KFP-H008 blocks gastric acid secretion through inhibiting H+-K+-ATPase

Li, Cheng-yuan; Su, Mei Tzu; Yan, Yun-yi; Zhou, Lin; Ao, Luyao; Fang, Weirong; Li, Yunman

doi:10.1016/j.ejphar.2017.06.020

Cited by 16 publications

(10 citation statements)

References 43 publications

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“…Ethanol-produced gastric lesions characterized by the interruption in the mucosal layer, necrosis, edema, and leucocytes" infiltration were significantly reversed by TPM pretreatment. Formation of the hemorrhagic lesions in the stomach involves diverse mechanisms, including enhanced gastric secretion and acidity, reduction in the protective mucosal barrier, disruption of micro-vessels, infiltration of activated neutrophils, oxidative stress, increased pro-inflammatory factors, and apoptosis [ [3] , [4] , [5] , 7 , 8 ]. A reduction in the severity of the hemorrhagic lesions in the TPM pretreated animals suggests an ameliorative influence of TPM on the hemorrhagic mechanisms.…”

Section: Discussionmentioning

confidence: 99%

“…Regular alcohol use damages gastric mucosa and is associated with gastric inflammation, ulceration, and even carcinoma of the gastric tissue [ 2 ]. Alcohol causes gastric damage through different mechanisms such as increased gastric secretion, decreased mucosal protection, the release of pro-inflammatory cytokines [ [3] , [4] , [5] , [6] ], and invasion of activated neutrophils, apoptosis, and oxidative stress [ 7 , 8 ]. On the other hand, different drugs, such as TPM, are effective against alcohol abuse and dependency.…”

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Gastro protecting influence of Topiramate in ethanol produced gastric ulcers in rats

Kadasah¹,

Eid²,

Alawad³

et al. 2021

Toxicology Reports

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Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Gastro protecting influence of Topiramate in ethanol produced gastric ulcers in rats

Kadasah¹,

Eid²,

Alawad³

et al. 2021

Toxicology Reports

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show abstract

“…Other agents, DWP14012, and 1-(5-(1H-indol-5-yl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-yl)-Nmethylmethanamine (KFP-H008), P-CABs, are under development. 31,32 Tegoprazan is another potent P-CAB 33 that was successfully tested in a phase III trial in Korea and will be released to the market in 2018 ( Table 2). A compound that has a pyrrole derivative in the center was found through high-throughput screening.…”

Section: Development Of Potassium-competitive Acid Blockersmentioning

confidence: 99%

Potent Potassium-competitive Acid Blockers: A New Era for the Treatment of Acid-related Diseases

Oshima

Miwa

2018

J Neurogastroenterol Motil

137

107

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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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“…Other P-CABs (YH4808, DWP14012, and KFP-H008) are still in clinical trials. [19][20][21][22][23] Vonoprazan was significantly effective in the treatment of H. pylori infection, GERD, and LDA-induced peptic ulcers. 6,24 There are several advantages to using vonoprazan than conventional PPIs from a pharmacological point of view.…”

Section: Introductionmentioning

confidence: 99%

“…22 KFP-H008 showed a more effective, potent, and longer-lasting inhibitory action than lansoprazole in a rat model. 23 However, there are no reports about the usefulness of tegoprazan, YH4808, DWP14012, and KFP-H008 in actual clinical practice.…”

Section: Introductionmentioning

confidence: 99%

Role of Acid Suppression in Acid-related Diseases: Proton Pump Inhibitor and Potassium-competitive Acid Blocker

Mori

Suzuki

2019

J Neurogastroenterol Motil

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Proton pump inhibitors are commonly utilized for the treatment of gastric acid-related diseases, such as gastroesophageal reflux disease, peptic ulcer disease, and Helicobacter pylori infection, and for the prevention of low-dose aspirin or nonsteroidal anti-inflammatory drug-induced peptic ulcers. Vonoprazan is a first-in-class potassium-competitive acid blocker, which has distinct advantages compared to other conventional proton pump inhibitors in terms of the efficacy for acid suppression. Due to its strong gastric acid suppression capabilities, vonoprazan serves as an effective drug for the treatment of gastroesophageal reflux disease and H. pylori infection.

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KFP-H008 blocks gastric acid secretion through inhibiting H+-K+-ATPase

Cited by 16 publications

References 43 publications

Gastro protecting influence of Topiramate in ethanol produced gastric ulcers in rats

Gastro protecting influence of Topiramate in ethanol produced gastric ulcers in rats

Potent Potassium-competitive Acid Blockers: A New Era for the Treatment of Acid-related Diseases

Role of Acid Suppression in Acid-related Diseases: Proton Pump Inhibitor and Potassium-competitive Acid Blocker

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