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]

NCT00282555

/ SuspendedPhase 2

Assessment of the Healing Rate of Erosive or Ulcerative Esophagitis After Two and Four Weeks of Treatment With S-Tenatoprazole-Na (STU-Na) 15 mg, 30 mg, 60 mg, 90 mg and Esomeprazole 40 mg. A Multicenter, Randomized, Double-Blind, Parallel Group Study.

STU-Na belongs to the proton pump inhibitors (PPI), a group of drugs that reduce gastric acidity. PPI are used to treat acid related diseases like erosive or ulcerative esophagitis. This trial aims to find out the therapeutic dose of STU-Na required for healing patients with erosive or ulcerative esophagitis. One of four dosages of STU-Na (15 mg, 30 mg, 60 mg, or 90 mg daily), or Esomeprazole 40 mg daily, an already marketed PPI, will be given to patients. The attribution to one of the 5 treatment groups will be by chance. Neither the patient nor the study physician will know, which treatment is administered to the patient.

Start Date01 Feb 2006

Sponsor / Collaborator

Steba France SASU

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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93

Literatures (Medical) associated with S-Tenatoprazole

11 Jun 2025·mBio

β-Coronaviruses exploit ESCRT for virion assembly and egress

Article

Author: Zhang, Yuanyuan ; Ren, Chaoqi ; Wang, Weiyang ; Huang, Linlong ; Wang, Xinlu ; Gao, Guangxia

ABSTRACT:

β-Coronaviruses assemble at the endoplasmic reticulum-to-Golgi compartment and exit cells through the lysosomal trafficking pathway. However, the molecular mechanisms of virion assembly and egress are largely unknown. Here, we report that β-coronaviruses recruit endosomal sorting complexes required for transport (ESCRTs) to facilitate virion assembly and egress. The viral proteins N and M interacted with ESCRT components TSG101 and VPS28, respectively. Electron microscopy analysis revealed that virion assembly was disrupted by TSG101 knockdown at an early stage and by VPS28 knockdown at a late stage. Knockdown of ESCRT components MVB12A and CHMP6 did not affect virion assembly but inhibited virion egress. Downregulation of these ESCRT factors or VPS4A, or treatment of cells with the TSG101 antagonist tenatoprazole significantly inhibited the production of the virion-like particles of β-coronaviruses and the replication of human coronavirus OC43. These findings indicate that β-coronaviruses exploit ESCRT for virion assembly and egress and suggest that the interaction interface between ESCRT and the viruses could be a target for the development of broad-spectrum anti-coronavirus therapeutics.

IMPORTANCE:

β-Coronaviruses have caused disastrous pandemics and may cause serious pandemics in the future. Virion assembly and egress are critical steps in the life cycle of coronaviruses. However, despite extensive studies in the past few years, the molecular mechanisms for virion assembly and egress are still largely unknown. Here we show that β-coronaviruses recruit ESCRT components TSG101 and VPS28 for virion assembly and that ESCRT components MVB12A and CHMP6 are required for virion egress. Treatment of cells with the TSG101 antagonist inhibited the assembly of multiple β-coronaviruses. These findings indicate that ESCRT participates in β-coronavirus assembly and egress and might be a potential target for the development of broad-spectrum anti-coronavirus therapeutics.

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.

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