2019 03 v.28 219-222
钾离子竞争性酸阻断剂——伏诺拉生
基金项目(Foundation):
邮箱(Email):
DOI:
10.19577/j.1007-4406.2019.03.014
中文作者单位:
复旦大学药学院药理学与生物化学教研室;
摘要(Abstract):
质子泵抑制剂(PPIs)是目前治疗胃酸相关疾病的主要治疗药物,然而在临床应用中常表现出某些局限性,如起效慢和个体间变异大等。钾离子竞争性酸阻断剂(P-CABs)是一类新型的抑酸药物,其代表药物为伏诺拉生。该类药物与K~+竞争H~+,K~+-ATP酶(质子泵)上的结合位点从而抑制胃壁细胞分泌胃酸,其新颖的作用机制及特有药动学特征,使其显示出优于PPIs的特性,如起效快、结构稳定、抑酸效果持久、个体差异小和不良反应少等。多项Ⅲ期临床研究的结果显示伏诺拉生在治疗反流性食管炎和根除幽门螺旋杆菌中安全有效且耐受性良好,有望为酸相关性疾病的临床治疗提供一个新的选择。
关键词(KeyWords):
伏诺拉生;;钾离子竞争性酸阻断剂;;质子泵抑制剂;;酸相关性疾病;;作用机制
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参考文献
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[22] SUZUKI S,GOTODA T,KUSANO C,et al.The efficacy and tolerability of a triple therapy containing a potassium-competitive acid blocker compared with a 7-day PPI-based low-dose clarithromycin triple therapy[J].Am J Gastroenterol,2016,111(7):949.
[23] MRAUYAMA M,TANAKA N,KUBOTA D,et al.Vonoprazan-based regimen is more useful than PPI-based one as a first-line helicobacter pylorieradication:a randomized controlled trial[J].Can J Gastroenterol Hepatol,2017,2017:4385161.
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[26] SUE S,KUWASHIMA H,IWATA Y,et al.The superiority of vonoprazan-based first-line triple therapy with clarithromycin:a prospective multi-center cohort study on helicobacter pylori eradication[J].Intern Med,2017,56(11):1277.
[27] TAMAKI H,MORITA M,NODA T,et al.Sa1190 - Open-label randomized controlled trial of vonoprazan and esomeprazole in first-line triple therapy against helicobacter pylori,infection[J].Gastroenterol,2017,152:5.
[28] YAMADA S,KAWAKAMI T,NAKATSUGAWA Y,et al.Usefulness of vonoprazan,a potassium ion-competitive acid blocker,for primary eradication of Helicobacter pylori[J].World J Gastrointest Pharmacol Ther,2016,7(4):550.
[29] ONO S,KATO M,NAKAWA S,et al.Vonoprazan improves the efficacy of Helicobacter pylori eradication therapy with a regimen consisting of clarithromycin and metronidazole in patients allergic to penicillin[J].Helicobacter,2017,22(3):e12374.
[30] PARSONS M E,KEELING D J.Novel approaches to the pharmacological blockade of gastric acid secretion[J].Expert Opin Investig Drugs,2005,14(4):411.
[31] JENKINS H,SAKURAI Y,NISHIMURA A,et al.Randomised clinical trial:safety,tolerability,pharmacokinetics and pharmacodynamics of repeated doses of TAK-438 (vonoprazan),a novel potassium-competitive acid blocker,in healthy male subjects[J].Aliment Pharmacol Ther,2015,41(7):636.
[32] SHINOZAKI S,NOMOTO H,KONDO Y,et al.Comparison of vonoprazan and proton pump inhibitors for eradication of Helicobacter pylori[J].Kaohsiung J Med Sci,2016,32(5):255.
[33] ASTRUC B,JENKINS H,JENKINS R.Effect of therapeutic and supratherapeutic doses of vonoprazan on the QT/QTc interval in a phase I randomized study in healthy subjects[J].Clin Transl Sci,2017,10(3):208.
[34] JOHNSON D A,KATZ P O,ARMSTRONG D,et al.The safety of appropriate use of over-the-counter proton pump inhibitors:an evidence-based review and delphi consensus[J].Drugs,2017,77(5):547.
[2] AGARWAL V,BANSAL M.Statistical optimization and fabrication of a press coated pulsatile dosage form to treat nocturnal acid breakthrough[J].Curr Drug Deliv,2013,10(4):444.
[3] 盛一梁,沈建飞,吴嫣,等.质子泵抑制剂与临床常用药物相互作用的研究进展[J].中国医院用药评价与分析,2017,17(11):1582.
[4] GEIBEL J P.Role of potassium in acid secretion[J].World J Gastroenterol,2005,11(34):5259.
[5] ECHIZEN H.The first-in-class potassium-competitive acid blocker,vonoprazan fumarate:pharmacokinetic and pharmacodynamic considerations[J].Clin Pharmacokinet,2016,55(4):409.
[6] 朱乐亭,韩容,赵志刚.奥美拉唑注射剂使用过程中变色原因及对策[J].中国药房,2008,19(10):800.
[7] OTAKE K,SASURAI Y,NISHIDA H,et al.Characteristics of the novel potassium-competitive acid blocker bonoprazan fumarate (TAK-438)[J].Adv Ther,2016,33(7):1140.
[8] MATSUKAWA J,KOGAME A,TAGAWA Y,et al.Radiographic localization study of a novel potassium-competitive acid blocker,vonoprazan,in the rat gastric mucosa[J].Dig Dis Sci,2016,61(7):1888.
[9] HORI Y,IMANISHI A,MATSUKAWA J,et al.1-[5-(2-Fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-yl]-N-methylmethanamine,monofumarate (TAK-438),a novel and potent potassium-competitive acid blocker for the treatment of acid-related diseases[J].J Pharmacol Exp Ther,2010,335(1):231.
[10] SCOTT D R,MUNSON K B,MARCUS E A,et al.The binding selectivity of vonoprazan (TAK-438) to the gastric H+,K+-ATPase[J].Aliment Pharmacol Ther,2015,42(11-12):1315.
[11] SHIN J M,INATOMI N,MUNSON K,et al.Characterization of a novel potassium-competitive acid blocker of the gastric H,K-ATPase,1-[5-(2-Fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-y1]-N-methylmethanamine monofumarate (TAK-438)[J].J Pharmacol Exp Ther,2011,339(2):412.
[12] 陈坚.质子泵抑制剂的分类及药理学特性[J].上海医药,2013,34(21):3.
[13] JENKINS H,SAKURAIY,NISHIMURA A,et al.Randomised clinical trial:safety,tolerability,pharmacokinetics and pharmacodynamics of repeated doses of TAK-438 (vonoprazan),a novel potassium-competitive acid blocker,in healthy male subjects[J].Aliment Pharmacol Ther,2015,41(7):636.
[14] SAKURAI Y,NISHIMURA A,KENNEDY G,et al.Safety,tolerability,pharmacokinetics and pharmacodynamics of single rising TAK-438 (Vonoprazan) doses in healthy male Japanese/non-Japanese subjects[J].Clin Transl Gastroenterol,2015,6:e94.
[15] KAGAMI T,SAHARA S,ICHIKAWA H,et al.Potent acid inhibition by vonoprazan in comparison with esomeprazole,with reference to CYP2C19 genotype[J].Aliment Pharmacol Ther,2016,43(10):1048.
[16] YANG X,LI Y,SUN Y,et al.Vonoprazan:a Novel and Potent alternative in the treatment of acid-related diseases[J].Dig Dis Sci,2018,63(2):302.
[17] WILLIAMS M P,SERCOMBE J,HAMILTON M I,et al.A placebo-controlled trial to assess the effects of 8 days of dosing with rabeprazole versus omeprazole on 24-h intragastric acidity and plasma gastrin concentrations in young healthy male subjects[J].Aliment Pharmacol Ther,1998,12(11):1079.
[18] SAKURAIY,MORI Y,OKAMOTO H,et al.Acid-inhibitory effects of vonoprazan 20 mg compared with esomeprazole 20 mg or rabeprazole 10 mg in healthy adult male subjects——a randomised open-label cross-over study[J].Aliment Pharmacol Ther,2015,42(6):719.
[19] ASHIDA K,SAKURAI Y,NISHIMURA A,et al.Randomised clinical trial:a dose-ranging study of vonoprazan,a novel potassium-competitive acid blocker,vs.lansoprazole for the treatment of erosive oesophagitis[J].Aliment Pharmacol Ther,2015,42(6):685.
[20] ASHIDA K,SAKURAI Y,HORI T,et al.Randomised clinical trial:vonoprazan,a novel potassium-competitive acid blocker,vs.lansoprazole for the healing of erosive oesophagitis[J].Aliment Pharmacol Ther,2016,43(2):240.
[21] ASHIDA K,IWAKRRI K,HIRAMATUS N,et al.Maintenance for healed erosive esophagitis:phase III comparison of vonoprazan with lansoprazole[J].World J Gastroenterol,2018,24(14):1550.
[22] SUZUKI S,GOTODA T,KUSANO C,et al.The efficacy and tolerability of a triple therapy containing a potassium-competitive acid blocker compared with a 7-day PPI-based low-dose clarithromycin triple therapy[J].Am J Gastroenterol,2016,111(7):949.
[23] MRAUYAMA M,TANAKA N,KUBOTA D,et al.Vonoprazan-based regimen is more useful than PPI-based one as a first-line helicobacter pylorieradication:a randomized controlled trial[J].Can J Gastroenterol Hepatol,2017,2017:4385161.
[24] YOSHIMICHI T ,SHINICHI O ,HIROYOSHI E ,et al.Tu1309-,Helicobacter pylori,eradication rate was not influenced by the life style including smoking and drinking and the life style related diseases,whereas eradication with vonoprazan was more effective compared to proton pump inhibitors[J].Gastroenterol,2018,154(6):930.
[25] TANABE H,YOSHINO K,ANDO K,et al.Vonoprazan-based triple therapy is non-inferior to susceptibility-guided proton pump inhibitor-based triple therapy for Helicobacter pylori eradication[J].Ann Clin Microbiol Antimicrob,2018,17(1):29.
[26] SUE S,KUWASHIMA H,IWATA Y,et al.The superiority of vonoprazan-based first-line triple therapy with clarithromycin:a prospective multi-center cohort study on helicobacter pylori eradication[J].Intern Med,2017,56(11):1277.
[27] TAMAKI H,MORITA M,NODA T,et al.Sa1190 - Open-label randomized controlled trial of vonoprazan and esomeprazole in first-line triple therapy against helicobacter pylori,infection[J].Gastroenterol,2017,152:5.
[28] YAMADA S,KAWAKAMI T,NAKATSUGAWA Y,et al.Usefulness of vonoprazan,a potassium ion-competitive acid blocker,for primary eradication of Helicobacter pylori[J].World J Gastrointest Pharmacol Ther,2016,7(4):550.
[29] ONO S,KATO M,NAKAWA S,et al.Vonoprazan improves the efficacy of Helicobacter pylori eradication therapy with a regimen consisting of clarithromycin and metronidazole in patients allergic to penicillin[J].Helicobacter,2017,22(3):e12374.
[30] PARSONS M E,KEELING D J.Novel approaches to the pharmacological blockade of gastric acid secretion[J].Expert Opin Investig Drugs,2005,14(4):411.
[31] JENKINS H,SAKURAI Y,NISHIMURA A,et al.Randomised clinical trial:safety,tolerability,pharmacokinetics and pharmacodynamics of repeated doses of TAK-438 (vonoprazan),a novel potassium-competitive acid blocker,in healthy male subjects[J].Aliment Pharmacol Ther,2015,41(7):636.
[32] SHINOZAKI S,NOMOTO H,KONDO Y,et al.Comparison of vonoprazan and proton pump inhibitors for eradication of Helicobacter pylori[J].Kaohsiung J Med Sci,2016,32(5):255.
[33] ASTRUC B,JENKINS H,JENKINS R.Effect of therapeutic and supratherapeutic doses of vonoprazan on the QT/QTc interval in a phase I randomized study in healthy subjects[J].Clin Transl Sci,2017,10(3):208.
[34] JOHNSON D A,KATZ P O,ARMSTRONG D,et al.The safety of appropriate use of over-the-counter proton pump inhibitors:an evidence-based review and delphi consensus[J].Drugs,2017,77(5):547.
基本信息:
DOI：10.19577/j.1007-4406.2019.03.014
中图分类号:R975
引用信息:
[1]何金杰,程能能.钾离子竞争性酸阻断剂——伏诺拉生[J].中国临床药学杂志,2019,28(03):219-222.DOI:10.19577/j.1007-4406.2019.03.014.
基金信息: