YH-4808(YH-4808) - 药物靶点：ATPase_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点

ATPase

作用机制

ATPase抑制剂(ATP酶抑制剂)

治疗领域

消化系统疾病

在研适应症-

非在研适应症

反流性食管炎

原研机构

Yuhan Corp.

在研机构-

非在研机构

Yuhan Corp.

最高研发阶段无进展临床2期

首次获批日期-

最高研发阶段(中国)-

特殊审评-

登录后查看时间轴

关联

9

项与 YH-4808 相关的临床试验

NCT02176668 / Completed临床1期

A Randomized, Open-label, Multiple-dose, Partial Crossover Study to Explore the Pharmacokinetics and the Pharmacodynamics of YH4808 New Formulation in Healthy Subjects

The objective of this clinical trial is to explore pharmacodynamics and pharmacokinetics of YH4808 New Formulation in healthy volunteers.

开始日期2014-06-01

申办/合作机构

Yuhan Corp.

NCT02072447 / Completed早期临床1期IIT

A Study to Determine the Absolute Bioavailability of YH4808 Using Simultaneous Oral Therapeutic- and [14C]-Labeled Intravenous Microdoses

This study aims to determine the absolute bioavailability of YH4808 using simultaneous oral therapeutic- and [14C]-labeled intravenous microdoses.

开始日期2014-03-01

申办/合作机构

Seoul National University Hospital

NCT01876615 / Completed临床1期

A Randomized, Open-Label, Single-dosing and Cross-over Clinical Trial to Investigate the Safety and Pharmacokinetic Drug-Drug Interaction of YH4808 and Diclofenac in Healthy Male Volunteers

The objective of this study is to compare pharmacokinetics after single oral administration of YH4808 and Diclofenac each separately versus coadministration of YH4808 and Diclofenac in healthy male volunteers

开始日期2013-07-01

申办/合作机构

Yuhan Corp.

100 项与 YH-4808 相关的临床结果

登录后查看更多信息

100 项与 YH-4808 相关的转化医学

登录后查看更多信息

100 项与 YH-4808 相关的专利（医药）

登录后查看更多信息

7

项与 YH-4808 相关的文献（医药）

2022-09-01·CPT: Pharmacometrics & Systems Pharmacology

A population PK–PD model of YH4808, a novel P‐CAB, and intragastric pH that incorporated negative feedback by increased intragastric pH onto the systemic exposure to YH4808

Article

作者: Jang, Seong Bok ; Yu, Kyung‐Sang ; Lee, Kyeong‐Ryoon ; Lee, Howard ; Lee, Hyun A. ; Chung, Tae Kyu

AbstractYH4808 is a novel potassium‐competitive acid blocker that is under clinical development to treat patients with gastroesophageal reflux disease and peptic ulcer diseases. In this study, the pharmacokinetic (PK) and pharmacodynamic (PD) profiles of YH4808 were modeled in healthy male volunteers who received a single oral dose of YH4808 at 30, 50, 100, 200, 400, 600, and 800 mg or matching placebo and multiple once‐daily oral doses of YH4808 at 100, 200, and 400 mg or matching placebo for 7 days. A population PK–PD model adequately described the time–concentration‐effect profiles of YH4808. The maximum increasing effect of YH4808 on intragastric pH was 4.38, which was higher than the observed maximum increase in intragastric pH after omeprazole at 40 mg (2.2 in pH). The maximum inhibitory effect by the increased intragastric pH on the exposure to repeated YH4808 was 58% from baseline. Monte–Carlo simulation experiments based on the final model showed that YH4808 at 200 mg will produce a higher percentage of time at pH > 4 over 24 h on day 1 than observed value of esomeprazole at 40 mg once‐daily, an active comparator (84.7% time vs. 58.3% time, respectively). Because YH4808 at ≥200 mg resulted in a higher percentage of time at intragastric pH > 4 than seen after once‐daily esomeprazole at 40 mg and YH4808 showed acceptable tolerability at a single‐dose of 30–800 mg, we suggest to test the 200 mg once daily dosage regimen in further clinical trials of YH4808.

2021-01-01·Translational and Clinical Pharmacology

Comparison of the pharmacokinetics and pharmacodynamics of YH4808 in healthy subjects for defining an appropriate dosing regimen

Article

作者: Kim, Choon Ok ; Oh, EunSil ; Yoon, Sukyong ; Park, Min Soo ; Park, Hyeonsoo ; Jang, Seong Bok ; Byun, Hae Mi ; Kim, Heeyoung

YH4808 is a novel potassium-competitive acid blocker developed for gastric acid-related disorders. Previous studies indicate its potential to improve symptoms of gastric acid-related disorders. The current study was aimed to find the optimal regimen of YH4808 for night time pH control. This study was performed in two parts. Each was a randomized, open-label, active-controlled, multiple-doses, two-treatment, two-period crossover study conducted in 20 healthy Korean volunteers. Subjects were randomly assigned to one of the four groups. The three groups received different dosage regimens of YH4808 (100 mg twice a day, 200 mg once a day, or 200 mg twice a day), and the fourth group received esomeprazole 40 mg twice a day. The pharmacokinetic parameters demonstrated that the systemic exposure of YH4808 increased in a dose-proportional manner. The difference in the proportion of time above pH 4 over 24 h from the baseline was the greatest in the group receiving YH4808 200 mg twice a day. The values of the area under the effect curve at night time (12 A.M.-7 A.M.) were higher in all YH4808 groups than in the esomeprazole group. However, the differences among the YH4808 groups were not statistically significant (p > 0.05). YH4808 exhibited potential for better pH control during the night in comparison to esomeprazole. The optimal regimen for night time pH control among all the YH4808 regimens was 200 mg twice a day.TRIAL REGISTRATIONClinicalTrials.gov Identifier: NCT01761513.

2019-03-01·European Journal of Pharmaceutical Sciences2区 · 医学

A physiologically-based pharmacokinetic model adequately predicted the human pharmacokinetic profiles of YH4808, a novel K+-competitive acid blocker

2区 · 医学

Article

作者: Lee, Hyun A ; Lee, Kyeong-Ryoon ; Chung, Soo Yong ; Yu, Kyung-Sang ; Lee, Howard ; Hyun A. Lee ; Jang, Seong Bok

A physiologically-based pharmacokinetic (PBPK) model was developed for YH4808, a novel potassium-competitive acid blocker, using the SimCYP® Simulator based on the physicochemical, in vitro preclinical and clinical data of YH4808. The PBPK model was optimized using YH4808 concentrations obtained from the single-dose phase I clinical trial. Overall, the PBPK model adequately predicted the observed pharmacokinetic profiles of YH4808 in humans. The pharmacokinetic profiles of YH4808 after multiple oral administrations were predicted using a refined PBPK model. The ratios of model-predicted to observed C_max, AUC_inf and AUC_τ values on Day 1 and Day 7 at 100 mg were 0.7-1.0. However, the model failed to predict a decreased exposure after multiple oral administration particularly at higher doses of 200 and 400 mg. The reduced solubility of YH4808 at higher pH was hypothesized as the main cause of the reduction in exposure such that absorption was decreased as pH was increased. This hypothesis was confirmed by PBPK modeling and simulation, where intragastric pH was increased by YH4808.

100 项与 YH-4808 相关的药物交易

登录后查看更多信息

研发状态

10 条进展最快的记录,

登录

后查看更多信息

适应症	最高研发状态	国家/地区	公司	日期
反流性食管炎	临床2期	韩国	Yuhan Corp.	2012-12-01

登录后查看更多信息

临床结果

适应症

分期

评价

查看全部结果

研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT01921647 (Pubmed)	临床1期	幽门螺杆菌感染	60	YH4808, amoxicillin, and clarithromycin	(顧築廠膚艱壓築顧艱鏇) = 壓鹹醖壓鹽網鹽糧選鏇膚觸顧蓋襯簾獵鹹獵願 (齋選衊艱艱艱鬱築製網 )	-	2020-09-01
				YH4808 and amoxicillin	(顧築廠膚艱壓築顧艱鏇) = 製蓋鬱繭鑰網齋網窪糧膚觸顧蓋襯簾獵鹹獵願 (齋選衊艱艱艱鬱築製網 )