Potent Potassium-competitive Acid Blockers: A New Era for the Treatment of Acid-related Diseases.
Potent Potassium-competitive Acid Blockers: A New Era for the Treatment of Acid-related Diseases.
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DOI：
10.5056/jnm18029
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发表时间：
2018-07-30
影响因子：
3.4
通讯作者：
Miwa H
中科院分区：
文献类型：
--
作者：
Oshima T;Miwa H
传统的质子泵抑制剂（PPI）在全球范围内被用作治疗酸相关疾病的一线疗法。然而，它们也存在一些局限性，包括起效缓慢、受细胞色素P450多态性影响、夜间效果不理想以及在酸性条件下不稳定等。传统 PPI 的替代配方已被开发出来以克服这些问题；然而，与传统 PPI 相比，这些药物在控制胃酸分泌方面仅具有很小的优势。钾竞争性酸阻滞剂 (P-CAB) 已被开发出来，具有有益的作用，包括快速、持久和可逆地抑制胃氢钾 ATP 酶（胃的质子泵）。 Vonoprazan 最近被创新为一种新型口服活性 P-CAB。目前在日本适用于治疗胃和十二指肠溃疡、反流性食管炎，以及预防小剂量阿司匹林或非甾体抗炎药相关的胃和十二指肠溃疡复发。沃诺拉赞对酸稳定，不需要肠溶衣，而且吸收很快，可以空腹服用。沃诺拉赞在酸性和中性条件下都会在壁细胞中积累。它不需要酸性环境来激活，在作用部位具有长期稳定性，并且具有令人满意的安全性和耐受性。因此，沃诺拉赞可以解决治疗酸相关疾病的未满足的医疗需求。
Conventional proton pump inhibitors (PPIs) are used as a first-line therapy to treat acid-related diseases worldwide. However, they have a number of limitations including slow onset of action, influence by cytochrome P450 polymorphisms, unsatisfactory effects at night, and instability in acidic conditions. Alternative formulations of conventional PPIs have been developed to overcome these problems; however, these drugs have only introduced small advantages for controlling acid secretion compared to conventional PPIs. Potassium-competitive acid blockers (P-CABs) were developed and have beneficial effects including rapid, long-lasting, and reversible inhibition of the gastric hydrogen potassium ATPase, the proton pump of the stomach. Vonoprazan was recently innovated as a novel, orally active P-CAB. It is currently indicated for the treatment of gastric and duodenal ulcers, reflux esophagitis, and prevention of low-dose aspirin- or nonsteroidal anti-inflammatory drug-related gastric and duodenal ulcer recurrence in Japan. Vonoprazan does not require enteric coating as it is acid-stable, and it can be taken without food because it is quickly absorbed. Vonoprazan accumulates in parietal cells under both acidic and neutral conditions. It does not require an acidic environment for activation, has long-term stability at the site of action, and has satisfactory safety and tolerability. Thus, vonoprazan may address the unmet medical need for the treatment of acid-related diseases.
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