Delving into the Latest Updates on Linaprazan glurate with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

+ [1]

Target

H+/K+ ATPase

Mechanism

P-CAB(Potassium-competitive acid blockers)

Therapeutic Areas

Digestive System DisordersMouth and Tooth DiseasesOtorhinolaryngologic Diseases+ [1]

Active Indication

Esophagitis, PepticGastroesophageal RefluxDuodenal Ulcer+ [1]

Inactive Indication

Stomach Ulcer

Originator Organization

Cinclus Pharma AGStartup

Active Organization

Sinorda Biomedicine Co., Ltd.Shanghai Sinorda Pharmaceutical Technology Co., Ltd.

Shanghai Pharmaceuticals Holding Co., Ltd.

+ [1]

Inactive Organization

Cinclus Pharma AGStartupAnhui Shengnuo Pharmaceutical Co. Ltd.

Drug Highest PhaseNDA/BLA

First Approval Date-

RegulationSpecial Review Project (CN)

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Structure

Molecular FormulaC26H32N4O5

InChIKeyGPHPBXRKAJSSIC-UHFFFAOYSA-N

CAS Registry1228559-81-6

主要研究目的：1. 定量分析男性健康受试者口服[14C]X842后，排泄物中的总放射性，获得人体放射性的累计排泄率和主要排泄途径；2. 考察男性健康受试者单次口服[14C]X842后，全血和血浆中的分配情况和血浆中总放射性的药代动力学；3. 鉴定男性健康受试者口服[14C]X842后人体内的主要代谢产物，确定主要生物转化途径和主要代谢产物（接近或大于10%总放射性AUC）；4. 采用已验证的LC-MS/MS方法定量分析血浆中X842、linaprazan及其他主要代谢产物（如适用）的浓度，获得血浆中X842、linaprazan及其他主要代谢产物（如适用）的药代动力学参数。次要研究目的：观察[14C]X842单次给药后男性健康受试者的安全性。

[Translation]

The main study objectives are as follows: 1. To quantitatively analyze the total radioactivity in the excreta after oral administration of [14C]X842 to healthy male subjects, and to obtain the cumulative excretion rate and main excretion pathway of radioactivity in the human body; 2. To investigate the distribution of [14C]X842 in whole blood and plasma and the pharmacokinetics of total radioactivity in plasma after a single oral administration of [14C]X842 to healthy male subjects; 3. To identify the main metabolites in the human body after oral administration of [14C]X842 to healthy male subjects, and to determine the main biotransformation pathways and main metabolites (close to or greater than 10% of the total radioactivity AUC); 4. To quantitatively analyze the concentrations of X842, linaprazan and other major metabolites (if applicable) in plasma using a validated LC-MS/MS method, and to obtain the pharmacokinetic parameters of X842, linaprazan and other major metabolites (if applicable) in plasma. Secondary study objectives: To observe the safety of [14C]X842 in healthy male subjects after a single administration.

Start Date15 Jun 2022

Sponsor / Collaborator

Sinorda Biomedicine Co., Ltd.

NCT05055128 / CompletedPhase 2

A Randomized Double-blind, Double Dummy, Active Comparator-controlled Dose-finding Study in Patients With Erosive Esophagitis Due to Gastro-esophageal Reflux Disease (GERD) Los Angeles Grade C or D, and Patients With at Least Partial Symptom Response But Endoscopically Still Unhealed After 8 Weeks History of Standard Treatment Healing Course With Proton-pump Inhibitor (PPI), to Investigate Safety, Tolerability, and Healing Rates After 4 Weeks Treatment of X842 or Lansoprazole, and Symptom Pattern During Subsequent 4 Weeks Treatment With Lansoprazole

This study will be conducted in patients with erosive esophagitis due to gastro-esophageal reflux disease (GERD) Los Angeles (LA) grades C or D, and in patients with at least partial symptom response but still endoscopically unhealed (LA grades A or B) after 8 weeks history of standard treatment healing course with PPI, designed to support dose selection for Phase 3 and to investigate safety, tolerability, and healing rates after 4 weeks treatment of X842 or Lansoprazole, and symptom pattern during subsequent 4 weeks treatment with Lansoprazole.

Start Date11 Aug 2021

Sponsor / Collaborator

Cinclus Pharma AGStartup

[+1]

CTR20210736 / CompletedPhase 3

多中心、随机、双盲双模拟、阳性药平行对照的Ⅲ期临床研究评价X842胶囊用于反流性食管炎患者的有效性和安全性

[Translation] A multicenter, randomized, double-blind, double-dummy, positive drug parallel controlled phase III clinical study to evaluate the efficacy and safety of X842 capsules in patients with reflux esophagitis

主要目的：与兰索拉唑肠溶胶囊相比，评价X842胶囊用于反流性食管炎患者的有效性。次要目的：与兰索拉唑肠溶胶囊相比，评价X842胶囊用于反流性食管炎患者的安全性；观察X842胶囊在反流性食管炎患者中的群体药代动力学特征。

[Translation]

Primary objective: To evaluate the effectiveness of X842 capsules in patients with reflux esophagitis compared with lansoprazole enteric-coated capsules. Secondary objective: To evaluate the safety of X842 capsules in patients with reflux esophagitis compared with lansoprazole enteric-coated capsules; to observe the population pharmacokinetic characteristics of X842 capsules in patients with reflux esophagitis.

Start Date24 Jun 2021

Sponsor / Collaborator

Sinorda Biomedicine Co., Ltd.

100 Clinical Results associated with Linaprazan glurate

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100 Translational Medicine associated with Linaprazan glurate

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100 Patents (Medical) associated with Linaprazan glurate

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1

Literatures (Medical) associated with Linaprazan glurate

01 Feb 2023·Archives of Microbiology

Formulation-based antagonistic endophyte Amycolatopsis sp. SND-1 triggers defense response in Vigna radiata (L.) R. Wilczek. (Mung bean) against Cercospora leaf spot disease

Article

Author: Kumar, Raju Suresh ; Basavarajappa, Dhanyakumara Shivapoojar ; Nayaka, Sreenivasa

In the present work, Amycolatopsis sp. SND-1 (SND-1) was isolated from Cleome chellidonii Linn. (C. chellidonii) was performed as biocontrol and resistance elicitor in Vigna radiata (L.) R. Wilczek (mung bean) plants against Cercospora leaf spot causing pathogen Cercospora canescens (C. canescens). The SND-1 isolate showed 74% of inhibition against C. canescens in dual culture and GC-MS analysis revealed the presence of antifungal compounds. Molecular characterization through 16S rRNA showed that the isolated SND-1 belongs to Amycolatopsis sp. The in vitro plant growth trials exhibited production of indole acetic acid, gibberellic acid, cytokinin, ammonia, hydrogen cyanide, and siderophore and phosphate solubilization. In vivo study with talcum formulation of SND-1 revealed a significant increase in plant root length, shoots length, root and shoot fresh weight, and reduced the disease severity in treated mung bean plants. Triggering of resistance by SND-1 formulation was studied by histochemical depositions and biochemical defense enzymes that resulted in the acceleration in defense response in comparison with control plants. The bioactive endophytic Amycolatopsis sp. SND-1 enhanced the defense against C. canescens infection; hence, it can be used as a biological control agent in mung bean cultivars.

1

News (Medical) associated with Linaprazan glurate

22 Aug 2023

·www.prnewswire.com

Sanyou Biopharmaceuticals and Sinorda Biomedicine signed Strategic Cooperation Agreement for Advancing Innovative Drug Research and Development

SHANGHAI, Aug. 22, 2023 /PRNewswire/ -- Sanyou Biopharmaceuticals (Shanghai) Co., Ltd. (referred to as "Sanyou" hereafter) and Sinorda Biomedicine (referred to as " Sinorda " hereafter) have officially signed a strategic cooperation agreement to advance the innovative bispecific antibody drug project. According to the cooperation agreement, leveraging Sanyou's world-leading core technology platform for integrated R&D and preclinical development of innovative biological drugs, along with a world-class "super-trillion innovative biologics discovery platform", a strong collaboration will be formed with Sinorda's rich experience in preclinical and clinical oncology immunotherapy. This collaboration aims to jointly advance the R&D of the product pipeline through cooperative efforts. Pingsheng Hu, CEO of Sinorda, stated, "Sinorda focuses on the research and development of innovative drug and industrialization of oncology immunotherapy. Our partnership with Sanyou merges our strengths, accelerating the drug development process and transforming innovative achievements into reality faster. This collaboration improves treatment choices for patients. With this shared vision, we can work together to advance innovative drug products and contribute to human health." Guojun Lang, CEO of Sanyou, commented, "We're truely honored to establish a strategic cooperation with Sinorda. Their strong scientific and medical expertise, robust clinical capabilities, and extensive experience in industrial collaboration perfectly align with Sanyou. Both Sanyou and Sinorda share the common goal of using biopharmaceutical technology to enhance human health. Our combined strengths and robust collaboration will open new opportunities and forge a pioneering model of cooperation between innovative drug research and development services and pharmaceutical enterprises. Together, we are committed to delivering positive outcomes for patients worldwide." About Sinorda Sinorda Biopharmaceuticals was founded in 2014 and focuses on the innovative drug development for gastrointestinal diseases and the industrialization of oncology immunotherapy. The company possesses comprehensive capabilities in innovative biopharmaceutical research and development, an experienced team in both technology and management, as well as international experience in innovative drug development and collaborations in China, the United States, and Europe, ensuring rapid project initiation and progress. The company has established extensive partnerships with renowned pharmaceutical enterprises, research institutions, CROs, CMOs, and government departments both domestically and internationally. This has led to the creation of a new drug development system characterized by resource sharing, synergistic advantages, and high competitiveness. Sinorda boasts a pipeline of several innovative drug candidates in clinical stages. Sinorda has three innovative drug candidates in clinical stages, including a Class 1 new drug, the potassium-competitive acid blocker X842 (NDA application accepted), the sentinel lymph node T-cell anti-tumor drug SLN-T (Phase II European clinical trial approval obtained), and the RIGVIR oncolytic virus drug (IND registration in progress). About Sanyou Sanyou Biopharmaceuticals Co., Ltd. is a world-leading high-tech biotechnology enterprise focusing on R&D and services of innovative biological drugs. Sanyou is committed to bridge drug R&D and all-life-cycle manufacture supply chain, and has built the 4C business patterns that integrate "differentiated CRO, integrated CDO, innovative CPO and characteristic CRS", to accomplish the mission "to make it easy to discover innovative biological drugs anywhere". Sanyou has established an integrated innovative biological drug R&D laboratory of twenty thousand square meters with advanced facilities, and has built three industry-leading innovative technology platforms featured by "super-trillion, integration, and intelligence" , which are comprised of more than 50 sub-platforms with the core innovative super-trillion phage display platform, and supported by platforms of material preparation, antibody discovery, molecule optimization, in vitro and in vivo efficacy, production cell line construction, upstream and downstream process development, preclinical R&D, industrialization development, etc.. Sanyou's proprietary platform and technology are in continuous optimisation，we launch from time to time upgrades and new version of services and technologies based on principles of innovation, outstanding and reliability. The company has established friendly business collaboration with more than 1000 pharmaceutical companies, drug R&D institutions and diagnostics companies worldwide. SOURCE Sanyoubio

ImmunotherapyPhase 2IND

100 Deals associated with Linaprazan glurate

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Esophagitis, Peptic	NDA/BLA	CN	Shanghai Sinorda Pharmaceutical Technology Co., Ltd.	10 Feb 2023
Esophagitis, Peptic	NDA/BLA	CN	STA Pharmaceutical Co. Ltd.	10 Feb 2023
Gastroesophageal Reflux	Phase 3	CN	Sinorda Biomedicine Co., Ltd.	30 Jan 2022
Duodenal Ulcer	Phase 2	CN	Sinorda Biomedicine Co., Ltd.	-
Helicobacter pylori infection	Phase 2	CN	Sinorda Biomedicine Co., Ltd.	-
Stomach Ulcer	Phase 1	CN	Sinorda Biomedicine Co., Ltd.	23 Oct 2018
Esophagitis	Phase 1	SE	Cinclus Pharma AGStartup	-

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT05055128 (CTgov)	Phase 2	Erosive esophagitis \| Gastroesophageal Reflux	248	Lansoprazole+X842 Dummy (X842 25 mg BID)	jbjceljzwe(ioiqyfjyzz) = swcrsahxsd qnagbgvgls (uvhkdgsgla, mqmvxbjrbl - mkyoihkekw) View more	-	01 Nov 2023
				Lansoprazole+X842 Dummy (X842 50 mg BID)	jbjceljzwe(ioiqyfjyzz) = vviqobvpbi qnagbgvgls (uvhkdgsgla, ldmsshywuw - kacggrhsla) View more
UEGW	Not Applicable	Erosive esophagitis	-	Linaprazan glurate 25 mg	auwstebzjd(euhzdnvryq) = In the double-blind period (Week 1-4), treatment-emergent adverse events (TEAEs) were reported by 18.2% of patients treated with LG (all 4 doses), and by 18.0% of patients treated with LAN. 2 patients (0.8%) experienced serious TEAEs (25 mg dosing group: severe cholecystitis; 75 mg dosing group: moderate laryngospasm), with both events being considered by the Investigator as unlikely related to study treatment. 8 patients (3.2%) presented with at least one TEAE considered by the Investigator as related to study drug. Treatment was discontinued in 5 patients (2.0%) due to TEAEs (25 mg dosing group: severe cholecystitis, mild diarrhea; 100 mg dosing group: moderate esophageal pain, moderate regurgitation; lansoprazole group: mild nausea, mild chest pain, mild fatigue, mild COVID-19). For the entire study period (Week 1-8), TEAEs were reported by 23.0% of patients. The most commonly reported TEAEs are presented in Table 1. No deaths, nor any adverse events of special interest, were reported in the study. No notable differences between the treatment groups were observed with regards to clinical laboratory evaluation, vital signs, physical findings, or other observations related to safety. xkzxuxonqn (lnkfbpwlyu )	-	15 Oct 2023
				Linaprazan glurate 50 mg