Delving into the Latest Updates on Flavoxate Hydrochloride with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

2-(1-piperidinyl)ethyl 3-methyl-4-oxo-2-phenyl-4H-chromene-8-carboxylate, 2-piperidinoethyl 3-methyl-4-oxo-2-phenyl-4H-1-benzopyran-8-carboxylate, 2-piperidinoethyl 3-methylflavone-8-carboxylate

+ [20]

Target

ORAI1

Action

inhibitors

Mechanism

ORAI1 inhibitors(Calcium release-activated calcium channel protein 1 inhibitors)

Therapeutic Areas

Urogenital Diseases

Active Indication

Urethral DiseasesChronic prostatitisCystitis+ [1]

Inactive Indication

DysuriaPainUrinary Bladder, Overactive+ [2]

Originator Organization

Johnson & Johnson

Active Organization

Nippon Shinyaku Co., Ltd.

Zhejiang Conba Pharmaceutical Co., Ltd.

Inactive Organization

Ortho-McNeil Pharmaceutical LLC

Drug Highest PhaseApproved

First Approval Date

United States (15 Jan 1970),

DysuriaPainUrinary Bladder, Overactive+ [2]

Regulation-

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Structure/Sequence

Molecular FormulaC24H25NO4

InChIKeySPIUTQOUKAMGCX-UHFFFAOYSA-N

CAS Registry15301-69-6

View All Structures (2)

Breast cancer, a leading cause of cancer-related mortality in women, is characterized by genomic instability and aberrant gene expression, often influenced by noncanonical nucleic acid structures such as G-quadruplexes (G4s). These structures, commonly found in the promoter regions and 5'-untranslated RNA sequences of several oncogenes, play crucial roles in regulating transcription and translation. Stabilizing these G4 structures offers a promising therapeutic strategy for targeting key oncogenic pathways. In this study, we employed a drug repurposing approach to identify FDA-approved drugs capable of binding and stabilizing G4s in breast cancer-related genes. Using ligand-based virtual screening and biophysical methods, we identified several promising compounds, such as azelastine, belotecan, and irinotecan, as effective G4 binders, with significant antiproliferative effects in breast cancer cell lines. Notably, belotecan and irinotecan exhibited a synergistic mechanism, combining G4 stabilization with their established topoisomerase I inhibition activity to enhance cytotoxicity in cancer cells. Our findings support the therapeutic potential of G4 stabilization in breast cancer, validate drug repurposing as an efficient strategy to identify G4-targeting drugs, and highlight how combining G4 stabilization with other established drug activities may improve anticancer efficacy.

02 Jan 2025·Expert Opinion on Drug Safety

Risk of drug-induced delirium in older patients- a pharmacovigilance study of FDA adverse event reporting system database

Article

Author: Cui, Yimin ; Li, Jiayu ; Zhou, Ying ; Wan, Liyan ; Jia, Boying ; Zhou, Shuang

BACKGROUNDDrug-induced delirium is known risk factors associated with increased morbidity and mortality in older patients. The objective was to evaluate the risk of drug-related delirium in older patients based on the FDA Adverse Event Reporting System (FAERS).RESEARCH DESIGN AND METHODSDelirium reports in older patients (age ≥65) extracted from the FAERS database using Open Vigil 2.1. The reported odds ratio and the proportional reported ratio were calculated to detect the adverse reaction signal of delirium. Combined with published evidence, suspected drugs were categorized as known, possible, or new potential delirium-risk-increasing drugs.RESULTSOf the 130,885 reports (including 28,850 delirium events and 1,857 drugs) analyzed for this study, 314 positive signal drugs were detected. Positive signal drugs are mainly concentrated on the drug of nervous system, cardiovascular system , alimentary tract and metabolism and anti-infectives for systemic use. Of the positive signal drugs, 26.11% (82/314) were known delirium-risk increasing drugs, 44.90% (141/314) were possible and 28.98% (91/314) were new potential.CONCLUSIONDrug-induced delirium risk is prevalent in older patients, according to the FAERS. The risk level of drug-induced delirium should be taken into account to optimize drug therapy in clinical practice.

01 Jan 2025·Journal of Ethnopharmacology

Huang-Lian-Jie-Du Decoction alleviates diabetic encephalopathy by regulating inflammation and pyroptosis via suppression of AGEs/RAGE/NF-κB pathways

Article

Author: Tang, Dan ; Chen, Meng-Di ; Deng, Chao-Fan ; Gu, Wen-Ting ; Deng, Si-Min ; Zhuang, Guo-Dong ; Wang, Shu-Mei

ETHNOPHARMACOLOGICAL RELEVANCECognitive dysfunction associated with diabetes, known as diabetic encephalopathy (DE), is a grave neurodegenerative condition triggered by diabetes, and persistent inflammation plays a vital role in its development. The renowned traditional Chinese medicine Huang-Lian-Jie-Du Decoction (HLJDD) is clinically proven to manage diabetes mellitus and Alzheimer's disease and is famous for its heat-clearing and detoxifying effects. However, the underlying mechanisms through which HLJDD affects DE remain to be elucidated.AIM OF THE STUDYTo explore the beneficial effects of HLJDD on improving cognitive dysfunction in DE mice.STUDY DESIGN AND METHODSA diabetic mouse was established through a high-fat diet and subsequent administration of streptozotocin over five consecutive days. After the animals were confirmed to have diabetes, they were treated with HLJDD. After oral administration of HLJDD or metformin for 14 weeks, behavioral tests were used to assess their cognitive capacity. Biochemical analyses were then performed to detect levels of glucose metabolism, followed by histological analyses to assess pathological damage. Furthermore, AGEs/RAGE/NF-κB axis related proteins were detected by Western blot or immunofluorescence techniques. An advanced UPLC-Q-Orbitrap HRMS/MS analytical technique utilizing a chemical derivatization strategy was employed for comprehensive metabolic profiling of carbonyl compounds in the plasma of DE mice.RESULTSPharmacological assessment revealed that HLJDD effectively mitigated cognitive dysfunction, normalized glucose metabolic imbalances, and repaired neuronal damage in DE mice. It reduced neuroinflammation by attenuating carbonyl stress, deactivating astrocytes and microglia, and preserving dopaminergic neurons. Additionally, metabolomics analysis revealed 18 carbonyl compounds with marked disparities between DE and control mice, with 12 metabolites approaching normal levels post-HLJDD intervention. Further investigations showed that HLJDD regulated inflammation and pyroptosis through suppressing AGEs/RAGE/NF-κB pathways.CONCLUSIONOur study indicated that HLJDD could ameliorate carbonyl stress via the regulation of carbonyl compound metabolism profiling, and inhibiting the AGEs/RAGE/NF-κB pathway, thereby alleviating inflammation and pyroptosis to exert beneficial effects on DE.

100 Deals associated with Flavoxate Hydrochloride

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External Link

KEGG	Wiki	ATC	Drug Bank
D00718	Flavoxate Hydrochloride	G04BD02	DB01148

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Urethral Diseases	China	Zhejiang Conba Pharmaceutical Co., Ltd.	01 Jan 1995
Chronic prostatitis	Japan	Nippon Shinyaku Co., Ltd.	01 Aug 1978
Cystitis	Japan	Nippon Shinyaku Co., Ltd.	01 Aug 1978
Pollakisuria	Japan	Nippon Shinyaku Co., Ltd.	01 Aug 1978