Ph 1, OL, Randomized, Parallel-group Study to Investigate PK and PD (Intragastric pH) of Linaprazan Glurate/Linaprazan After 14 Days Administration of Linaprazan Glurate to Healthy Subjects

This is a Phase I, single-center, open label parallel-group, randomized study designed to evaluate the pharmacokinetics (PK), pharmacodynamics (PD), safety and tolerability of single and repeated oral doses of Linaprazan Glurate for up to 14 days at 3 dose levels in healthy male and female subjects.
The subjects will be followed up to 28 days post IMP dosing.

Start Date26 Jan 2023

Sponsor / Collaborator

Cinclus Pharma Holding AB

NCT05633147

/ CompletedPhase 1

Effect of Repeated Dosing of Clarithromycin on PK of Linaprazan Glurate/Linaprazan, Effect of Single Dose of Linaprazan Glurate on PK of Clarithromycin, Single/Repeated Dosing of Linaprazan Glurate on PK of Midazolam to Healthy Subjects

This is a phase I, open-label, fixed sequence design, drug-drug-interaction (DDI) study divided in 2 parts. Part I is designed to evaluate whether concomitant treatment with linaprazan glurate and clarithromycin, a strong inhibitor of cytochrome P450 3A4 (CYP3A4) and P-glycoprotein P (PgP), leads to an effect on the systemic exposure to linaprazan glurate and linaprazan and whether there is an effect on the pharmacokinetics of clarithromycin after a single dose of linaprazan glurate. Part II is designed to evaluate the effect of repeated doses of linaprazan glurate on the pharmacokinetics (PK) of a sensitive substrate of CYP3A (midazolam).

Start Date27 Nov 2022

Sponsor / Collaborator

Cinclus Pharma Holding AB

NCT05627518

/ CompletedPhase 1

A Randomized, Single Dose, Crossover Study in Healthy Volunteers to Investigate the Relative Bioavailability of Linaprazan for a New Oral Tablet Formulation of Linaprazan Glurate, and to Assess the Effect of Food on the Pharmacokinetics of Linaprazan

This is a single-center, open-label, randomized, single dose, 3-way crossover study in healthy volunteers designed to evaluate the relative bioavailability of a new oral tablet formulation of linaprazan glurate in comparison to a previously studied oral tablet formulation under fasting conditions, and to assess the effect of a high fat, high calorie meal on the pharmacokinetics (PK) of linaprazan glurate and the active substance linaprazan after the administration of the new oral tablet formulation.

Start Date15 Nov 2022

Sponsor / Collaborator

Cinclus Pharma Holding AB

100 Clinical Results associated with Linaprazan glurate

100 Translational Medicine associated with Linaprazan glurate

100 Patents (Medical) associated with Linaprazan glurate

Literatures (Medical) associated with Linaprazan glurate

01 Nov 2024·Current gastroenterology reports

Potassium-competitive Acid Blockers: Current Clinical Use and Future Developments

Review

Author: Scarpignato, Carmelo ; Hunt, Richard H

Abstract:

Purpose of the Review:

Acid suppression with proton pump inhibitors (PPIs) represents the standard of care in the treatment of acid-related diseases. However, despite their effectiveness, PPIs display some intrinsic limitations, which underlie the unmet clinical needs that have been identified over the past decades. The aims of this review are to summarize the current status and future development of the new class of antisecretory drugs (potassium-competitive acid blockers, P-CABs) that have recently been introduced into medical practice.

Recent Findings:

Over the past decades, clinical needs unmet by the current acid suppressants have been recognized, especially in the management of patients with GERD, Helicobacter pylori infection and NSAID-related peptic ulcer. The failure to address these needs is mainly due to their inability to achieve a consistent acid suppression in all patients and, particularly, to control nighttime acidity. It was then realized that an extended duration of acid suppression would exert additional benefits. The available data with P-CABs show that they are able to address these unmet clinical needs.

Summary:

Four different P-CABs (vonoprazan, tegoprazan, fexuprazan and keverprazan) are currently available. However, only two of them are approved outside Asia. Vonoprazan is available in North, Central and South America while tegoprazan is marketed only in Latin American countries. Two other compounds (namely linazapran glurate and zestaprazan) are presently under clinical development. While clinical trials on GERD have been performed with all P-CABs, only vonoprazan and tegoprazan have been investigated as components of Helicobacter pylori eradication regimens. The available data show that—in the above two clinical indications—P-CABs provide similar or better efficacy in comparison with PPIs. Their safety in the short-term overlaps that of PPIs, but data from long-term treatment are needed.

01 May 2024·Journal of pharmaceutical and biomedical analysis

Absorption, distribution, metabolism and excretion of linaprazan glurate in rats

Article

Author: Zhang, Xinyue ; Zheng, Yuandong ; Yuan, Yali ; Yang, Ying ; Diao, Xingxing ; Yang, Chen ; Xiu, Jin ; Lu, Ming ; Liu, Donghui ; Hu, Pingsheng

Linaprazan (AZD0865, TX07) is one of potassium-competitive acid blockers. However, linaprazan is rapidly excreted from the body, shortening its acid inhibition property. Linaprazan glurate (X842) is a prodrug of linaprazan with a prolonged inhibitory effect on gastric acid secretion. Linaprazan glurate has entered clinical trials, but few studies have reported its metabolism in non-clinical and clinical settings. In this study, we studied the pharmacokinetics, tissue distribution, mass balance, and metabolism of linaprazan glurate in rats after a single oral dose of 2.4 mg/kg (100 µCi/kg) [¹⁴C]linaprazan glurate. The results demonstrated that linaprazan glurate was mainly excreted via feces in rats with 70.48% of the dose over 168 h. The plasma AUC₀_-_∞ of linaprazan glurate in female rats was 2 times higher than that in male rats. Drug-related substances were mainly concentrated in the stomach, eyes, liver, small intestine, and large intestine after administration. In blood, drug-related substances were mostly distributed into plasma instead of hemocytes. In total, 13 metabolites were detected in rat plasma, urine, feces, and bile. M150 (2,6-dimethylbenzoic acid) was the predominant metabolite in plasma, accounting for 80.65% and 67.65% of AUC_0-24_h in male and female rats, respectively. Based on the structures, linaprazan glurate was mainly hydrolyzed into linaprazan, followed by a series of oxidation, dehydrogenation, and glucuronidation in rats. Besides, CES2 is the main metabolic enzyme involved in the hydrolysis of linaprazan glurate to linaprazan.

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 ; Nayaka, Sreenivasa ; Basavarajappa, Dhanyakumara Shivapoojar

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.

News (Medical) associated with Linaprazan glurate

07 Apr 2025

·cincluspharma.com

New scientific article highlights good healing results for Cinclus Pharma's drug candidate linaprazan glurate for the treatment of eGERD

Cinclus Pharma AB (publ), a developer of drugs for the treatment of gastric acid-related diseases, announced today that a scientific article has been published with data from a phase II study showing high healing rates for patients with severe forms of erosive gastroesophageal reflux disease, eGERD. The results support the continued development of linaprazan glurate as a next-generation drug for gastric acid-related diseases. The article, titled Randomised Controlled Trial: A Dose-Finding Study of Linaprazan glurate, A Novel Potassium Competitive Acid Blocker, vs. Lansoprazole for the Treatment of Erosive Esophagitis, has been published online in the scientific journal Alimentary Pharmacology & Therapeutics and is written by Prateek Sharma, Michael Vaezi, Peter Unge, Kjell Andersson, Kajsa Larsson, Ivan Popadiyn, Maria Rosenholm, Andras Rosztóczy, Elham Yektaei and David Armstrong. The published article presents data from a phase II clinical trial in which the treatment with linaprazan glurate (the next generation of PCAB) showed a high healing rate among patients suffering from eGERD. For patients who were not healed after eight weeks of treatment with proton pump inhibitor, the best-performing dose of linaprazan glurate achieved a 100 percent healing rate after four weeks, a higher rate of 28 percentage points compared to the treatment with the proton pump inhibitor lansoprazole. The healing rate for patients with moderate to severe eGERD was 93 percent, which was 50 percentage points higher than the treatment with lansoprazole. The results support the continued development of linaprazan glurate as a next-generation drug for gastric acid-related diseases. "The study shows very good healing rates, both for patients previously treated with PPI without being healed and for patients with severe eGERD, which highlights the potential of our drug candidate. We look forward to initiating the phase III program of linaprazan glurate during 2025”, says Kajsa Larsson, Chief Medical Officer at Cinclus Pharma. "The results show how effective treatment with linaprazan glurate is compared to today's standard treatment, and in extension also the first generation of PCAB. Cinclus Pharma's drug meets the medical need of the patients who suffer the most with the severe forms of eGERD, which constitutes a large market with blockbuster potential," said Christer Ahlberg, CEO of Cinclus Pharma. To access the article, please click the following link: http://doi.org/10.1111/apt.70109 For additional information, please contact: Christer Ahlberg, CEO Phone: +46 70 675 33 30 e-mail: christer.ahlberg@cincluspharma.com Henrik Vikström, IR Phone: +46 70 952 80 06 e-mail: henrik.vikström@cincluspharma.com About Cinclus Pharma Cinclus Pharma Holding AB (publ) is a late-stage clinical pharmaceutical company developing drugs for the treatment of acid-related diseases and disorders of the upper gastrointestinal tract. The company's leading drug candidate is linaprazan glurate, a prodrug of P-CAB linaprazan, which was originally developed by AstraZeneca. Linaprazan glurate has the potential to heal erosions in the esophageal mucosa and relieve symptoms of gastroesophageal reflux disease (GERD) more effectively than current treatments like proton pump inhibitors (PPI). The safety and efficacy of linaprazan and linaprazan glurate have been documented in over 30 phase I and two phase II studies involving more than 3,000 participants. Planning for phase III studies is currently underway, with an expected start in 2025. GERD affects approximately 133 million adults in the US and EU, and there is a significant need for new drugs to treat the most severe cases: around 10 million patients. Linaprazan glurate is developed to meet these needs. For more information, visit www.cincluspharma.com. Attachments New scientific article highlights good healing results for Cinclus Pharma's drug candidate linaprazan glurate for the treatment of eGERD

Phase 2Clinical ResultPhase 3

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

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Esophagitis, Peptic	China	Shanghai Sinorda Pharmaceutical Technology Co., Ltd.	01 Dec 2024

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Erosive esophagitis	Phase 2	United States	Cinclus Pharma AGStartup	11 Aug 2021
Erosive esophagitis	Phase 2	Bulgaria	Cinclus Pharma AGStartup	11 Aug 2021
Erosive esophagitis	Phase 2	Czechia	Cinclus Pharma AGStartup	11 Aug 2021
Erosive esophagitis	Phase 2	Georgia	Cinclus Pharma AGStartup	11 Aug 2021
Erosive esophagitis	Phase 2	Hungary	Cinclus Pharma AGStartup	11 Aug 2021
Erosive esophagitis	Phase 2	Poland	Cinclus Pharma AGStartup	11 Aug 2021
Erosive esophagitis	Phase 2	Serbia	Cinclus Pharma AGStartup	11 Aug 2021
Erosive esophagitis	Phase 2	Ukraine	Cinclus Pharma AGStartup	11 Aug 2021
Gastroesophageal Reflux	Phase 2	European Union	Cinclus Pharma AGStartup	22 Jan 2020
Duodenal Ulcer	Phase 2	China	Sinorda Biomedicine Co., Ltd.	-

Clinical Result

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Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT05055128 (Pubmed \| Aliment Pharmacol Ther) Manual	Phase 2	Erosive esophagitis	248	Linaprazan Glurate	gluupvltyq(ujdwdzzjzr) = orfgchlnzk zreolxczma (foglgdkzkp ) View more	Positive	04 Apr 2025
				Lansoprazole	gluupvltyq(ujdwdzzjzr) = uyksbymafn zreolxczma (foglgdkzkp ) View more
NCT04531475 (Phase 2 study, Pubmed \| Clin Transl Gastroenterol)	Phase 2	Erosive esophagitis	90	X842 50 mg	jbnrbynlqt(cctnycbhli) = The incidence of drug-related treatment-emergent adverse events did not differ among groups fgmhxjtqyl (nwlqpbrbug ) View more	Positive	21 Jan 2025
				X842 100 mg
NCT05633147 (CTgov)	Phase 1	Medication interactions	35	Linaprazan glurate+Clarithromycin (Part I)	cemuumjqum(utmbilcdfo) = hgyqbngwyc ulolfqumoc (peubruyktf, 5649) View more	-	03 Jan 2025
				Midazolam+Linaprazan glurate hydrochloride (HCl) (Part II)	fuojavyicv(fvbmdkdioi) = pfbdvuqalf jnrpztggro (cgpiycgstm, 13.98) View more
DDW2024	Not Applicable	-	-	Vonoprazan-based triple therapy	zpludcdwgp(odukknonwx): RR = 1.17 (95% CI, 1.11 - 1.22)	-	18 May 2024
				Conventional PPI-based triple therapy
NCT05055128 (CTgov)	Phase 2	Erosive esophagitis \| Gastroesophageal Reflux	248	Lansoprazole+X842 Dummy (X842 25 mg BID)	dlxvpkxdbf = tiwjqakims irufqijghr (bdjacckmyw, pqsqnhybyp - kclbjaujtj) View more	-	01 Nov 2023
				Lansoprazole+X842 Dummy (X842 50 mg BID)	dlxvpkxdbf = vwtukmkhtb irufqijghr (bdjacckmyw, cenlibbyvw - bvsprpulqw) View more

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