendazole The metabolism of Triclabendazole can be decreased when combined with Asunaprevir.
Nevirapine The metabolism of Nevirapine can be decreased when combined with Asunaprevir.
Diltiazem The metabolism of Diltiazem can be decreased when combined with Asunaprevir.
Clobazam The serum concentration of Asunaprevir can be increased when it is combined with Clobazam.
Risperidone The metabolism of Risperidone can be decreased when combined with Asunaprevir.
Fusidic acid The metabolism of Asunaprevir can be decreased when combined with Fusidic acid.
Netupitant The metabolism of Netupitant can be decreased when combined with Asunaprevir.

Target Protein

Gag-Pol polyprotein gag-pol
Genome polyprotein

Referensi & Sumber

Artikel (PubMed)
  • PMID: 22256805
    Lok AS, Gardiner DF, Lawitz E, Martorell C, Everson GT, Ghalib R, Reindollar R, Rustgi V, McPhee F, Wind-Rotolo M, Persson A, Zhu K, Dimitrova DI, Eley T, Guo T, Grasela DM, Pasquinelli C: Preliminary study of two antiviral agents for hepatitis C genotype 1. N Engl J Med. 2012 Jan 19;366(3):216-24. doi: 10.1056/NEJMoa1104430.
  • PMID: 22508297
    McPhee F, Friborg J, Levine S, Chen C, Falk P, Yu F, Hernandez D, Lee MS, Chaniewski S, Sheaffer AK, Pasquinelli C: Resistance analysis of the hepatitis C virus NS3 protease inhibitor asunaprevir. Antimicrob Agents Chemother. 2012 Jul;56(7):3670-81. doi: 10.1128/AAC.00308-12. Epub 2012 Apr 16.
  • PMID: 25061308
    Gentile I, Buonomo AR, Zappulo E, Minei G, Morisco F, Borrelli F, Coppola N, Borgia G: Asunaprevir, a protease inhibitor for the treatment of hepatitis C infection. Ther Clin Risk Manag. 2014 Jun 26;10:493-504. doi: 10.2147/TCRM.S66731. eCollection 2014.

Contoh Produk & Brand

Produk: 2 • International brands: 0
Produk
  • Asunaprevir
    Capsule • 100 mg/1 • Not applicable • US
  • Sunvepra
    Capsule • 100 mg • Oral • Canada • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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