A 4-week, Randomised, Double-blind, Multicentre, Dose-finding Phase IIb Study With AZD0865 25, 50, 75 mg and Esomeprazole 20 mg, Given Orally Once Daily for the Treatment of GERD Without Erosive Esophagitis According to the LA Classification in Adult Subjects.

The primary objective is to compare the efficacy between three doses of AZD0865 (25, 50 and 75 mg). The secondary objectives are to compare the efficacy between the three doses of AZD0865 and esomeprazole 20 mg and to evaluate the safety and tolerability of AZD0865.

Start Date01 May 2004

Sponsor / Collaborator

AstraZeneca PLC

NCT00206245

/ CompletedPhase 2

A Randomised, Double-blind, Multicentre Dose-finding Phase IIb Study for up to 8 Weeks' Treatment With AZD0865 25, 50, 75 mg and Esomeprazole 40 mg, Given Orally Once Daily for the Healing of Erosive Esophagitis in Adult Subjects With GERD With Erosive Esophagitis According to the LA Classification in Adult Subjects.

The primary objective is to compare the efficacy between three doses of AZD0865 (25, 50 and 75 mg).
The secondary objectives are to compare the efficacy between the three doses of AZD0865 and esomeprazole 40 mg and to evaluate the safety and tolerability of AZD0865.

Start Date01 May 2004

Sponsor / Collaborator

AstraZeneca PLC

100 Clinical Results associated with Linaprazan

100 Translational Medicine associated with Linaprazan

100 Patents (Medical) associated with Linaprazan

Literatures (Medical) associated with Linaprazan

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 ; Diao, Xingxing ; Yang, Ying ; 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.

10 Mar 2020·Asian Journal of Chemistry

Design, Synthesis and Pharmacological Evaluation of Novel Imidazopyridine Analogues as Proton Pump Antagonist

Author: Patil, Kiran D. ; Patil, Avinash V. ; Sonawane, Ravindra S.

A series of novel imidazopyridine derivatives as proton pump inhibitors was designed with compounds of CID data base and explored considering AZD0865 as standard. Many compounds were identified and docked in proton pump ATPase pocket (PDB ID: 4ux2). Molecular docking studies revealed that many compounds showed good proton pump ATPase inhibitory activity. The docking poses revealed the interaction of ligands with amino acid. The standard drug AZD0865 had docking score of -7.112302 and displayed interactions with Asn138 and Asp137. A series of novel imidazopyridine derivatives as proton pump inhibitors were docked, synthesized and characterized by IR, NMR, CHN and MS spectral analysis. The target imidazopyridines were prepared from substituted 2-aminonicotinic acid and 2-bromo-1-substituted ethanone. in vitro Studies explained that few compounds exhibited moderate to good proton pump ATPase inhibitory activity in comparison with the reference drugs i.e. AZD0865. Compounds 11 and 12 shown higher activities with the IC50 4.3. Compounds 1, 4, 6, 7, 8, 10 and 13 showed weak anti-ulcer activity with its IC50 5.2, 5.8, 5.5, 5.1, 4.9, 4.6 and 5.9 and positive control AZD0865 shown IC50 2.0.

01 Mar 2020·Journal of pharmaceutical sciences

Prediction Characteristics of Oral Absorption Simulation Software Evaluated Using Structurally Diverse Low-Solubility Drugs

Article

Author: Tamura, Naomi ; Yoneda, Kazuhiro ; Matsumura, Naoya ; Kimoto, Takahiro ; Fujita, Takuya ; Sarashina, Akiko ; Hayashi, Shun ; Nakanishi, Misato ; Kim, Soonih ; Akiyama, Yoshiyuki ; Fushimi, Masahiro ; Funaki, Satoko ; Kojima, Yukiko ; Ishida, Masahiro ; Haruna, Yuka ; Nishiyama, Kotaro ; Sugano, Kiyohiko ; Jiko, Maiko ; Ono, Asami

The purpose of the present study was to characterize current biopharmaceutics modeling and simulation software regarding the prediction of the fraction of a dose absorbed (Fa) in humans. As commercial software products, GastroPlus™ and Simcyp® were used. In addition, the gastrointestinal unified theoretical framework, a simple and publicly accessible model, was used as a benchmark. The Fa prediction characteristics for a total of 96 clinical Fa data of 27 model drugs were systematically evaluated using the default settings of each software product. The molecular weight, dissociation constant, octanol-water partition coefficient, solubility in biorelevant media, dose, and particle size of model drugs were used as input data. Although the same input parameters were used, GastroPlus™, Simcyp®, and the gastrointestinal unified theoretical framework showed different Fa prediction characteristics depending on the rate-limiting steps of oral drug absorption. The results of the present study would be of great help for the overall progression of physiologically based absorption models.

News (Medical) associated with Linaprazan

04 Dec 2024

·cincluspharma.com

Linaprazan glurate receives marketing approval in China

Cinclus Pharma, a clinical-stage pharmaceutical company developing molecules for the treatment of gastric acid-related diseases, today announced that its leading drug candidate, linaprazan glurate, has received its first marketing approval for the treatment of gastroesophageal reflux disease (GERD). The approval by the National Medical Products Administration (NMPA) paves the way for commercialization in the People’s Republic of China in 2025. The approved product was developed together with Cinclus Pharma’s partner Jiangsu Sinorda Biomedicine Co., Ltd, (“Sinorda”) in preclinical studies and independently developed in clinical phases in China by Sinorda. The approval of linaprazan glurate in China follows local clinical trials that demonstrated the drug's safety, efficacy, and ability to address a significant unmet need in GERD. Following the approval, pricing and reimbursement discussions will be initiated laying the foundation for expected product launch in China in 2025. “We are thrilled to announce this highly significant marketing approval for linaprazan glurate in China, a market that represents an immense opportunity for expanding access to this innovative treatment. This achievement clearly reflects the strength of our partner Sinorda, our science, and takes us one important step closer to delivering a therapy meeting an unmet need in a global patient population,” said Christer Ahlberg, CEO of Cinclus Pharma. Cinclus Pharma has a license agreement with Sinorda for the development and commercialization of linaprazan glurate in China and other selected regions of Asia. Sinorda sub-licensed the manufacturing and industrial sales rights for linaprazan glurate in China, Hong Kong, Macau and Taiwan to SPH Sine Pharmaceutical Laboratories Co., Ltd, a company within the Shanghai Pharmaceuticals group, one of China’s leading public pharmaceutical and healthcare companies. For additional information, please contact: Christer Ahlberg, CEO Phone: +46 70 675 33 30 e-mail: christer.ahlberg@cincluspharma.com Charlotte Stjerngren, IR Phone: +46 70 876 87 87 e-mail: charlotte.stjerngren@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. This information is information that Cinclus Pharma Holding AB (publ) is obliged to make public pursuant to the EU Market Abuse Regulation. The information was submitted for publication, through the agency of the contact persons set out above, at 2024-12-04 15:40 CET. Attachments Linaprazan glurate receives marketing approval in China

License out/inDrug ApprovalPhase 2Phase 3

22 Nov 2024

·cincluspharma.com

Cinclus Pharma agrees on pediatric study plan with FDA

Cinclus Pharma, a clinical-stage pharmaceutical company developing molecules for the treatment of acid-related diseases, today announces that it has reached an agreement with the US Food and Drug Administration (FDA) on the company’s initial Pediatric Study Plan (iPSP). The regulatory agreement on a pediatric study plan is a prerequisite for market approval of a new medicine for adult patients, such as linaprazan glurate. It also provides an opportunity for an expanded approval for use in children. "The agreement on our pediatric study plan with the FDA is a prerequisite for market approval in the US, so it’s really a milestone. Now that we have agreed with both the EMA and the FDA, we have taken an important step towards making linaprazan glurate available to patients, thereby fulfilling a large unmet need. Furthermore, an approved pediatric indication would significantly increase the target population for linaprazan glurate,” said Christer Ahlberg, CEO of Cinclus Pharma. The company’s agreed iPSP mainly includes a clinical efficacy and safety trial where approximately 100 pediatric patients will be treated with linaprazan glurate on the same treatment schedule as in the company’s phase III trials in adult eGERD patients. The study plan is essentially the same as Cinclus Pharma recently agreed with the European Medicines Agency (EMAs) Pediatric Committee (PDCO). A regulatory agreement of a pediatric study plan must be obtained before a sponsor may submit a Marketing Authorization Application for approval to commercialize a new medicine for adult patients. Cinclus Pharma submitted its proposed iPSP to FDA in December 2023 and has been going through the regulatory review processes since then. The company’s agreed iPSP includes a deferral under which the pediatric efficacy and safety trial is anticipated to be undertaken after a Marketing Authorization Application has been submitted. For additional information, please contact: Christer Ahlberg, CEO Phone: +46 70 675 33 30 e-mail: christer.ahlberg@cincluspharma.com Charlotte Stjerngren, IR Phone: +46 70 876 87 87 e-mail: charlotte.stjerngren@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 Cinclus Pharma agrees on pediatric study plan with FDA

Phase 2Phase 3

29 Oct 2024

·cincluspharma.com

Cinclus Pharma agrees on Pediatric Investigation Plan (PIP) with EMA

Cinclus Pharma, a clinical-stage pharmaceutical company developing molecules for the treatment of acid-related diseases, today announces that it has reached an agreement with the European Medicines Agency’s (EMA) Paediatric Commmittee (PDCO) on the company’s Pediatric Investigation Plan (PIP). The regulatory agreement on a pediatric study plan is a pre-requisite for marketing approval of a new medicine for adult patients, such as linaprazan glurate. It also provides an opportunity for an expanded approval for use in children. "It is incredibly satisfying that our pediatric study plan has been agreed. It is a prerequisite for market approval in the EU, so it’s really a milestone. In addition, an approved pediatric indication would of course also significantly increase our target population,” said Christer Ahlberg, CEO of Cinclus Pharma. The company’s agreed PIP mainly includes a clinical efficacy and safety trial where approximately 100 pediatric patients will be treated with linaprazan glurate on the same treatment schedule as in the company’s phase III trials in adult eGERD patients. When a new medicine is developed for adult patients, that medicine must also be tested for potential application to pediatric patients. The sponsor must develop an overall plan to select the specific form or stage of the disease to be treated, to adapt the dosing and administration of the medicine for pediatric physiology, and to evaluate the safety and efficacy of the medicine in pediatric patients. A regulatory agreement of a pediatric study plan must be obtained before a sponsor may submit a Marketing Authorization Application for approval to commercialize a new medicine for adult patients. Cinclus Pharma submitted its proposed PIP to EMA in December 2023 and has been going through the regulatory review processes since then. The company’s agreed PIP includes a deferral under which the pediatric efficacy and safety trial is anticipated to be undertaken after a Marketing Authorization Application has been submitted. For additional information, please contact: Christer Ahlberg, CEO Phone: +46 70 675 33 30 e-mail: christer.ahlberg@cincluspharma.com Charlotte Stjerngren, IR Phone: +46 70 876 87 87 e-mail: charlotte.stjerngren@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 Cinclus Pharma agrees on Pediatric Investigation Plan (PIP) with EMA

Phase 3Phase 2

100 Deals associated with Linaprazan

R&D Status

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Indication	Highest Phase	Country/Location	Organization	Date
Erosive esophagitis	Phase 2	United States	AstraZeneca PLC	01 May 2004
Erosive esophagitis	Phase 2	Canada	AstraZeneca PLC	01 May 2004
Erosive esophagitis	Phase 2	Denmark	AstraZeneca PLC	01 May 2004
Erosive esophagitis	Phase 2	Finland	AstraZeneca PLC	01 May 2004
Erosive esophagitis	Phase 2	France	AstraZeneca PLC	01 May 2004
Erosive esophagitis	Phase 2	Germany	AstraZeneca PLC	01 May 2004
Erosive esophagitis	Phase 2	Italy	AstraZeneca PLC	01 May 2004
Erosive esophagitis	Phase 2	Norway	AstraZeneca PLC	01 May 2004
Erosive esophagitis	Phase 2	Sweden	AstraZeneca PLC	01 May 2004
Erosive esophagitis	Phase 2	United Kingdom	AstraZeneca PLC	01 May 2004

Clinical Result

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


UEGW2023	Not Applicable	Erosive esophagitis	-	Linaprazan glurate 25 mg	fcqwhcvila(rnssuoyhhl) = 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. llykjlcmry (bclhuqwrlt )	-	15 Oct 2023
				Linaprazan glurate 50 mg

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