Peringatan Keamanan

Overdose with vonoprazan has not been reported. No serious adverse reactions were observed during clinical studies in subjects given a single dose of 120 mg of vonoprazan. Vonoprazan is not removed from the circulation by hemodialysis. In case of overdose, the FDA label for Voquezna Triple Pak and Voquezna Dual Pak recommends symptomatic and supportive treatment.L41695

Animal studies evaluating vonoprazan mutagenicity (Ames test) have reported negative results. No effects on fertility and reproductive performance were observed in rats given 300 mg/kg/day of vonoprazan orally (133, the maximum recommended human dose). Mice given 6, 20, 60 and 200 mg/kg/day of vonoprazan orally (0.4, 4, 19, and 93 times the maximum recommended human dose) developed hyperplasia of neuroendocrine cells, gastropathy and benign and/or malignant neuroendocrine cell tumors (carcinoids) in the stomach.L41695

Vonoprazan

DB11739

small molecule approved investigational

Deskripsi

Vonoprazan is a potassium-competitive acid blocker (PCAB) that inhibits H+, K+-ATPase-mediated gastric acid secretion. PCABs represent an alternative to proton-pump inhibitors for the treatment of acid-related disorders. Unlike proton-pump inhibitors, PCABs are not affected by CYP2C19 genetic polymorphisms and do not require acid-resistant formulations.A253702 Furthermore, vonoprazan is 350-times more potent than the proton-pump inhibitor lansoprazole, thanks to its ability to accumulate in the gastric corpus mucosa, specifically in the parietal cells.A253707

In February 2015, vonoprazan was first marketed in Japan for the treatment of acid-related disorders and as an adjunct to Helicobacter pylori (H. pylori) eradication.A253702 In May 2022, the FDA approved the use of vonoprazan in a co-packaged product containing amoxicillin and clarithromycin for the treatment of H. pylori infection.L41695 Studies have shown that the concomitant use of vonoprazan, amoxicillin, and clarithromycin leads to an H. pylori eradication rate of approximately 90%.A253742

Struktur Molekul 2D

Berat 345.39
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Vonoprazan has an elimination half-life of 7.1 h following a single dose (20 mg). At steady state, the elimination half-life of vonoprazan is 6.8 h.[L41695]
Volume Distribusi Vonoprazan has an apparent oral volume of distribution of 1001 L following a single dose (20 mg). At steady state, the apparent oral volume of distribution of vonoprazan is 782.7 L.[L41695]
Klirens (Clearance) Vonoprazan has an apparent oral clearance of 97.3 L/h following a single dose (20 mg). At steady state, the apparent oral clearance of vonoprazan is 81.3 L/h.[L41695]

Absorpsi

Vonoprazan has time-independent pharmacokinetics, and steady-state concentrations are reached after 3 to 4 days. In patients given a single dose of vonoprazan, the AUC0-12h, Cmax and Tmax were 154.8 ng*hr/mL, 25.2 ng/mL, and 2.5 h. In patients given vonoprazan twice daily, the AUC0-12h, Cmax and Tmax were 272.5 ng*hr/mL, 37.8 ng/mL, and 3.0 h.L41695 In patients given 10 mg to 40 mg of vonoprazan daily for 7 days, the AUC and Cmax increased in a dose-proportional manner. In healthy subjects given 20 mg of vonoprazan, a high-fat meal led to a 5% and 15% increase in Cmax and AUC; however, these changes were not considered clinically significant.L41695

Metabolisme

Vonoprazan is metabolized by several cytochrome P450 (CYP) isoforms, mainly CYP3A4, and to a lesser extent CYP3A5, CYP2B6, CYP2C19, CYP2C9 and CYP2D6. Sulfo- and glucuronosyl-transferases also participate in the metabolism of vonoprazan, and all metabolites are pharmacologically inactive.L41695,A253702 CYP3A4 converts vonoprazan into metabolites M-I and M-II, which are then converted to glucuronic-acid-conjugated products M-I-G and M-II-G, respectively.A253707 Unlike proton pump inhibitors, the presence of CYP2C19 polymorphisms does not have a significant effect on the pharmacokinetics of vonoprazan.L41695

Rute Eliminasi

Vonoprazan is excreted in urine (67%) and feces (31%). Approximately 8% and 1.4% of the dose administered are recovered unchanged in urine and feces, respectively.L41695

Interaksi Makanan

1 Data
  • 1. Take with or without food. High-fat meals may decrease the absorption of vonoprazan; however, these changes are not considered clinically significant.

Interaksi Obat

433 Data
Atazanavir Vonoprazan can cause a decrease in the absorption of Atazanavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Bosutinib Vonoprazan can cause a decrease in the absorption of Bosutinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Cefditoren The serum concentration of Cefditoren can be decreased when it is combined with Vonoprazan.
Dabigatran etexilate Vonoprazan can cause a decrease in the absorption of Dabigatran etexilate resulting in a reduced serum concentration and potentially a decrease in efficacy.
Dabrafenib Vonoprazan can cause a decrease in the absorption of Dabrafenib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Dasatinib Vonoprazan can cause a decrease in the absorption of Dasatinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Delavirdine Vonoprazan can cause a decrease in the absorption of Delavirdine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Erlotinib Vonoprazan can cause a decrease in the absorption of Erlotinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Gefitinib Vonoprazan can cause a decrease in the absorption of Gefitinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Indinavir The metabolism of Vonoprazan can be decreased when combined with Indinavir.
Itraconazole Vonoprazan can cause a decrease in the absorption of Itraconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ledipasvir Vonoprazan can cause a decrease in the absorption of Ledipasvir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Methylphenidate Vonoprazan can cause an increase in the absorption of Methylphenidate resulting in an increased serum concentration and potentially a worsening of adverse effects.
Dexmethylphenidate Vonoprazan can cause an increase in the absorption of Dexmethylphenidate resulting in an increased serum concentration and potentially a worsening of adverse effects.
Nelfinavir The absorption of Nelfinavir can be decreased when combined with Vonoprazan.
Pazopanib Vonoprazan can cause a decrease in the absorption of Pazopanib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Raltegravir Vonoprazan can cause an increase in the absorption of Raltegravir resulting in an increased serum concentration and potentially a worsening of adverse effects.
Riociguat Vonoprazan can cause a decrease in the absorption of Riociguat resulting in a reduced serum concentration and potentially a decrease in efficacy.
Saquinavir The metabolism of Vonoprazan can be decreased when combined with Saquinavir.
Levothyroxine Vonoprazan can cause a decrease in the absorption of Levothyroxine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Bisacodyl The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Vonoprazan.
Captopril Vonoprazan can cause a decrease in the absorption of Captopril resulting in a reduced serum concentration and potentially a decrease in efficacy.
Cefuroxime The serum concentration of Cefuroxime can be decreased when it is combined with Vonoprazan.
Rifampin The therapeutic efficacy of Vonoprazan can be decreased when used in combination with Rifampicin.
Memantine Vonoprazan may decrease the excretion rate of Memantine which could result in a higher serum level.
Sulpiride The therapeutic efficacy of Sulpiride can be increased when used in combination with Vonoprazan.
Mesalazine Vonoprazan can cause a decrease in the absorption of Mesalazine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Mycophenolate mofetil Vonoprazan can cause a decrease in the absorption of Mycophenolate mofetil resulting in a reduced serum concentration and potentially a decrease in efficacy.
Mycophenolic acid Vonoprazan can cause a decrease in the absorption of Mycophenolic acid resulting in a reduced serum concentration and potentially a decrease in efficacy.
Tolevamer The therapeutic efficacy of Tolevamer can be decreased when used in combination with Vonoprazan.
Cysteamine The bioavailability of Cysteamine can be decreased when combined with Vonoprazan.
Ketoconazole Vonoprazan can cause a decrease in the absorption of Ketoconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Methenamine The therapeutic efficacy of Methenamine can be decreased when used in combination with Vonoprazan.
Iron Dextran Vonoprazan can cause a decrease in the absorption of Iron Dextran resulting in a reduced serum concentration and potentially a decrease in efficacy.
Iron Vonoprazan can cause a decrease in the absorption of Iron resulting in a reduced serum concentration and potentially a decrease in efficacy.
Prussian blue Vonoprazan can cause a decrease in the absorption of Prussian blue resulting in a reduced serum concentration and potentially a decrease in efficacy.
Iron sucrose Vonoprazan can cause a decrease in the absorption of Iron sucrose resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferric pyrophosphate Vonoprazan can cause a decrease in the absorption of Ferric pyrophosphate resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferric ammonium citrate Vonoprazan can cause a decrease in the absorption of Ferric ammonium citrate resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferumoxsil Vonoprazan can cause a decrease in the absorption of Ferumoxsil resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferumoxides Vonoprazan can cause a decrease in the absorption of Ferumoxides resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferric sulfate Vonoprazan can cause a decrease in the absorption of Ferric sulfate resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferrous bisglycinate Vonoprazan can cause a decrease in the absorption of Ferrous bisglycinate resulting in a reduced serum concentration and potentially a decrease in efficacy.
Gleptoferron Vonoprazan can cause a decrease in the absorption of Gleptoferron resulting in a reduced serum concentration and potentially a decrease in efficacy.
Perflubutane Vonoprazan can cause a decrease in the absorption of Perflubutane resulting in a reduced serum concentration and potentially a decrease in efficacy.
Sodium feredetate Vonoprazan can cause a decrease in the absorption of Sodium feredetate resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferric hydroxide Vonoprazan can cause a decrease in the absorption of Ferric hydroxide resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferric cation Vonoprazan can cause a decrease in the absorption of Ferric cation resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferrous gluconate Vonoprazan can cause a decrease in the absorption of Ferrous gluconate resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferrous succinate Vonoprazan can cause a decrease in the absorption of Ferrous succinate resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferrous fumarate Vonoprazan can cause a decrease in the absorption of Ferrous fumarate resulting in a reduced serum concentration and potentially a decrease in efficacy.
Tetraferric tricitrate decahydrate Vonoprazan can cause a decrease in the absorption of Tetraferric tricitrate decahydrate resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferric oxyhydroxide Vonoprazan can cause a decrease in the absorption of Ferric oxyhydroxide resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferric maltol Vonoprazan can cause a decrease in the absorption of Ferric maltol resulting in a reduced serum concentration and potentially a decrease in efficacy.
Iron polymaltose Vonoprazan can cause a decrease in the absorption of Iron polymaltose resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ritonavir The serum concentration of Vonoprazan can be increased when it is combined with Ritonavir.
Amprenavir The metabolism of Vonoprazan can be decreased when combined with Amprenavir.
Tipranavir The metabolism of Vonoprazan can be decreased when combined with Tipranavir.
Darunavir The metabolism of Vonoprazan can be decreased when combined with Darunavir.
Fosamprenavir Vonoprazan can cause a decrease in the absorption of Fosamprenavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Lopinavir The metabolism of Vonoprazan can be decreased when combined with Lopinavir.
Asunaprevir Vonoprazan can cause a decrease in the absorption of Asunaprevir resulting in a reduced serum concentration and potentially a decrease in efficacy.
TMC-310911 Vonoprazan can cause a decrease in the absorption of TMC-310911 resulting in a reduced serum concentration and potentially a decrease in efficacy.
Palbociclib The absorption of Palbociclib can be decreased when combined with Vonoprazan.
Ferrous sulfate anhydrous Vonoprazan can cause a decrease in the absorption of Ferrous sulfate anhydrous resulting in a reduced serum concentration and potentially a decrease in efficacy.
Octreotide Vonoprazan can cause a decrease in the absorption of Octreotide resulting in a reduced serum concentration and potentially a decrease in efficacy.
Infigratinib The serum concentration of Infigratinib can be decreased when it is combined with Vonoprazan.
Levoketoconazole Vonoprazan can cause a decrease in the absorption of Levoketoconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Phenytoin The therapeutic efficacy of Vonoprazan can be decreased when used in combination with Phenytoin.
Pentobarbital The therapeutic efficacy of Vonoprazan can be decreased when used in combination with Pentobarbital.
Carbamazepine The therapeutic efficacy of Vonoprazan can be decreased when used in combination with Carbamazepine.
Mitotane The therapeutic efficacy of Vonoprazan can be decreased when used in combination with Mitotane.
Primidone The therapeutic efficacy of Vonoprazan can be decreased when used in combination with Primidone.
Phenobarbital The therapeutic efficacy of Vonoprazan can be decreased when used in combination with Phenobarbital.
Rifapentine The therapeutic efficacy of Vonoprazan can be decreased when used in combination with Rifapentine.
Dexamethasone The therapeutic efficacy of Vonoprazan can be decreased when used in combination with Dexamethasone.
Fosphenytoin The therapeutic efficacy of Vonoprazan can be decreased when used in combination with Fosphenytoin.
St. John's Wort The therapeutic efficacy of Vonoprazan can be decreased when used in combination with St. John's Wort.
Midostaurin The therapeutic efficacy of Vonoprazan can be decreased when used in combination with Midostaurin.
Enzalutamide The therapeutic efficacy of Vonoprazan can be decreased when used in combination with Enzalutamide.
Lumacaftor The therapeutic efficacy of Vonoprazan can be decreased when used in combination with Lumacaftor.
Apalutamide The therapeutic efficacy of Vonoprazan can be decreased when used in combination with Apalutamide.
Rilpivirine The absorption of Rilpivirine can be decreased when combined with Vonoprazan.
Clopidogrel The therapeutic efficacy of Clopidogrel can be decreased when used in combination with Vonoprazan.
Citalopram The risk or severity of adverse effects can be increased when Vonoprazan is combined with Citalopram.
Cilostazol The risk or severity of adverse effects can be increased when Vonoprazan is combined with Cilostazol.
Cyclosporine The metabolism of Cyclosporine can be decreased when combined with Vonoprazan.
Fluvoxamine The metabolism of Vonoprazan can be decreased when combined with Fluvoxamine.
Fluconazole The metabolism of Vonoprazan can be decreased when combined with Fluconazole.
Erythromycin The serum concentration of Vonoprazan can be increased when it is combined with Erythromycin.
Lovastatin The metabolism of Vonoprazan can be decreased when combined with Lovastatin.
Ziprasidone The metabolism of Vonoprazan can be decreased when combined with Ziprasidone.
Isradipine The metabolism of Vonoprazan can be decreased when combined with Isradipine.
Diltiazem The metabolism of Vonoprazan can be decreased when combined with Diltiazem.
Clozapine The metabolism of Vonoprazan can be decreased when combined with Clozapine.
Haloperidol The serum concentration of Haloperidol can be increased when it is combined with Vonoprazan.
Ciprofloxacin The metabolism of Vonoprazan can be decreased when combined with Ciprofloxacin.
Voriconazole The metabolism of Vonoprazan can be decreased when combined with Voriconazole.
Nicardipine The metabolism of Vonoprazan can be decreased when combined with Nicardipine.
Verapamil The metabolism of Vonoprazan can be decreased when combined with Verapamil.

Target Protein

Hydrogen potassium ATPase ATP4A

Referensi & Sumber

Synthesis reference: Ikemoto, T., et al. (2016). Process for producing pyrrole compound (U.S. Patent No. US 9,266,831 B2). U.S. Patent and Trademark Office. https://patentimages.storage.googleapis.com/62/60/80/823d4e469ef018/US9266831.pdf
Artikel (PubMed)
  • PMID: 26369775
    Echizen H: The First-in-Class Potassium-Competitive Acid Blocker, Vonoprazan Fumarate: Pharmacokinetic and Pharmacodynamic Considerations. Clin Pharmacokinet. 2016 Apr;55(4):409-18. doi: 10.1007/s40262-015-0326-7.
  • PMID: 29383028
    Sugano K: Vonoprazan fumarate, a novel potassium-competitive acid blocker, in the management of gastroesophageal reflux disease: safety and clinical evidence to date. Therap Adv Gastroenterol. 2018 Jan 9;11:1756283X17745776. doi: 10.1177/1756283X17745776. eCollection 2018.
  • PMID: 31243237
    Kiyotoki S, Nishikawa J, Sakaida I: Efficacy of Vonoprazan for Helicobacter pylori Eradication. Intern Med. 2020 Jan 15;59(2):153-161. doi: 10.2169/internalmedicine.2521-18. Epub 2019 Jun 27.

Contoh Produk & Brand

Produk: 4 • International brands: 0
Produk
  • Voquezna
    Tablet • 13.36 mg/1 • Oral • US • Approved
  • Voquezna
    Tablet • 26.72 mg/1 • Oral • US • Approved
  • Voquezna Dual Pak
    Capsule; Kit; Tablet • - • Oral • US • Approved
  • Voquezna Triple Pak
    Capsule; Kit; Tablet • - • Oral • US • Approved

Sekuens Gen/Protein (FASTA)

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