[Translation] A single-dose and multiple-dose ascending phase I clinical study to evaluate the safety, tolerability, pharmacokinetic and pharmacodynamic characteristics of JP-1366 for injection in healthy subjects

主要目的：评价在健康成年受试者中单次及多次静脉输注注射用JP-1366的安全性和耐受性。次要目的： ● 评价在健康成年受试者中单次及多次静脉输注注射用JP-1366后原型药物及主要活性代谢产物M1的药代动力学（PK）特征； ● 比较健康成年受试者单次静脉输注注射用JP-1366与口服JP-1366片的药代动力学特征及药效动力学特征，评价口服JP-1366片的生物利用度； ● 评价在健康成年受试者中单次及多次静脉输注注射用JP-1366的药效动力学（PD）特征。 ● 比较注射用JP-1366与阳性药物注射用艾司奥美拉唑钠多次给药在健康受试者中的PD特征。探索性目的：探索在健康成年受试者中单次及多次静脉输注不同剂量注射用JP1366暴露效应关系。

[Translation]

Primary objectives: To evaluate the safety and tolerability of single and multiple intravenous infusions of JP-1366 for injection in healthy adult subjects. Secondary objectives: ● To evaluate the pharmacokinetic (PK) characteristics of the parent drug and the main active metabolite M1 of JP-1366 for injection after single and multiple intravenous infusions in healthy adult subjects; ● To compare the pharmacokinetic and pharmacodynamic characteristics of single intravenous infusion of JP-1366 for injection and oral JP-1366 tablets in healthy adult subjects, and to evaluate the bioavailability of oral JP-1366 tablets; ● To evaluate the pharmacodynamic (PD) characteristics of single and multiple intravenous infusions of JP-1366 for injection in healthy adult subjects. ● To compare the PD characteristics of JP-1366 for injection and the positive drug esomeprazole sodium for injection after multiple administration in healthy subjects. Exploratory objectives: To explore the exposure-effect relationship of single and multiple intravenous infusions of different doses of JP1366 for injection in healthy adult subjects.

Start Date26 Feb 2025

Sponsor / Collaborator

Livzon Pharmaceutical Group, Inc.

[+1]

CTR20244931

/ CompletedPhase 1

[14C]JP-1366在健康男性研究参与者中的物质平衡研究

[Translation] [14C] Study on the Material Balance of JP-1366 in Healthy Male Research Participants

主要目的 1、定量分析健康男性研究参与者单次口服[14C]JP-1366后排泄物中的总放射性，获得人体放射性排泄率和主要排泄途径； 2、定量分析健康男性研究参与者单次口服[14C]JP-1366后全血和血浆中的总放射性，获得全血和血浆中总放射性的药代动力学参数，并考察全血和血浆中的分配情况； 3、分析健康男性研究参与者单次口服[14C]JP-1366后血浆、尿液、粪便中的放射性代谢物谱，鉴定主要代谢产物，确定JP-1366在人体内的代谢及消除途径。次要目的 1、采用经过验证的LC-MS/MS方法定量分析血浆中JP-1366和代谢物M1及其他代谢产物（如适用）的浓度，获得血浆中JP-1366和代谢物M1及其他代谢产物（如适用）的药动学参数； 2、评估[14C]JP-1366单次给药后在健康男性研究参与者中的安全性。

[Translation]

Main objectives 1. Quantitatively analyze the total radioactivity in the excreta of healthy male study participants after a single oral administration of [14C] JP-1366, and obtain the human radioactive excretion rate and main excretion pathway; 2. Quantitatively analyze the total radioactivity in whole blood and plasma of healthy male study participants after a single oral administration of [14C] JP-1366, obtain the pharmacokinetic parameters of total radioactivity in whole blood and plasma, and investigate the distribution in whole blood and plasma; 3. Analyze the radioactive metabolite spectrum in plasma, urine, and feces of healthy male study participants after a single oral administration of [14C] JP-1366, identify the main metabolites, and determine the metabolism and elimination pathway of JP-1366 in the human body. Secondary objectives 1. To quantitatively analyze the concentrations of JP-1366 and metabolite M1 and other metabolites (if applicable) in plasma using a validated LC-MS/MS method and obtain the pharmacokinetic parameters of JP-1366 and metabolite M1 and other metabolites (if applicable) in plasma; 2. To evaluate the safety of [14C]JP-1366 in healthy male study participants after a single dose.

Start Date06 Jan 2025

Sponsor / Collaborator

Livzon Group Livzon Pharmaceutical Factory

[+1]

CTR20243824

/ RecruitingPhase 3

JP-1366片与耐信®在反流性食管炎受试者中的多中心、随机、双盲双模拟、阳性平行对照的III期临床研究

[Translation] A multicenter, randomized, double-blind, double-dummy, positive parallel controlled phase III clinical study of JP-1366 tablets and Nexium® in subjects with reflux esophagitis

评价JP-1366片与耐信®（艾司奥美拉唑镁肠溶片）在反流性食管炎受试者中的有效性与安全性。

[Translation]

To evaluate the efficacy and safety of JP-1366 tablets and Nexium® (esomeprazole magnesium enteric-coated tablets) in subjects with reflux esophagitis.

Start Date05 Dec 2024

Sponsor / Collaborator

Livzon Group Livzon Pharmaceutical Factory

[+1]

100 Clinical Results associated with Zastaprazan citrate

100 Translational Medicine associated with Zastaprazan citrate

100 Patents (Medical) associated with Zastaprazan citrate

Literatures (Medical) associated with Zastaprazan citrate

01 May 2025·ANNALS OF INTERNAL MEDICINE

Gastroenterology/Hepatology: What You May Have Missed in 2024

Review

Author: Samnani, Sunil ; Bretthauer, Michael ; Jamal, Imran ; Song, Yi Nong ; Cintosun, Amber

This article highlights selected major advances in gastroenterology and hepatology from 2024 that are relevant for internal medicine specialists. In colorectal cancer (CRC) screening, new developments include a head-to-head comparison of different fecal immunochemical tests and a new blood-based DNA screening test, benefits and harms of artificial intelligence-assisted colonoscopy, and adenoma detection rate improvement and risk for cancer. Treatment options for metabolic dysfunction-associated steatotic liver disease now include resmetirom, a recently approved drug for treatment of patients with moderate-to-severe fibrosis, and liver transplantation may now be an option in patients with unresectable colorectal liver metastases. Also featured are new data on the efficacy of indomethacin and pancreatic stent placement for prevention of pancreatitis after endoscopic retrograde cholangiopancreatography and news on the efficacy and safety of zastaprazan, a new potassium-competitive acid blocker for reflux esophagitis. Finally, a recent randomized trial is highlighted that has dispelled concerns about potential harms of proton-pump inhibitors for stress ulcer prophylaxis in patients receiving invasive mechanical ventilation.

01 Feb 2025·AMERICAN JOURNAL OF GASTROENTEROLOGY

Randomized, Double-Blind, Active-Controlled Phase 3 Study to Evaluate Efficacy and Safety of Zastaprazan Compared With Esomeprazole in Erosive Esophagitis

Article

Author: Kim, John ; Lee, Dong Ho ; Lee, Hang Lak ; Yu, Eunju ; Kim, Hyun-Soo ; Jung, Hwoon-Yong ; Kim, Jun ; Kim, Gwang Ha ; Choi, Suck Chei ; Chung, Woo Chul ; Kwon, Hyesoo ; Kim, Ji Won ; Cheung, Dae Young ; Cho, Yu Kyung ; Oh, Jung-Hwan

INTRODUCTION::

Zastaprazan is a potent potassium-competitive acid blocker developed to treat gastroesophageal reflux disease. The aim of this study was to evaluate the efficacy and safety of zastaprazan compared with esomeprazole in patient with erosive esophagitis (EE).

METHODS::

A phase III, multicenter, randomized, double-blind, noninferiority clinical study was conducted with 300 subjects with confirmed EE. Subjects were randomized to receive zastaprazan 20 mg or esomeprazole 40 mg once daily up to 8 weeks. The primary end point was the cumulative proportion of subject with healed EE confirmed by endoscopy at week 8. The secondary end points included the healing rate at week 4, symptom response, and quality of life assessment. Safety profiles and serum gastrin levels were also assessed.

RESULTS::

In the full analysis set, the cumulative healing rate at week 8 were 97.92% (141/144) for zastaprazan and 94.93% (131/138) (P = 0.178) for esomeprazole. The healing rate at week 4 in the zastaprazan group was higher than the esomeprazole group (95.14% [137/144] vs 87.68% [121/138]; P = 0.026). There was no significant difference between groups in healing rates (the per-protocol set) at week 8 and week 4, symptom responses, quality of life assessments, and safety profiles. In addition, serum gastrin levels increased during treatment in both groups, with a significant difference between the 2 groups (P = 0.047), but both decreased after treatment.

DISCUSSION::

An 8-week therapy of zastaprazan 20 mg is noninferior to esomeprazole 40 mg in subjects with predominantly low-grade EE. The healing rate at week 4 appears to be higher for zastaprazan than esomeprazole.

01 Dec 2024·CPT-Pharmacometrics & Systems Pharmacology

Population pharmacokinetic analysis of zastaprazan (JP‐1366), a novel potassium‐competitive acid blocker, in patients and healthy volunteers

Article

Author: Lee, SeungHwan ; Hwang, Inyoung ; Yang, Eunsol ; Ji, Sang Chun ; Kim, John

Abstract:

Zastaprazan (JP‐1366) is a novel potassium‐competitive acid blocker for the treatment of acid‐related disorders. We aimed to establish a population pharmacokinetic (PK) model of zastaprazan, thereby characterizing the PK of zastaprazan in patients with gastroesophageal reflux disease (GERD) as well as evaluating the impact of various covariates, including CYP2C19 phenotypes, on zastaprazan PK. This population PK analysis included zastaprazan plasma concentration–time data from 92 patients with erosive GERD and 68 healthy volunteers without any gastrointestinal disorders and was performed using nonlinear mixed‐effect modeling. Simulations were conducted to predict zastaprazan PK under various dosing regimens in patients with GERD. The plasma PK of zastaprazan was adequately described by a two‐compartment model with Erlang‐type absorption (six sequential compartments) and first‐order elimination. CYP2C19 phenotypes had no significant effect on zastaprazan PK. The disease status was identified as a significant covariate on apparent clearance of zastaprazan, showing lower values in patients with GERD compared to healthy volunteers. However, the model‐based simulation indicated that the impact of disease status on zastaprazan exposure was not clinically meaningful. Overall, the current population PK model successfully characterized the observed zastaprazan PK in both patients with GERD and healthy volunteers.

News (Medical) associated with Zastaprazan citrate

29 May 2024

·www.prnewswire.com

Onconic Therapeutics Announces Positive Phase 3 Results for JAQBO at Digestive Diseases Week 2024

SEOUL, South Korea and WASHINGTON, May 29, 2024 /PRNewswire/ -- Onconic Therapeutics, a clinical-stage biopharmaceutical company dedicated to developing innovative treatments for oncology and gastrointestinal disorders, announced today the results of its Phase 3 ZERO-1 study of JAQBO (zastaprazan citrate) at Digestive Disease Week (DDW) 2024, held in Washington D.C. from May 18-21, 2024. Dr. Jung-hwan Oh, MD, PhD, a professor and gastroenterologist at Eunpyeong St. Mary's Hospital in Korea, and the lead author of the ZERO-1 study, presented the phase 3 trial results during an oral presentation session. This randomized, double-blind, active-controlled study compared the efficacy and safety of zastaprazan to esomeprazole in patients with erosive esophagitis. Participants received either 20 mg of zastaprazan or 40 mg of esomeprazole daily for up to eight weeks. Among the 300 enrolled patients, the study demonstrated a cumulative healing rate of 97.9% in the zastaprazan group at week 8, compared to 94.9% in the esomeprazole group. By week 4, the healing rate was 95.1% for zastaprazan compared to 87.7% for esomeprazole, a statistically significant difference. These results confirmed that zastaprazan is non-inferior to esomeprazole. Additionally, zastaprazan showed a rapid onset of action within one hour and maintained a gastric pH above four for 85% of the 24-hour period, highlighting its potential to effectively alleviate nighttime acid reflux symptoms with its long-lasting efficacy. "We are encouraged by the positive results of the ZERO-1 study, which highlight the efficacy and safety of JAQBO for patients with erosive esophagitis," said John Kim, Ph.D., CEO of Onconic Therapeutics. "The recent approval by the MFDS of Korea is a significant milestone for Onconic Therapeutics. We are hopeful that JAQBO can improve patient care globally by providing rapid and sustained relief from symptoms, and we are committed to pursuing its development for broader international markets." In March 2023, JAQBO was licensed to Livzon Pharmaceutical Group, the leading pharmaceutical company in China, for development and commercialization in the Greater China market. About Zastaprazan Zastaprazan, developed by Onconic Therapeutics, was approved for the treatment of erosive esophagitis under the brand name JAQBO by the Ministry of Food and Drug Safety (MFDS) of Korea in April 2024. About Onconic Therapeutics Onconic Therapeutics is a clinical-stage biopharmaceutical company focused on developing novel therapeutics to address unmet medical needs. The company is dedicated to improving patient outcomes and providing innovative healthcare solutions for cancer and gastrointestinal disorders. SOURCE Onconic Therapeutics

Clinical ResultPhase 3Drug Approval

29 May 2024

·firstwordpharma.com

Onconic presents latest Phase III Jaqbo data in erosive esophagitis

Onconic Therapeutics announced on Wednesday that Jaqbo (zastaprazan citrate) demonstrated efficacy and safety in a Phase III study of patients with erosive esophagitis. The results on the next-generation potassium competitive blocker (P-CAB) were presented at Digestive Disease Week (DDW)."We are hopeful that Jaqbo can improve patient care globally by providing rapid and sustained relief from symptoms, and we are committed to pursuing its development for broader international markets," said CEO John Kim. Jaqbo was approved for the treatment of erosive esophagitis by the Ministry of Food and Drug Safety (MFDS) of Korea in April.The ZERO-1 trial compared the efficacy and safety of Jaqbo to AstraZeneca's Nexium (esomeprazole) in 300 patients with erosive esophagitis. Participants received either Jaqbo or Nexium daily for up to eight weeks.Non-inferior to NexiumAt week eight, the cumulative healing rate was 97.9% in the Jaqbo group and 94.9% in the Nexium group. By week four, the respective healing rates were 95.1% and 87.7%, representing a statistically significant difference. The results confirm that Jaqbo is non-inferior to Nexium.Additionally, Jaqbo showed a "rapid onset of action within one hour and maintained a gastric pH above four for 85% of the 24-hour period, highlighting its potential to effectively alleviate nighttime acid reflux symptoms with its long-lasting efficacy," the company said.In 2023, Jaqbo was licensed to China's Livzon Pharmaceutical Group for development and commercialisation in the Greater China market.

Clinical ResultPhase 3Drug Approval

25 Apr 2024

·www.prnewswire.com

Onconic Therapeutics Receives MFDS Approval for JAQBO, a New Treatment for Gastroesophageal Reflux Disease (GERD)

SEOUL, South Korea, April 25, 2024 /PRNewswire/ -- Onconic Therapeutics, a leading biotechnology company in Korea, today announced that the Ministry of Food and Drug Safety (MFDS) of Korea has approved JAQBO (zastaprazan citrate) for the treatment of erosive gastroesophageal reflux disease (GERD) in adults. JAQBO is a next-generation potassium competitive blocker (P-CAB) expected to become the new standard treatment in the market for gastric acid related diseases. JAQBO directly binds to proton pumps in a competitive manner to reduce gastric acid secretion. This novel mechanism allows quick onset of action regardless of the acidity level in the stomach, offering immediate symptom relief. In addition, longer duration of acid suppression with no food effect could provide a new paradigm in GERD treatment. The MFDS approval of JAQBO is based on comprehensive results including the Phase III clinical trial across 28 sites in Korea. The study demonstrated JAQBO's effectiveness on erosive esophagitis, with a healing rate of 97.9% after 8 weeks of treatment. These results were presented at the United European Gastroenterology Week in October 2023. Onconic Therapeutics aims to launch JAQBO this year after listing for National Healthcare Insurance Reimbursement in Korea. Domestic sales of JAQBO will be handled by Jeil Pharmaceutical, Onconic Therapeutics's parent company. In March 2023, JAQBO was licensed out to Livzon Pharmaceutical Group, the leading seller of PPIs in China for development and commercialization, in a deal value of $127.5 million for Greater China. Onconic Therapeutics is committed to enhancing gastrointestinal treatment and improving patient outcomes by expanding additional indications. About Onconic Therapeutics Onconic Therapeutics is a Korean leader in developing novel drugs. With a focus on innovative research and clinical excellence, Onconic Therapeutics is dedicated to improving patient outcomes and providing quality healthcare solutions for cancer and gastrointestinal disorders. Forward-Looking Statement This press release contains forward-looking statements that are based on our current expectations, forecasts, and assumptions. These statements involve risks and uncertainties that could cause actual results to differ materially from those anticipated or projected. Forward-looking statements include statements about our future financial performance, business strategy, plans and objectives. Factors that could cause such differences include but are not limited to economic conditions, market demand, competitive pressures, and regulatory changes. We undertake no obligation to update any forward-looking statements to reflect events or circumstances after the date of this press release. SOURCE Onconic Therapeutics

Phase 3Clinical ResultDrug ApprovalBiosimilar

100 Deals associated with Zastaprazan citrate

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Erosive gastro-esophageal reflux disease	South Korea	Onconic Therapeutics, Inc.	24 Apr 2024

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Esophagitis, Peptic	Phase 3	China	Lizhu Group Lizhu Medicine Research Institute	05 Dec 2024
Esophagitis, Peptic	Phase 3	China	Livzon Group Livzon Pharmaceutical Factory	05 Dec 2024
Stomach Ulcer	Phase 3	United States	Onconic Therapeutics, Inc.	19 Sep 2022
Erosive esophagitis	Phase 3	South Korea	Onconic Therapeutics, Inc.	17 Jan 2022
Peptic Ulcer Hemorrhage	Phase 1	China	Livzon Pharmaceutical Group, Inc.	26 Feb 2025
Helicobacter-associated gastritis	Phase 1	United States	Onconic Therapeutics, Inc.	18 Nov 2020
Ulcer	Phase 1	United States	Jeil Pharmaceutical Co., Ltd.	22 Dec 2017

Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT05443984 (Pubmed) Manual	Phase 3	Erosive esophagitis	300	Zastaprazan 20 mg	uzofexfjeo(fwhpnewebm) = kpirnikdrm nqmiorfekc (pbqkysbipl ) View more	Positive	03 Jul 2024
				Esomeprazole 40 mg	uzofexfjeo(fwhpnewebm) = wipqfghwxa nqmiorfekc (pbqkysbipl ) View more
NCT05443984 (ZERO-1, PRNewswire) Manual	Phase 3	Erosive esophagitis	300	zastaprazan 20 mg	chocnrkpkk(vnsfqoxujk) = bcbjyxvtaf zkqyoalmgk (ixvieksgvv ) View more	Non-inferior	29 May 2024
				埃索美拉唑 40 mg	chocnrkpkk(vnsfqoxujk) = sirbpwvbjo zkqyoalmgk (ixvieksgvv ) View more
Pubmed Manual	Clinical	Hyperchlorhydria	-	Zastaprazan 20mg	ltpyfjweqg(tyvksfszkv) = kmgtvqacsu gfjxgmcwaz (ofeitbljsc )	Positive	02 Feb 2023
				Zastaprazan 40mg	ltpyfjweqg(tyvksfszkv) = lxbhmlwvru gfjxgmcwaz (ofeitbljsc )

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