Voxilaprevir

DB12026

small molecule approved investigational

Deskripsi

Voxilaprevir is a Direct-Acting Antiviral (DAA) medication used as part of combination therapy to treat chronic Hepatitis C, an infectious liver disease caused by infection with Hepatitis C Virus (HCV). HCV is a single-stranded RNA virus that is categorized into nine distinct genotypes, with genotype 1 being the most common in the United States, and affecting 72% of all chronic HCV patients L852.

Voxilaprevir exerts its antiviral action by reversibly binding and inhibiting the NS3/4A serine protease of Hepatitis C Virus (HCV) FDA Label. Following viral replication of HCV genetic material and translation into a single polypeptide, Nonstructural Protein 3 (NS3) and its activating cofactor Nonstructural Protein 4A (NS4A) are responsible for cleaving genetic material into the following structural and nonstructural proteins required for assembly into mature virus: NS3, NS4A, NS4B, NS5A, and NS5B A19643. By inhibiting viral protease NS3/4A, voxilaprevir therefore prevents viral replication and function. Treatment options for chronic Hepatitis C have advanced significantly since 2011, with the development of Direct Acting Antivirals (DAAs) such as voxilaprevir.

Voxilaprevir has been available since July 2017 in a fixed dose combination product with sofosbuvir and velpatasvir as the commercially available product Vosevi. Vosevi is approved for the treatment of adult patients with chronic HCV infection with genotype 1, 2, 3, 4, 5, or 6 infection FDA Label. Notably, Vosevi is approved for use in patients with genotypes 1-6 who have been previously treated with an NS5A inhibitor, or patients with genotypes 1a or 3 infection and have previously been treated with an HCV regimen containing sofosbuvir without an NS5A inhibitor L935. Prior to Vosevi, there were no approved retreatment options for patients who have previously received, and failed, a regimen containing an NS5A inhibitor for treatment of chronic HCV infection.

Struktur Molekul 2D

Berat 868.94
Wujud -

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) 33 hr [FDA Label]
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

When provided as the fixed dose combination product Vosevi with DB08934 and DB11613, voxilaprevir reaches a maximum concentration (Cmax) of 192 ng/mL at a maximum time (Tmax) of 4 hours post-dose FDA Label.

Metabolisme

Voxilaprevir is primarily metabolized by Cytochrome P450 3A4 (CYP3A4) and to a lesser extent by CYP2C8 and CYP1A2FDA Label.

Rute Eliminasi

Voxilaprevir is primarily eliminated via biliary excretion FDA Label.

Interaksi Makanan

3 Data
  • 1. Avoid St. John's Wort. This herb induces CYP3A metabolism and may reduce serum levels of voxilaprevir.
  • 2. Take separate from antacids. Take Vosevi (sofosbuvir, velpatasvir, and voxilaprevir) at least 4 hours before or after antacids. Antacids have been shown to reduce the serum levels of velpatasvir and may not impact voxilaprevir.
  • 3. Take with food.

Interaksi Obat

783 Data
Afatinib The serum concentration of Afatinib can be increased when it is combined with Voxilaprevir.
Bosutinib The serum concentration of Bosutinib can be increased when it is combined with Voxilaprevir.
Brentuximab vedotin The serum concentration of Brentuximab vedotin can be increased when it is combined with Voxilaprevir.
Colchicine The serum concentration of Colchicine can be increased when it is combined with Voxilaprevir.
Edoxaban The serum concentration of Edoxaban can be increased when it is combined with Voxilaprevir.
Ledipasvir The serum concentration of Ledipasvir can be increased when it is combined with Voxilaprevir.
Naloxegol The serum concentration of Naloxegol can be increased when it is combined with Voxilaprevir.
Pazopanib The serum concentration of Pazopanib can be increased when it is combined with Voxilaprevir.
Prucalopride The serum concentration of Prucalopride can be increased when it is combined with Voxilaprevir.
Ranolazine The serum concentration of Ranolazine can be increased when it is combined with Voxilaprevir.
Silodosin The excretion of Silodosin can be decreased when combined with Voxilaprevir.
Topotecan The serum concentration of Topotecan can be increased when it is combined with Voxilaprevir.
Deferasirox The serum concentration of Voxilaprevir can be increased when it is combined with Deferasirox.
Peginterferon alfa-2b The serum concentration of Voxilaprevir can be increased when it is combined with Peginterferon alfa-2b.
Leflunomide The serum concentration of Voxilaprevir can be decreased when it is combined with Leflunomide.
Teriflunomide The serum concentration of Voxilaprevir can be decreased when it is combined with Teriflunomide.
Everolimus The serum concentration of Everolimus can be increased when it is combined with Voxilaprevir.
Rifaximin The serum concentration of Rifaximin can be increased when it is combined with Voxilaprevir.
Mifepristone The serum concentration of Voxilaprevir can be increased when it is combined with Mifepristone.
Abiraterone The serum concentration of Voxilaprevir can be increased when it is combined with Abiraterone.
Eluxadoline The serum concentration of Eluxadoline can be increased when it is combined with Voxilaprevir.
Vincristine The excretion of Vincristine can be decreased when combined with Voxilaprevir.
Cyproterone acetate The metabolism of Voxilaprevir can be increased when combined with Cyproterone acetate.
Doxorubicin The serum concentration of Doxorubicin can be increased when it is combined with Voxilaprevir.
Lumacaftor The serum concentration of Voxilaprevir can be decreased when it is combined with Lumacaftor.
Primidone The metabolism of Voxilaprevir can be increased when combined with Primidone.
Rifampin The metabolism of Voxilaprevir can be increased when combined with Rifampicin.
Carbamazepine The metabolism of Voxilaprevir can be increased when combined with Carbamazepine.
Albendazole The metabolism of Voxilaprevir can be increased when combined with Albendazole.
Caffeine The metabolism of Voxilaprevir can be decreased when combined with Caffeine.
Moxifloxacin The metabolism of Voxilaprevir can be decreased when combined with Moxifloxacin.
Mexiletine The metabolism of Voxilaprevir can be decreased when combined with Mexiletine.
Alosetron The metabolism of Voxilaprevir can be decreased when combined with Alosetron.
Gatifloxacin The metabolism of Voxilaprevir can be decreased when combined with Gatifloxacin.
Simeprevir The metabolism of Voxilaprevir can be decreased when combined with Simeprevir.
Lobeglitazone The metabolism of Voxilaprevir can be decreased when combined with Lobeglitazone.
Pazufloxacin The metabolism of Voxilaprevir can be decreased when combined with Pazufloxacin.
Lidocaine The metabolism of Voxilaprevir can be decreased when combined with Lidocaine.
Osilodrostat The metabolism of Voxilaprevir can be decreased when combined with Osilodrostat.
Secobarbital The metabolism of Voxilaprevir can be increased when combined with Secobarbital.
Phenobarbital The metabolism of Voxilaprevir can be increased when combined with Phenobarbital.
Bexarotene The metabolism of Voxilaprevir can be decreased when combined with Bexarotene.
Diltiazem The metabolism of Voxilaprevir can be decreased when combined with Diltiazem.
Medroxyprogesterone acetate The metabolism of Voxilaprevir can be decreased when combined with Medroxyprogesterone acetate.
Nicardipine The metabolism of Voxilaprevir can be decreased when combined with Nicardipine.
Irbesartan The metabolism of Voxilaprevir can be decreased when combined with Irbesartan.
Oxybutynin The metabolism of Voxilaprevir can be decreased when combined with Oxybutynin.
Fluvastatin The metabolism of Voxilaprevir can be decreased when combined with Fluvastatin.
Pioglitazone The metabolism of Voxilaprevir can be decreased when combined with Pioglitazone.
Levothyroxine The metabolism of Voxilaprevir can be decreased when combined with Levothyroxine.
Loratadine The metabolism of Voxilaprevir can be decreased when combined with Loratadine.
Trimethoprim The metabolism of Voxilaprevir can be decreased when combined with Trimethoprim.
Fluticasone propionate The metabolism of Voxilaprevir can be decreased when combined with Fluticasone propionate.
Clopidogrel The metabolism of Voxilaprevir can be decreased when combined with Clopidogrel.
Candesartan cilexetil The metabolism of Voxilaprevir can be decreased when combined with Candesartan cilexetil.
Salmeterol The metabolism of Voxilaprevir can be decreased when combined with Salmeterol.
Gemfibrozil The metabolism of Voxilaprevir can be decreased when combined with Gemfibrozil.
Fluticasone The metabolism of Voxilaprevir can be decreased when combined with Fluticasone.
Mometasone furoate The metabolism of Voxilaprevir can be decreased when combined with Mometasone furoate.
Felodipine The metabolism of Voxilaprevir can be decreased when combined with Felodipine.
Osimertinib The serum concentration of Voxilaprevir can be decreased when it is combined with Osimertinib.
Betrixaban The serum concentration of Betrixaban can be increased when it is combined with Voxilaprevir.
Vemurafenib The serum concentration of Voxilaprevir can be increased when it is combined with Vemurafenib.
Apalutamide The serum concentration of Voxilaprevir can be decreased when it is combined with Apalutamide.
Pitolisant The serum concentration of Voxilaprevir can be decreased when it is combined with Pitolisant.
Isavuconazole The serum concentration of Voxilaprevir can be increased when it is combined with Isavuconazole.
Isavuconazonium The serum concentration of Voxilaprevir can be increased when it is combined with Isavuconazonium.
Imatinib Imatinib may decrease the excretion rate of Voxilaprevir which could result in a higher serum level.
Sulfasalazine Sulfasalazine may decrease the excretion rate of Voxilaprevir which could result in a higher serum level.
Novobiocin Novobiocin may decrease the excretion rate of Voxilaprevir which could result in a higher serum level.
Hesperetin Hesperetin may decrease the excretion rate of Voxilaprevir which could result in a higher serum level.
Rabeprazole Rabeprazole may decrease the excretion rate of Voxilaprevir which could result in a higher serum level.
Genistein The metabolism of Voxilaprevir can be decreased when combined with Genistein.
Topiroxostat The metabolism of Voxilaprevir can be decreased when combined with Topiroxostat.
Daidzin Daidzin may decrease the excretion rate of Voxilaprevir which could result in a higher serum level.
Fusidic acid The metabolism of Voxilaprevir can be decreased when combined with Fusidic acid.
Naringenin Naringenin may decrease the excretion rate of Voxilaprevir which could result in a higher serum level.
Vandetanib Vandetanib may decrease the excretion rate of Voxilaprevir which could result in a higher serum level.
Eltrombopag The metabolism of Voxilaprevir can be decreased when combined with Eltrombopag.
Safinamide Safinamide may decrease the excretion rate of Voxilaprevir which could result in a higher serum level.
Cannabidiol Cannabidiol may decrease the excretion rate of Voxilaprevir which could result in a higher serum level.
Palbociclib Palbociclib may decrease the excretion rate of Voxilaprevir which could result in a higher serum level.
Glasdegib Glasdegib may decrease the excretion rate of Voxilaprevir which could result in a higher serum level.
Fostamatinib Fostamatinib may decrease the excretion rate of Voxilaprevir which could result in a higher serum level.
Folic acid Voxilaprevir may decrease the excretion rate of Folic acid which could result in a higher serum level.
Allopurinol Voxilaprevir may decrease the excretion rate of Allopurinol which could result in a higher serum level.
Celecoxib Voxilaprevir may decrease the excretion rate of Celecoxib which could result in a higher serum level.
Oxaliplatin Voxilaprevir may decrease the excretion rate of Oxaliplatin which could result in a higher serum level.
Methotrexate Voxilaprevir may decrease the excretion rate of Methotrexate which could result in a higher serum level.
Clofarabine Voxilaprevir may decrease the excretion rate of Clofarabine which could result in a higher serum level.
Tamoxifen The metabolism of Voxilaprevir can be decreased when combined with Tamoxifen.
Nitrofurantoin Voxilaprevir may decrease the excretion rate of Nitrofurantoin which could result in a higher serum level.
Riluzole Voxilaprevir may decrease the excretion rate of Riluzole which could result in a higher serum level.
Rosuvastatin Voxilaprevir may decrease the excretion rate of Rosuvastatin which could result in a higher serum level.
Alvocidib Voxilaprevir may decrease the excretion rate of Alvocidib which could result in a higher serum level.
Riociguat Voxilaprevir may decrease the excretion rate of Riociguat which could result in a higher serum level.
Lenvatinib Voxilaprevir may decrease the excretion rate of Lenvatinib which could result in a higher serum level.
Fimasartan Voxilaprevir may decrease the excretion rate of Fimasartan which could result in a higher serum level.
Delafloxacin Voxilaprevir may decrease the excretion rate of Delafloxacin which could result in a higher serum level.
Gilteritinib Gilteritinib may decrease the excretion rate of Voxilaprevir which could result in a higher serum level.

Target Protein

Genome polyprotein NS3/4A
Genome polyprotein

Referensi & Sumber

Artikel (PubMed)
  • PMID: 28564569
    Bourliere M, Gordon SC, Flamm SL, Cooper CL, Ramji A, Tong M, Ravendhran N, Vierling JM, Tran TT, Pianko S, Bansal MB, de Ledinghen V, Hyland RH, Stamm LM, Dvory-Sobol H, Svarovskaia E, Zhang J, Huang KC, Subramanian GM, Brainard DM, McHutchison JG, Verna EC, Buggisch P, Landis CS, Younes ZH, Curry MP, Strasser SI, Schiff ER, Reddy KR, Manns MP, Kowdley KV, Zeuzem S: Sofosbuvir, Velpatasvir, and Voxilaprevir for Previously Treated HCV Infection. N Engl J Med. 2017 Jun 1;376(22):2134-2146. doi: 10.1056/NEJMoa1613512.
  • PMID: 23463199
    Moradpour D, Penin F: Hepatitis C virus proteins: from structure to function. Curr Top Microbiol Immunol. 2013;369:113-42. doi: 10.1007/978-3-642-27340-7_5.

Contoh Produk & Brand

Produk: 4 • International brands: 0
Produk
  • Vosevi
    Tablet, film coated • - • Oral • EU • Approved
  • Vosevi
    Tablet • - • Oral • Canada • Approved
  • Vosevi
    Tablet, film coated • - • Oral • US • Approved
  • Vosevi
    Tablet, film coated • - • Oral • EU • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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