Delving into the Latest Updates on S-Tenatoprazole with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Benatoprazole, S-Tenatoprazole-Na, STU-Na

+ [3]

Target

Proton pump

Action

inhibitors

Mechanism

Proton pump inhibitors

Therapeutic Areas

Digestive System DisordersMouth and Tooth DiseasesOtorhinolaryngologic Diseases

Active Indication-

Inactive Indication

Duodenal UlcerErosive esophagitisEsophagitis+ [3]

Originator Organization

Mitsubishi Tanabe Pharma Corp.

Active Organization-

Inactive Organization

Steba France SASU

Mitsubishi Tanabe Pharma Corp.

Abbott Laboratories

License Organization-

Drug Highest PhaseSuspendedNDA/BLA

First Approval Date-

Regulation-

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Structure/Sequence

Molecular FormulaC16H18N4O3S

InChIKeyZBFDAUIVDSSISP-UHFFFAOYSA-N

CAS Registry113712-98-4

S-Tenatoprazole-Na (STU-Na), a new drug currently under clinical development, belongs to a class of drugs, called proton pump inhibitors (PPls). Some PPIs are already commercially available. STU-Na will be used for treatment of acid related diseases (gastroduodenal ulcers, erosive or ulcerative esophagitis due to gastroesophageal reflux disease). This study evaluates the degree of acid suppression by different doses of STU-Na. The degree of acid suppression is considered to be correlated with clinical efficacy.
In this study four dosages of STU-Na (30 mg, 60 mg, 90 mg, and 120 mg) will be tested in each volunteer. First, one of the dosages will be orally administered for five days. Then, a nine to sixteen day period without study drug administration will follow prior to the administration of the next dosage, for again five days. Each volunteer will have a total of four study drug administration periods.
After the last study drug intake in period 1, 2 and 3 pharmacokinetic blood sampling will be done for four days. After the last study drug intake in period 4 pharmacokinetic blood sampling will be done for five days. Pharmacokinetic blood sampling consists of several blood draws over a pre-determined time period. The pharmacokinetic blood sampling measures the medication concentration in the blood at pre-defined time points.
After the last study drug intake in period 1, 2, 3, and 4, gastric acidity will be measured for 24 hours by means of a thin tube that will be inserted into the stomach through the nostril to evaluate the efficacy of the different dosages of STU-Na.

Start Date01 Sep 2006

Sponsor / Collaborator

Steba France SASU

[+1]

100 Clinical Results associated with S-Tenatoprazole

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100 Translational Medicine associated with S-Tenatoprazole

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100 Patents (Medical) associated with S-Tenatoprazole

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138

Literatures (Medical) associated with S-Tenatoprazole

01 Sep 2024·DRUG RESISTANCE UPDATES

Lansoprazole (LPZ) reverses multidrug resistance (MDR) in cancer through impeding ATP-binding cassette (ABC) transporter-mediated chemotherapeutic drug efflux and lysosomal sequestration

Article

Author: Wang, Peiyu ; Wang, Ran ; Li, Hui ; Ji, Ning ; Chen, Xin ; Chen, Zhe-Sheng ; Yang, Yuqi ; Liu, Yi-Nan ; Wang, Jing-Quan ; Li, Yuelin ; Kong, Dexin ; Li, Yueguo ; Zhang, Yixuan

AIMS:

Lansoprazole is one of the many proton pump inhibitors (PPIs) that acts more strongly with ABCB1 and ABCG2. The present study is to investigate the potential of lansoprazole on reversal of ABCB1/G2-mediated MDR in cancer, in vitro and in vivo.

METHODS:

Reversal studies and combination evaluation were conducted to determine the synergistic anti-MDR effects on lansoprazole. Lysosomal staining was used to determination of lansoprazole on ABCB1-mediated lysosomal sequestration. Substrate accumulation and efflux assays, ATPase activity, and molecular docking were conducted to evaluate lansoprazole on ABCB1/G2 functions. Western blot and immunofluorescence were used to detect lansoprazole on ABCB1/G2 expression and subcellular localization. MDR nude mice models were established to evaluate the effects of lansoprazole on MDR in vivo.

RESULTS:

Lansoprazole attenuated ABCB1/G2-mediated MDR and exhibited synergistic effects with substrate drugs in MDR cells. In vivo experiments demonstrated that lansoprazole attenuated ABCB1/G2-mediated MDR and exhibited synergistic effects that augmented the sensitivity of substrate anticancer drugs in ABCB1/G2-mediated settings without obvious toxicity. Lansoprazole impeded lysosomal sequestration mediated by ABCB1, leading to a substantial increase in intracellular accumulation of substrate drugs. The effects of lansoprazole were not attributable to downregulation or alterations in subcellular localization of ABCB1/G2. Lansoprazole promoted the ATPase activity of ABCB1/G2 and competitively bound to the substrate-binding region of ABCB1/G2.

CONCLUSIONS:

These findings present novel therapeutic avenues whereby the combination of lansoprazole and chemotherapeutic agents mitigates MDR mediated by ABCB1/G2 overexpression.

01 Aug 2024·MICROCHIMICA ACTA

Preparation and study of a capillary electrochromatographic column prepared by conjugating β-CD COFs and gold-poly glycidyl methacrylate nanoparticles

Article

Author: Zhang, Dongxiang ; Shi, Shuang ; Long, Ke ; Yu, Jiatong ; Guan, Jin

A new enantioselective open-tubular capillary electrochromatography (OT-CEC) was developed employing β-cyclodextrin covalent organic frameworks (β-CD COFs) conjugated gold-poly glycidyl methacrylate nanoparticles (Au-PGMA NPs) as a stationary phase. The resulting coating layer on the inner wall of the fabricated capillary column was characterized by scanning electron microscopy (SEM), Fourier transform infrared spectroscopy (FT-IR), energy dispersive spectroscopy (EDS), and electroosmotic flow (EOF) experiments. The performance of the fabricated capillary column was evaluated by CEC using enantiomers of seven model analytes, including two proton pump inhibitors (PPIs, omeprazole and tenatoprazole), three amino acids (AAs, tyrosine, phenylalanine, and tryptophan), and two fluoroquinolones (FQs, gatifloxacin and sparfloxacin). The influences of coating time, buffer concentration, buffer pH, and applied voltage on enantioseparation were investigated to obtain satisfactory enantioselectivity. In the optimum conditions, the enantiomers of seven analytes were fully resolved within 10 min with high resolutions of 3.03 to 5.25. The inter- to intra-day and column-to-column repeatabilities of the fabricated capillary column were lower than 4.26% RSD. Furthermore, molecular docking studies were performed based on the chiral fabricated column and as ligand isomers of analytes using Auto Dock Tools. The binding energies and interactions acquired from docking results of analytes supported the experimental data.

01 Feb 2024·Pharmacotherapy

Acid‐suppressive drugs: A systematic review and network meta‐analysis of their nocturnal acid‐inhibitory effect

Review

Author: Zou, Shupeng ; Cheng, Qian ; Sun, Minghui ; Shi, Xuan ; Ouyang, Mengling

Abstract:

Background and Aims:

Acid‐suppressive drugs (ASDs) are widely used in many gastric acid‐associated diseases. Nocturnal acid breakthrough has been a common problem of many ASDs, such as proton‐pump inhibitors (PPIs) and H2‐receptor antagonists (H2RAs). Potassium‐competitive acid blockers (P‐CABs) are expected to solve this continuing conundrum. This article examined major ASDs and compared them with placebo in terms of nocturnal acid‐inhibitory effects, using a network meta‐analysis of randomized controlled trials (RCTs).

Methods:

To compare the effectiveness of major ASDs, a Bayesian network meta‐analysis (NMA) was applied to process data extracted from RCTs. The plausible ranking for each regimen and some subgroups were assessed by surface under the cumulative ranking curves (SUCRA).

Results:

Fifty‐five RCTs were conducted with 2015 participants. In terms of nocturnal acid‐inhibitory effects, the overall results showed that tegoprazan (SUCRA 91.8%) and vonoprazan (SUCRA 91.0%) had the best performance, followed by new PPIs (including tenatoprazole and ilaprazole) (SUCRA 76.6%), additional H2RAs once at bedtime (AHB) (SUCRA 61.3%), isomer PPIs (including esomeprazole and dexlansoprazole) (SUCRA 38.6%), revaprazan (SUCRA 34.7%), traditional PPIs (including omeprazole, rabeprazole, pantoprazole, lansoprazole) (SUCRA 32.6%), H2RAs (SUCRA 23.1%), and placebo (SUCRA 0.3%). In some subgroups, the nocturnal acid‐inhibitory effect of vonoprazan or tegoprazan was better than most of the other regimens, even new PPIs and AHB.

Conclusions:

This is the first study to compare the effect of ASDs on inhibiting nocturnal acid breakthrough. Overall, in terms of nocturnal acid‐inhibitory effect, vonoprazan and tegoprazan had an advantage against other regimens including H2RAs, isomer PPIs, traditional PPIs, AHB, and new PPIs. Even in some subgroups, such as language classification (English), types of study design (crossover‐RCT), age (≤40 years), BMI (18.5–24.9 kg/m2), continent (Asia and North America), disease status (health), the duration of therapy (2 weeks), and time of administration (at daytime or at night‐time), the nocturnal acid‐inhibitory effect of vonoprazan or tegoprazan were better than most regimens, even AHB and new PPIs.

100 Deals associated with S-Tenatoprazole

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External Link

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Gastroesophageal Reflux	NDA/BLA	Japan	Mitsubishi Tanabe Pharma Corp.	01 Mar 1999
Erosive esophagitis	Phase 2	Canada	Steba France SASU	01 Feb 2006
Esophagitis, Peptic	Phase 2	Canada	Steba France SASU	01 Feb 2006
Duodenal Ulcer	Phase 1	United States	Steba France SASU	01 Sep 2006
Esophagitis	Phase 1	United States	Steba France SASU	01 Sep 2006
Stomach Ulcer	Phase 1	United States	Steba France SASU	01 Sep 2006