Delving into the Latest Updates on Imidazofurin with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

imidazofurin, TAD

Target

IMPDH

Action

inhibitors

Mechanism

IMPDH inhibitors(Inosine-5'-monophosphate dehydrogenase (IMPDH) inhibitors)

Therapeutic Areas

Neoplasms

Active Indication-

Inactive Indication

Neoplasms

Originator Organization

University of Camerino

Active Organization-

Inactive Organization

University of Camerino

License Organization-

Drug Highest PhasePendingDiscovery

First Approval Date-

Regulation-

Patients with severe asthma (SA) experience significant morbidity, due to high exacerbation rates and frequent use of oral corticosteroids (OCS). In randomized trials, biologic therapies (biologics) consistently improve SA outcomes. Using pharmacy claims data, the AUBOCIAS study estimated OCS use before and after initiation of biologics, and yearly trend of biologics use among SA patients.

PROCEDURES:

Anonymized dispensation data from pharmacies (IQVIA Switzerland LRx network) were retrieved between 2018 and 2023. SA patients aged ≥12 were identified by regular use of fixed-dose combinations over ≥12 months, or OCS, or any biologics used for SA. Main outcome was the change in total annual dose (TAD) of OCS after initiation of biologics.

MAIN FINDINGS:

In 2023, among a total of 26,146 patients with likely asthma, 3882 (10.6 %) were identified as having SA. The mean age was 61 years and 57.0 % were females. Of those 63.0 % were using OCS, with a mean TAD of 1760 mg. Initiations of biologics for SA increased from 0.4 % (2018) to 14.3 % (2023). Over the study period, among 532 biologics initiators, 282 (53.0 %) used OCS: 87 patients (36.0 %) could be weaned (p < 0.0001). Among persistent OCS users, the mean TAD decreased from 1200-375 mg (-68.8 %; p < 0.0001).

CONCLUSIONS:

In Switzerland, 10.6 % of patients with likely asthma identified in the LRx database were considered to have SA. OCS were frequently used at high TAD, while biologics were increasingly initiated. Most biologics initiators were able to reduce or discontinue OCS.

01 Nov 2025·PHYTOMEDICINE

Genistein ameliorates thoracic aortic dissection by inhibiting CB1 receptor hyperactivation and modulating its-mediated cAMP-PKA signaling

Article

Author: Huang, Tao ; Xing, Bo ; Chi, Yanbang ; Zhao, Jikai ; Jiang, Hui ; Fu, Yao ; Huang, Yuting ; Yu, Liming ; Sun, Jingli ; Zhou, Zijun ; Wang, Huishan ; Qu, Dongying

BACKGROUND:

Thoracic aortic dissection (TAD) is a fatal cardiovascular disease characterized by vascular smooth muscle cell (VSMC) phenotypic remodeling and inflammation. Cannabinoid 1 (CB1/Cnr1) receptor has been implicated in cardiovascular diseases, but its role in TAD and its downstream signaling remains unclear. Genistein (Gen), an isoflavone abundant in legumes, has demonstrated promising therapeutic potential in cardiovascular diseases such as vascular calcification, hypertension, and atherosclerosis due to its anti-inflammatory, antioxidant, and metabolic regulatory properties. However, the role of Gen in the progression of TAD remains poorly understood.

PURPOSE:

The present study was designed to investigate the potential of Gen in alleviating medial degeneration and delaying TAD progression by inhibiting the CB1 receptor and modulating its associated cAMP-PKA signaling.

METHODS:

In vitro and in vivo experiments evaluated the effects of AM251, a selective CB1 receptor antagonist, and genistein (Gen), a natural CB1 receptor inhibitor, on VSMC remodeling, NLRP3-mediated pyroptosis, and TAD progression. The involvement of cAMP-PKA signaling was validated using the PKA inhibitor H-89.

RESULTS:

CB1 receptor was highly expressed in VSMCs and significantly upregulated in TAD group, while cAMP-PKA signaling was suppressed. Elevated CB1 receptor expression correlated with increased NLRP3-mediated pyroptosis and enhanced VSMC phenotypic modulation. AM251 and Gen treatment restored cAMP-PKA signaling, reduced pyroptosis, and preserved the contractile phenotype of VSMCs, thereby delaying TAD progression. However, overexpression of CB1 receptor diminished the beneficial effects of Gen treatment in VSMCs. Single-cell RNA sequencing further confirmed that Gen reversed the CB1 receptor -induced suppression of cAMP-PKA signaling and mitigated VSMC remodeling. Notably, the protective effects of Gen were abrogated upon PKA inhibition by H-89, highlighting the essential role of cAMP-PKA activation. In vivo, Gen administration significantly reduced TAD incidence, improved aortic wall integrity, and decreased inflammatory cell infiltration.

CONCLUSION:

CB1 receptor overexpression contributes to TAD development by suppressing cAMP-PKA signaling, promoting pyroptosis, and inducing VSMC remodeling. Genistein exerts protective effects via CB1 receptor inhibition and cAMP-PKA upregulation, suggesting CB1 receptor as a promising therapeutic target for TAD.

15 Sep 2025·WATER SCIENCE AND TECHNOLOGY

Intensification of thermophilic anaerobic digestion of sewage sludge by thermal hydrolysis

Article

Author: Appels, Lise ; Sykora, Petr ; Jenicek, Pavel ; Rosicky, Jiri ; Srb, Martin ; Cardova, Anna

ABSTRACT:

Thermal hydrolysis (THP) combined with thermophilic anaerobic digestion (TAD) offers promising pathways for enhancing sewage sludge treatment. This study is among the first to directly compare THP as both pre- and post-treatment options for TAD. Pre-treatment of waste activated sludge (THP-WAS) and post-treatment of digested sludge (THP-DS) were evaluated on their impacts on process stability, biogas production, and sludge dewaterability. Pilot-scale trials at a wastewater treatment plant (WWTP) in Prague revealed that THP-WAS increased sludge solubilization but faced challenges such as volatile fatty acid accumulation, adversely affecting reactor stability and specific biogas yield. In contrast, THP-DS enhanced biogas production by 10%, improved sludge dewaterability, and achieved superior methane content (73.2%). Further research is needed to optimize THP parameters for reactor stability and to better understand interactions between hydrolyzed WAS and primary sludge.

100 Deals associated with Imidazofurin

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