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主要目的是评价安纳拉唑钠肠溶片治疗反流性食管炎的有效性。次要目的是评价安纳拉唑钠肠溶片对反流性食管炎患者的症状控制和生活质量改善的有效性；评价安纳拉唑钠肠溶片治疗反流性食管炎的安全性；评价安纳拉唑钠肠溶片口服给药在反流性食管炎受试者中的群体药代动力学。探索性目的是探索药物代谢酶的基因多态性对药物暴露量和/或疗效的影响。

[Translation]

The primary objective was to evaluate the effectiveness of Anaprazole Sodium Enteric-coated Tablets in the treatment of reflux esophagitis. The secondary objectives were to evaluate the effectiveness of Anaprazole Sodium Enteric-coated Tablets in symptom control and quality of life improvement in patients with reflux esophagitis; to evaluate the safety of Anaprazole Sodium Enteric-coated Tablets in the treatment of reflux esophagitis; and to evaluate the population pharmacokinetics of Anaprazole Sodium Enteric-coated Tablets in subjects with reflux esophagitis after oral administration. The exploratory objective was to explore the effects of genetic polymorphisms of drug-metabolizing enzymes on drug exposure and/or efficacy.

Start Date06 Dec 2022

Sponsor / Collaborator

Xuanzhu (Beijing) Pharmaceutical Technology Co., Ltd.

NCT05604261

/ Unknown statusPhase 2

A Multicenter, Randomized, Double-blind, Double-dummy, Positive Drug Parallel Controlled Phase II Clinical Trial to Evaluate Efficacy and Safety of Anaprazole Sodium Enteric-coated Tablets in the Treatment of Reflux Esophagitis

A phase 2, randomized, double-blind, double-dummy, positive drug parallel controlled, multicenter trial to evaluate efficacy and safety of within 8 weeks (including 8 weeks) treatment of Anaprazole 40mg QD, 60mg QD compared with Rabeprazole 20mg QD in patients with reflux esophagitis.

Start Date01 Dec 2022

Sponsor / Collaborator

Xuanzhu Biopharmaceutical Co., Ltd.

CTR20201309

/ CompletedPhase 1

单中心、开放、单剂量的物质平衡试验，研究口服20 mg/100 μCi [14C]-安纳拉唑钠肠溶胶囊后体内吸收、代谢和排泄

[Translation] A single-center, open-label, single-dose, mass balance trial to investigate the absorption, metabolism, and excretion of 20 mg/100 μCi of [14C]-anaprazole sodium enteric-coated capsules

考察[14C]-安纳拉唑钠在健康受试者全血和血浆中总放射性的药代动力学；定量分析健康受试者口服[14C]-安纳拉唑钠肠溶胶囊后排泄物的总放射性，获得人体内物质平衡数据及主要排泄途径；测定健康受试者口服[14C]-安纳拉唑钠肠溶胶囊后血浆、尿液和粪便中的放射性代谢物谱并鉴定主要代谢产物，提供安纳拉唑钠在人体内主要代谢途径数据。

[Translation]

To investigate the pharmacokinetics of total radioactivity of [14C]-anaprazole sodium in whole blood and plasma of healthy subjects; To quantitatively analyze the total radioactivity excreted in the excreta of healthy subjects after oral administration of [14C]-anaprazole sodium enteric-coated capsules, and obtain the material balance data and main excretion pathways in the human body; To determine the radioactive metabolite profile in the plasma, urine and feces of healthy subjects after oral administration of [14C]-anaprazole sodium enteric-coated capsules and identify the main metabolites, and provide data on the main metabolic pathways of anaprazole sodium in the human body.

Start Date08 Sep 2020

Sponsor / Collaborator

Beijing Sihuan Pharmaceutical Co. Ltd.

[+1]

100 Clinical Results associated with Anaprazole Sodium

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100 Translational Medicine associated with Anaprazole Sodium

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100 Patents (Medical) associated with Anaprazole Sodium

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11

Literatures (Medical) associated with Anaprazole Sodium

01 Oct 2024·Clinical Pharmacology in Drug Development

Absorption, Metabolism, and Excretion of [¹⁴C]‐Labeled Anaprazole: A New Proton Pump Inhibitor, After a Single Oral Administration in Healthy Chinese Male Subjects

Article

Author: Xie, Lijun ; Shao, Feng ; Zhang, Lingling ; Wang, Li ; Zhou, Chen ; Zhou, Sufeng ; Liu, Wei ; Guo, Lian ; Xu, Lingmei ; Li, Huan ; Ding, Sijia ; Zhang, Chen ; Wang, Lu ; Zhu, Bei ; Chen, Juan ; Xu, Yanjun

AbstractAnaprazole is a proton pump inhibitor. This study aims to elucidate absorption, metabolism, and excretion pathways of anaprazole sodium in the human body. A total of 4 healthy Chinese male subjects were administered a single oral dose of 20 mg/100 µCi of [14C]‐anaprazole sodium enteric‐coated capsules. The whole blood, plasma, and excreta were analyzed for a total radioactivity (TRA) and metabolite profile. The cumulative radioactivity excretion rate was 93.2%, with 53.3% and 39.9% of the radioactive dose excreted in urine and feces, respectively, and 91.6% of dose recovered within 96 hours after dosing. The parent drug, anaprazole, showed good absorption and was extensively metabolized majorly to thioether M8‐1 via nonenzymatic metabolism. Overall, 35 metabolites were identified in plasma, urine, and fecal samples. Anaprazole was the most abundant component in plasma followed by the thioether M8‐1, accounting for 28.3% and 16.6%, respectively, of the plasma TRA. Thioether carboxylic acid XZP‐3409 (26.3% of urine TRA) and XZP‐3409 oxidation and dehydrogenation product M417a (15.1% of fecal TRA) were the major metabolites present in urine and feces, respectively. Anaprazole was undetectable in urine, while fecal samples showed traces (0.07% dose). Blood/plasma ratios of the radioactivity (approximately 0.60) remained consistent over time. Anaprazole showed good absorption and was extensively metabolized majorly to thioether M8‐1 via nonenzymatic metabolism, and cytochrome P450 3A4 also contributed to its metabolism in healthy individuals.

01 Jul 2024·Clinical Pharmacology in Drug Development

Safety, Tolerability, and Pharmacokinetics of Anaprazole, a Novel Proton Pump Inhibitor, in Healthy Chinese Subjects

Article

Author: Xu, Haiyan ; Li, Haiyan ; Xu, Yanjun ; Niu, Xiaoye ; Ma, Xifeng ; Wang, Li ; Liu, Fei ; Cheng, Fang ; Wang, Fangfang

AbstractAnaprazole, a newly developed oral proton pump inhibitor, was evaluated for safety, tolerability, and pharmacokinetics in healthy Chinese subjects. This study involved administering either anaprazole sodium enteric‐coated tablet or placebo, followed by monitoring the incidence and severity of any adverse events (AEs). The pharmacokinetic parameters of anaprazole, its isomer, and main metabolisms were determined. The results showed that both single‐dose (2.5‐120 mg) and multiple‐dose (20 mg once daily, 40 mg once daily, or 20 mg twice daily) oral administration of anaprazole sodium enteric‐coated tablet were safe and well tolerated. Following single‐dose administration, the median time to reach maximum plasma concentration of anaprazole was between 3.50 and 5.25 hours, with mean elimination half‐life of 1.22‐3.79 hours. The absorption and elimination of anaprazole in the human body appeared to basically follow linear kinetics. After repeated dosing, steady‐state concentrations of anaprazole, its isomer, and primary metabolites were achieved, with a median time to reach maximum plasma concentration of 3‐3.75 hours and a mean elimination half‐life of 1.61‐2.27 hours for anaprazole. There was no significant drug accumulation after multiple‐dose oral administration. In conclusion, anaprazole sodium enteric‐coated tablets were found to be safe and well tolerated in healthy Chinese individuals. Anaprazole is absorbed and metabolized consistently in the human body without any accumulation.

01 Jul 2024·European Journal of Pharmaceutical Sciences

Integrated models of population pharmacokinetics and exposure response to optimize dosage regimen for anaprazole sodium in duodenal ulcer

Article

Author: Yao, Xueting ; Liu, Dongyang ; Zhang, Yi ; Cui, Cheng ; Zhang, Lei ; Wang, Chunyang ; Song, Ling

Anaprazole sodium enteric-coated tablet is a novel proton pump inhibitor which has been approved for the treatment of duodenal ulcer. The aim of this study is to provide reliable information for the design of an optimal dosage regimen. Population pharmacokinetics and exposure-response models were integrated to evaluate the pharmacokinetic parameters and covariates of Anaprazole and its metabolite M21-1, and subsequently provided dosage suggestions based on clinical trials and simulation data. A pharmacokinetic model incorporating two-compartment for the parent drug and one-compartment for the metabolite, with both first-order and zero-order mixed absorption was used to describe the pharmacokinetics of Anaprazole and M21-1. Age emerged as a significant covariate affecting the elimination rate constant of M21-1, with clearance decreasing as age advances. No correlation was observed between the pharmacokinetics of Anaprazole or M21-1 and the adverse reactions under the current dosages. BMI might be the influence factor of the mild gastrointestinal adverse reactions. Meanwhile, Anaprazole had a good healing rate (94.0 %) in duodenal ulcer patients and the exposure-response analysis indicated that the cured results were not influenced by the exposure parameters of parent drug or metabolite. In conclusion, the drug is safe when dosing between 20 and 100 mg once a day.

100 Deals associated with Anaprazole Sodium

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R&D Status

Approved

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Indication	Country/Location	Organization	Date
Duodenal Ulcer	China	Xuanzhu (Beijing) Pharmaceutical Technology Co., Ltd.	21 Jun 2023

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Esophagitis, Peptic	Phase 2	China	Xuanzhu (Beijing) Pharmaceutical Technology Co., Ltd.	06 Dec 2022
Gastroesophageal Reflux	Preclinical	China	Xuanzhu Biopharmaceutical Co., Ltd.	01 Dec 2022
Helicobacter pylori infection	Preclinical	China	Shandong Xuanzhu Pharmaceutical Technology Co., Ltd.	10 Aug 2020
Helicobacter pylori infection	Preclinical	China	Beijing Sihuan Pharmaceutical Co. Ltd.	10 Aug 2020
Duodenal Ulcer	Preclinical	China	Beijing Sihuan Pharmaceutical Co. Ltd.	20 Jan 2020
Stomach Ulcer	Preclinical	China	Shandong Xuanzhu Pharmaceutical Technology Co., Ltd.	14 Aug 2014

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Clinical Result

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT04215653 (Pubmed)	Phase 3	Duodenal Ulcer	448	Anaprazole 20 mg	iwwitjzjdy(zffidmhiio) = akkrfntpyr wksoxwebst (tuyyxuurnp )	Positive	30 Dec 2022
				Rabeprazole 10 mg	iwwitjzjdy(zffidmhiio) = fgnyyayodl wksoxwebst (tuyyxuurnp )
CTR20181464 \| NCT04503629 (Pubmed \| Front Med (Lausanne))	Phase 2	Duodenal Ulcer	150	Rabeprazole 10 mg	siijjrpkkv(avqexkokuk) = The incidence rates of adverse events were of no significant differences among the treatment groups hybahzjuju (mbonslvswd ) View more	Positive	01 Jan 2021
				Anaprazole 20 mg