Delving into the Latest Updates on Butylphthalide with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

3-n-butylphthalide, Butylphthalide and Sodium Chloride

+ [6]

Target

KCNK

Mechanism

KCNK inhibitors(Potassium two pore domain channel subfamily K inhibitors), Platelet aggregation inhibitors

Therapeutic Areas

Nervous System DiseasesCardiovascular DiseasesOther Diseases

Active Indication

StrokeDementia, VascularIschemic stroke+ [2]

Inactive Indication

Brain Ischemia

Originator Organization

CSPC Ouyi Pharmaceutical Co., Ltd.

Active Organization

CSPC NBP Pharmaceutical Co., Ltd.

CSPC Zhongqi Pharmaceutical Technology Shijiazhuang Co., Ltd.Hebei Saipu Ruisi Pharmaceutical Technology Co., Ltd.

+ [7]

Inactive Organization

Sichuan Huiyu Pharmaceutical Co., Ltd.

Drug Highest PhaseApproved

First Approval Date

CN (30 Sep 2002),

Stroke

Regulation-

Login to view timeline

Structure

Molecular FormulaC12H14O2

InChIKeyHJXMNVQARNZTEE-UHFFFAOYSA-N

CAS Registry6066-49-5

主要目的：以药代动力学参数作为主要终点评价指标，比较在空腹状态下静脉输注受试制剂丁苯酞氯化钠注射液（生产厂家：辰欣药业股份有限公司，规格：100ml：丁苯酞25mg与氯化钠0.9g）与参比制剂丁苯酞氯化钠注射液（持证商：石药集团恩必普药业有限公司，商品名：恩必普，规格：100ml：丁苯酞25mg与氯化钠0.9g）后在健康受试者体内的药代动力学行为，评价两种制剂的生物等效性。次要目的：观察受试制剂丁苯酞氯化钠注射液和参比制剂丁苯酞氯化钠注射液在健康受试者中的安全性。

[Translation]

Main purpose: Using pharmacokinetic parameters as the primary endpoint evaluation index, compare the pharmacokinetic behavior of the test preparation sodium butylphthalide injection (manufacturer: Chenxin Pharmaceutical Co., Ltd., specification: 100ml: 25mg butylphthalide and 0.9g sodium chloride) and the reference preparation sodium butylphthalide injection (certificate holder: CSPC Pharmaceutical Group Enbi Pharmaceutical Co., Ltd., trade name: Enbi, specification: 100ml: 25mg butylphthalide and 0.9g sodium chloride) in healthy subjects after intravenous infusion in the fasting state, and evaluate the bioequivalence of the two preparations. Secondary purpose: Observe the safety of the test preparation sodium butylphthalide injection and the reference preparation sodium butylphthalide injection in healthy subjects.

Start Date17 Oct 2024

Sponsor / Collaborator

Cisen Pharmaceutical Ltd.

CTR20243013 / Active, not recruitingNot Applicable

丁苯酞氯化钠注射液人体生物等效性研究

[Translation] Study on the bioequivalence of sodium chloride butylphthalide injection in healthy volunteers

主要目的：本试验旨在研究健康受试者单次空腹静脉滴注江西科伦药业有限公司研制、生产的丁苯酞氯化钠注射液（100 ml：丁苯酞25 mg与氯化钠0.9 g）的药代动力学特征；以石药集团恩必普药业有限公司生产的丁苯酞氯化钠注射液（恩必普®，100 ml：丁苯酞25 mg与氯化钠0.9 g）为参比制剂，比较两制剂中的药动学参数，评价两制剂的人体生物等效性。次要目的：评估受试制剂和参比制剂在健康受试者中的安全性。

[Translation]

Main purpose: This study aims to study the pharmacokinetic characteristics of a single fasting intravenous drip of sodium butylphthalide injection (100 ml: 25 mg butylphthalide and 0.9 g sodium chloride) developed and produced by Jiangxi Kelun Pharmaceutical Co., Ltd. in healthy subjects; using sodium butylphthalide injection (ENBIP®, 100 ml: 25 mg butylphthalide and 0.9 g sodium chloride) produced by CSPC Pharmaceutical Group Enbi Pharmaceutical Co., Ltd. as the reference preparation, compare the pharmacokinetic parameters of the two preparations and evaluate the human bioequivalence of the two preparations. Secondary purpose: To evaluate the safety of the test preparation and the reference preparation in healthy subjects.

Start Date08 Oct 2024

Sponsor / Collaborator

Jiangxi Kelun Medicine Industry Co. Ltd.

CTR20243257 / Active, not recruitingNot Applicable

丁苯酞软胶囊在空腹条件下的人体生物等效性试验

[Translation] Bioequivalence study of butylphthalide soft capsules in humans under fasting conditions

考察健康受试者在空腹条件下，单次口服1粒由安徽艾立德制药有限公司提供的丁苯酞软胶囊（受试制剂，规格：0.1g）与单次口服1粒由石药集团恩必普药业有限公司生产的丁苯酞软胶囊（参比制剂，商品名：恩必普®，规格：0.1g）的药代动力学特征，评价两制剂间的生物等效性和安全性，为该受试制剂注册申请提供依据。

[Translation]

To investigate the pharmacokinetic characteristics of healthy subjects under fasting conditions, when taking a single oral dose of 1 tablet of butylphthalide soft capsule (test preparation, specification: 0.1g) provided by Anhui Ailede Pharmaceutical Co., Ltd. and a single oral dose of 1 tablet of butylphthalide soft capsule (reference preparation, trade name: Enbipu®, specification: 0.1g) produced by CSPC Pharmaceutical Group Enbipu Pharmaceutical Co., Ltd., and evaluate the bioequivalence and safety of the two preparations, so as to provide a basis for the registration application of the test preparation.

Start Date07 Oct 2024

Sponsor / Collaborator

Anhui Ailide Pharmaceutical Co., Ltd.Startup

100 Clinical Results associated with Butylphthalide

Login to view more data

100 Translational Medicine associated with Butylphthalide

Login to view more data

100 Patents (Medical) associated with Butylphthalide

Login to view more data

335

Literatures (Medical) associated with Butylphthalide

01 Jan 2025·Journal of Ethnopharmacology

Butylphthalide mitigates traumatic brain injury by activating anti-ferroptotic AHR-CYP1B1 pathway

Article

Author: Qian, Wenqi ; Yan, Lin ; Yang, Su ; Ni, Haoqi ; Chen, Zhibo ; Yuan, Lin ; Zhuge, Qichuan ; Gu, Liuqing ; Ni, Zhihui ; Lv, Xinhuang

ETHNOPHARMACOLOGICAL RELEVANCEIncreasing evidence suggests that ferroptosis, an iron-dependent form of cell death characterized by lipid peroxidation, may play a substantial role in the traumatic brain injury (TBI) pathophysiology. 3-n-butylphthalide (NBP), a compound extracted from the seeds of Apium graveolens Linn (Chinese celery) and used in China to treat ischemic stroke, has demonstrated encouraging anti-reactive oxygen species (ROS) effects. Ascertaining whether NBP can inhibit ferroptosis and its mechanism could potentially expand its use in models of neurological injury and neurodegenerative diseases.METHODS AND RESULTSIn this study, we used erastin-induced in vitro ferroptosis models (HT22 cells, hippocampal slices, and primary neurons) and an in vivo controlled cortical impact mouse model. Our study revealed that NBP administration mitigated erastin-induced death in HT-22 cells and decreased ROS levels, lipid peroxidation, and mitochondrial superoxide indicators, resulting in mitochondrial protection. Moreover, the ability of NBP to inhibit ferroptosis was confirmed in organotypic hippocampal slice cultures and a TBI mouse model. NBP rescued neurons, inhibited microglial activation, and reduced iron levels in the brain tissue. The protective effect of NBP can be partly attributed to the inhibition of the AHR-CYP1B1 axis, as evidenced by RNA-seq and CYP1B1 overexpression/inhibition experiments in HT22 cells and primary neurons.CONCLUSIONSOur study underscores that NBP inhibition of the AHR-CYP1B1 axis reduces ferroptosis in neuronal damage and ameliorates brain injury.

01 Oct 2024·Neurotherapeutics

Cerebroprotective action of butylphthalide in acute ischemic stroke: Potential role of Nrf2/HO-1 signaling pathway

Article

Author: Patel, Rakesh B. ; Chauhan, Anil K ; Chauhan, Anil K. ; Patel, Rakesh B

01 Oct 2024·Zhongguo yi xue ke xue yuan xue bao. Acta Academiae Medicinae Sinicae

[Mechanism of Butylphthalide in Treating Delayed Encephalopathy After Carbon Monoxide Poisoning Based on Activation of Microglia].

Article

Author: Zhang, Jun ; Xu, Mao-Mao ; Pang, Jiang-Xia ; Wang, Bao-Jun ; Shi, Yu ; Chen, Chao ; Li, Yang

Objective To explore the mechanism of butylphthalide (NBP) in regulating microglia activation and inflammatory cytokine expression in the hippocampus of the mouse model of delayed encephalopathy after carbon monoxide poisoning (DEACMP). Methods Wild-type C57 adult mice with normal cognitive function were selected,and DEACMP was modeled by static inhalation of carbon monoxide.The mice were randomized into three groups:DEACMP,control,and NBP.The NBP group was administrated with NBP suspension at 6 mg/kg by gavage for 21 days,and the DEACMP and control groups were administrated with the same amount of vegetable oil by gavage.The hippocampal injury was observed by HE staining.The protein level of ionized calcium-binding adapter molecule 1 (IBA1) was determined by Western blotting,and the levels of downstream inflammatory cytokines were measured by ELISA. Results Compared with the control group,the DEACMP and NBP groups showed prolonged escape latency (P=0.001,P=0.029),reduced nerve cells (P=0.001,P=0.035),up-regulated expression of IBA1 (P=0.001,P=0.042),increased mean fluorescence intensity of IBA1 (P=0.001,P=0.021),and elevated levels of tumor necrosis factor-α (TNF-α) (P=0.002,P=0.024),interleukin (IL)-6 (P=0.001,P=0.015),and IL-1β (P=0.001,P=0.023).Compared with the DEACMP group,the NBP group showed shortened escape latency (P=0.025),increased nerve cells (P=0.039),down-regulated expression of IBA1 (P=0.035),decreased average fluorescence intensity of IBA1 (P=0.031),and lowered levels of TNF-α (P=0.028),IL-6 (P=0.037),and IL-1β (P=0.034). Conclusion NBP can inhibit the activation of microglia and reduce the expression of inflammatory factors,thereby alleviating cognitive dysfunction and brain tissue damage caused by DEACMP.

100 Deals associated with Butylphthalide

Login to view more data

External Link

KEGG	Wiki	ATC	Drug Bank
-	Butylphthalide	B01	DB12749

R&D Status

Approved

10 top approved records.

Login

to view more data

Indication	Country/Location	Organization	Date
Stroke	CN	Shijiazhuang Pharmaceutical Group Huasheng Pharmaceutical Co., Ltd.	30 Sep 2002

Developing

10 top R&D records.

Login

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Dementia, Vascular	Phase 3	CN	CSPC Zhongqi Pharmaceutical Technology Shijiazhuang Co., Ltd.	27 Nov 2019
Dementia, Vascular	Phase 3	CN	CSPC NBP Pharmaceutical Co., Ltd.	27 Nov 2019
Ischemic stroke	Phase 2	US	CSPC Pharmaceutical Group Ltd.	15 Jul 2022
Peripheral Nerve Injuries	Phase 2	CN	CSPC Zhongqi Pharmaceutical Technology Shijiazhuang Co., Ltd.	30 Mar 2022
Peripheral Nerve Injuries	Phase 2	CN	CSPC NBP Pharmaceutical Co., Ltd.	30 Mar 2022
Acute Ischemic Stroke	Phase 1	CN	Chengdu Shibeikang Biomedical Technology Co Ltd	24 Aug 2023
Brain Ischemia	Phase 1	CN	CSPC NBP Pharmaceutical Co., Ltd.	01 Jul 2011

Login to view more data

Clinical Result

Indication

Phase

Evaluation

View All Results

Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT02149875 (CTgov)	Phase 1/2	Acute Ischemic Stroke	84	Dl-3-n-butylphthalide (Dl-3-n-butylphthalide)	gpuueytbwa(npcsyqimdr) = prowyjsvvp jraorikgbq (obrudihywk, txxmdeelah - zqvxycdaup) View more	-	18 May 2016
				Cerebrolysin (Cerebrolysin)	gpuueytbwa(npcsyqimdr) = yzyzddnpjl jraorikgbq (obrudihywk, roigtbfozo - yfuqyaahid) View more