A multi-national, multi-centre, double-masked, placebo-controlled proof of concept trial to evaluate the safety and efficacy of oral soraprazan in Stargardt disease

Start Date14 May 2019

Sponsor / Collaborator-

100 Clinical Results associated with Soraprazan(Takeda Pharmaceutical Co., Ltd.)

100 Translational Medicine associated with Soraprazan(Takeda Pharmaceutical Co., Ltd.)

100 Patents (Medical) associated with Soraprazan(Takeda Pharmaceutical Co., Ltd.)

Literatures (Medical) associated with Soraprazan(Takeda Pharmaceutical Co., Ltd.)

15 Mar 2024·ChemBioChem

Enzymatic Synthesis of Indole‐Based Imidazopyridine using α‐Amylase

Article

Author: Tyagi, Vikas ; Kamboj, Priya

AbstractThe imidazo[1,2‐a]pyridine scaffold has gained significant attention due to its presence as a lead structure in several commercially available pharmaceuticals like zolimidine, zolpidem, olprinone, soraprazan, etc. Further, indole‐based imidazo[1,2‐a]pyridine derivatives have been found interesting due to their anticancer and antibacterial activities. However, limited methods have been reported for the synthesis of indole‐based imidazo[1,2‐a]pyridines. In this study, we have successfully developed a biocatalytic process for synthesizing indole‐based imidazo[1,2‐a]pyridine derivatives using the α‐amylase enzyme catalyzed Groebke‐Blackburn‐Bienayme (GBB) multicomponent reaction of 2‐aminopyridine, indole‐3‐carboxaldehyde, and isocyanide. The generality and robustness of this protocol were shown by synthesizing differently substituted indole‐based imidazo[1,2‐a]pyridines in good isolated yields. Furthermore, to make α‐amylase a reusable catalyst for GBB multicomponent reaction, it was immobilized onto magnetic metal‐organic framework (MOF) materials [Fe3O4@MIL‐100(Fe)] and found reusable up to four consecutive catalytic cycles without the significant loss in catalytic activity.

09 Jun 2022·Journal of Medicinal ChemistryQ1 · MEDICINE

Structural Basis for Binding of Potassium-Competitive Acid Blockers to the Gastric Proton Pump

Q1 · MEDICINE

Article

Author: Madapally, Hridya Valia ; Abe, Kazuhiro ; Hayashida, Kenichi ; Morita, Mikio ; Shigematsu, Hideki ; Khandelia, Himanshu ; Yamagishi, Tatsuya ; Tanaka, Saki ; Oshima, Atsunori ; Gerle, Christoph

As specific inhibitors of the gastric proton pump, responsible for gastric acidification, K⁺-competitive acid blockers (P-CABs) have recently been utilized in the clinical treatment of gastric acid-related diseases in Asia. However, as these compounds have been developed based on phenotypic screening, their detailed binding poses are unknown. We show crystal and cryo-EM structures of the gastric proton pump in complex with four different P-CABs, tegoprazan, soraprazan, PF-03716556 and revaprazan, at resolutions reaching 2.8 Å. The structures describe molecular details of their interactions and are supported by functional analyses of mutations and molecular dynamics simulations. We reveal that revaprazan has a novel binding mode in which its tetrahydroisoquinoline moiety binds deep in the cation transport conduit. The mechanism of action of these P-CABs can now be evaluated at the molecular level, which will facilitate the rational development and improvement of currently available P-CABs to provide better treatment of acid-related gastrointestinal diseases.

01 Mar 2022·Free Radical Biology and MedicineQ2 · MEDICINE

Removal of RPE lipofuscin results in rescue from retinal degeneration in a mouse model of advanced Stargardt disease: Role of reactive oxygen species

Q2 · MEDICINE

Article

Author: Fang, Yuan ; Schraermeyer, Ulrich ; Biesemeier, Antje ; Peters, Tobias ; Szewczyk, Grzegorz ; Tschulakow, Alexander V ; Heiduschka, Peter ; Burnet, Michael ; Julien-Schraermeyer, Sylvie ; Taubitz, Tatjana ; Sarna, Tadeusz

Accumulation of lipofuscin in the retinal pigment epithelium (RPE) is a hallmark of aging and is associated with retinal degeneration encountered in age-related macular degeneration (AMD) and Stargardt disease (SD). Currently, treatment for lipofuscin-induced retinal degeneration is unavailable. Here, we report that Remofuscin (INN: soraprazan, a tetrahydropyridoether small molecule) reverses lipofuscin accumulation in aged primary human RPE cells and is non-cytotoxic in aged SD mouse RPE cells in vitro. In addition, we show that the removal of lipofuscin after a single intravitreal injection of Remofuscin results in a rescue from retinal degeneration in a mouse model of advanced SD which is even accompanied by an amelioration of the retinal dysfunction. Finally, we demonstrate that the mechanism causing lipofuscinolysis may involve the reactive oxygen species generated via the presence of Remofuscin. These data suggest a possible therapeutic approach to untreatable lipofuscin-mediated diseases like AMD, SD and lipofuscinopathies in neurodegenerative diseases.

100 Deals associated with Soraprazan(Takeda Pharmaceutical Co., Ltd.)

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Indication	Highest Phase	Country/Location	Organization	Date
Stargardt Disease	Phase 2	-	Takeda Pharmaceutical Co., Ltd.	-
Gastroesophageal Reflux	Preclinical	-	Takeda Pharmaceutical Co., Ltd.	-
Gastroesophageal Reflux	Preclinical	DE	ALTANA Pharma AG	-

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