盐酸黄酮哌酯(Flavoxate Hydrochloride) - 药物靶点：ORAI1_在研适应症：尿道疾病，慢性前列腺炎，膀胱炎_专利_临床

概要

基本信息

药物类型

小分子化药

别名

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]

靶点

ORAI1

作用方式

抑制剂

作用机制

ORAI1抑制剂(钙离子释放激活钙通道蛋白-1抑制剂)

治疗领域

在研适应症

非在研适应症

原研机构

在研机构

Nippon Shinyaku Co., Ltd.

浙江康恩贝制药股份有限公司

非在研机构

Ortho-McNeil Pharmaceutical LLC

最高研发阶段批准上市

首次获批日期

美国 (1970-01-15),

排尿困难疼痛膀胱过度活动症+ [2]

最高研发阶段(中国)批准上市

特殊审评-

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结构/序列

分子式C24H25NO4

InChIKeySPIUTQOUKAMGCX-UHFFFAOYSA-N

CAS号15301-69-6

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关联

5

项与盐酸黄酮哌酯相关的临床试验

CTRI/2024/09/073950

/ Not yet recruitingN/AIIT

Effect of oral flavoxate on postoperative catheter related bladder dysfunction in adult males undergoing transurethral resection of bladder tumors- A randomized controlled trial vs solifenacin and placebo - Nil

开始日期2024-09-17

申办/合作机构-

CTRI/2020/04/024700

/ CompletedN/A

Single dose oral bioavailability pilot study of two test formulations ofFlavoxate XR Tablet 600 mg, once a day (T1) and Flavoxate XR Tablet800 mg, once a day (T2) and reference formulation of Flavoxate Tablet200 mg, thrice a day (R) in healthy adult male subjects under fastingconditions.

开始日期2020-04-20

申办/合作机构-

JPRN-UMIN000009999

/ CompletedN/AIIT

Clinical evaluation of add-on administration of flavoxate hydrochloride in nocturia patients resistant to an anticholinergic agent - Clinical evaluation of add-on administration of flavoxate hydrochloride in nocturia patients

开始日期2013-02-12

申办/合作机构-

100 项与盐酸黄酮哌酯相关的临床结果

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100 项与盐酸黄酮哌酯相关的转化医学

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100 项与盐酸黄酮哌酯相关的专利（医药）

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343

项与盐酸黄酮哌酯相关的文献（医药）

2025-03-01·European Journal of Medicinal Chemistry

Repurposing FDA-approved drugs to target G-quadruplexes in breast cancer

Article

作者: Marzano, Simona ; Randazzo, Antonio ; Landolfi, Laura ; Catalanotti, Bruno ; Malfitano, Anna Maria ; Pagano, Bruno ; Moraca, Federica ; Castellano, Giuliano ; Napolitano, Fabiana ; Arciuolo, Valentina ; Di Porzio, Anna ; D'Aria, Federica ; Amato, Jussara

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.

2025-01-02·Expert Opinion on Drug Safety

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

Article

作者: 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.

2025-01-01·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

作者: 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 项与盐酸黄酮哌酯相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D00718	盐酸黄酮哌酯	G04BD02	DB01148

研发状态

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
尿道疾病	中国	浙江康恩贝制药股份有限公司	1995-01-01
慢性前列腺炎	日本	Nippon Shinyaku Co., Ltd.	1978-08-01
膀胱炎	日本	Nippon Shinyaku Co., Ltd.	1978-08-01
尿频	日本	Nippon Shinyaku Co., Ltd.	1978-08-01