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

Action

inhibitors

Mechanism

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

Therapeutic Areas

Nervous System DiseasesCardiovascular DiseasesOther Diseases

Active Indication

StrokeST Elevation Myocardial InfarctionDementia, Vascular+ [3]

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.

+ [8]

Inactive Organization

Sichuan Huiyu Pharmaceutical Co., Ltd.

Drug Highest PhaseApproved

First Approval Date

China (30 Sep 2002),

Stroke

Regulation-

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Structure/Sequence

Molecular FormulaC12H14O2

InChIKeyHJXMNVQARNZTEE-UHFFFAOYSA-N

CAS Registry6066-49-5

主要研究目的：研究空腹状态下单次给药受试制剂丁苯酞注射液（规格：5 ml:25 mg，吉林省奇健生物技术有限公司生产）与参比制剂丁苯酞氯化钠注射液（恩必普®，规格：100 ml:丁苯酞25 mg与氯化钠0.9 g；石药集团恩必普药业有限公司生产）在健康受试者体内的药代动力学，比较空腹状态下静脉输注受试制剂和参比制剂的生物利用度。次要研究目的：评估受试制剂丁苯酞注射液（规格：5 ml:25 mg和参比制剂丁苯酞氯化钠注射液（恩必普®，规格：100 ml:丁苯酞 25 mg与氯化钠 0.9 g）在健康受试者中的安全性。

[Translation]

The main purpose of the study is to study the pharmacokinetics of a single dose of the test preparation butylphthalide injection (specification: 5 ml: 25 mg, produced by Jilin Qijian Biotechnology Co., Ltd.) and the reference preparation butylphthalide sodium chloride injection (ENBIP®, specification: 100 ml: butylphthalide 25 mg and sodium chloride 0.9 g; produced by CSPC ENBIP Pharmaceutical Co., Ltd.) in healthy subjects, and to compare the bioavailability of the test preparation and the reference preparation after intravenous infusion in the fasting state. Secondary purpose of the study: to evaluate the safety of the test preparation butylphthalide injection (specification: 5 ml: 25 mg) and the reference preparation butylphthalide sodium chloride injection (ENBIP®, specification: 100 ml: butylphthalide 25 mg and sodium chloride 0.9 g) in healthy subjects.

Start Date15 Jan 2025

Sponsor / Collaborator

Jilin Qijian Biotechnology Co., Ltd

NCT06704685

/ Not yet recruitingPhase 3IIT

A Randomized Controlled Trial on the Efficacy and Safety of Butylphthalide in Reducing Myocardial Infarction Size and Improving Outcomes in STEMI Patients After Primary PCI - A Prospective, Multicenter, Randomized, Placebo, Double-blinded End Trial.

This study is a prospective, randomized, placebo-double-blind, multicenter clinical trial. The purpose of this study is to investigate whether "butylphthalide +PCI" combined treatment mode on the basis of traditional drug therapy could reduce myocardial infarct size, improve cardiac function and long-term prognosis of patients with acute myocardial infarction, and verify the drug safety of butylphthalide in the treatment of STEMI within the window period of 12 hours.

Start Date01 Dec 2024

Sponsor / Collaborator

Xiangya Hospital Central South University

[+1]

CTR20242962

/ CompletedNot Applicable

丁苯酞氯化钠注射液在健康受试者中单中心、随机、开放、两制剂、单次给药、两周期、双交叉空腹生物等效性试验

[Translation] A single-center, randomized, open-label, two-dose, single-dose, two-period, double-crossover fasting bioequivalence study of sodium chloride butylphthalide injection in healthy volunteers

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.

100 Clinical Results associated with Butylphthalide

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100 Translational Medicine associated with Butylphthalide

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100 Patents (Medical) associated with Butylphthalide

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1,598

Literatures (Medical) associated with Butylphthalide

04 Mar 2025·International Journal of Neuroscience

Effects of butylphthalide on cerebral vascular circulation, coagulation function, and neurological function in patients with acute severe ischemic stroke following intravenous thrombolysis: a preliminary study

Article

Author: Xia, Lei ; Xiong, Kaiju ; Zhao, Jiansen ; Zhong, Huaping ; Wang, Hui ; Li, Yu

OBJECTIVETo analyze the effects of Butylphthalide on cerebral vascular circulation, coagulation function, and neurological function in patients with acute severe ischemic stroke following intravenous thrombolysis.METHODSClinical efficacy, cerebral vascular circulation indicators [anterior cerebral artery (ACA), middle cerebral artery (MCA), vertebral artery (VA) blood flow velocity], coagulation function indicators [prothrombin time (PT), activated partial thromboplastin time (APTT), thrombin time (TT), fibrinogen (FIB)], neurological function indicators [Activities of Daily Living (ADL) score.RESULTSThe total effective rate of treatment in the control group was 76.47%, while in the observation group, it was 96.08%, with the observation group showing a significantly higher total effective rate than the control group (p < 0.05). Before treatment, there was no significant difference in ACA, MCA, and VA blood flow velocity between the two groups (p > 0.05). However, after treatment, the ACA, MCA, and VA blood flow velocity in the observation group were significantly higher than those in the control group (p < 0.05). Before treatment, there was no significant difference in PT, APTT, TT, and FIB levels between the two groups (p > 0.05).CONCLUSIONIn patients with acute severe ischemic stroke undergoing intravenous thrombolysis, the addition of Butylphthalide to the treatment regimen yields favorable clinical outcomes. Compared to Alteplase alone, the addition of Butylphthalide further improves cerebral vascular circulation and coagulation function, promoting the recovery and reconstruction of neurological function in patients. Importantly, the addition of Butylphthalide does not increase the risk of adverse reactions, making it a safe and ideal option for clinical application.

01 Mar 2025·Epilepsy & Behavior

Butylphthalide may inhibit blood–brain barrier disruption through complement-related pathways to alleviate cognitive impairment in epileptic mice

Article

Author: Xiao, Yuqing ; Jin, Xing ; Zhuang, Weihao ; Zhao, Linqian ; Liu, Qichang ; Chen, Shihao ; Xu, Huiqin

BACKGROUNDTemporal lobe epilepsy is often accompanied by comorbid symptoms such as anxiety, depression, and cognitive dysfunction. Research indicates a close relationship between blood-brain barrier (BBB) impairment and these symptoms. DL-3n-butylphthalide (NBP) has been reported to protect the BBB, but the molecular mechanisms by which NBP protects the BBB in epilepsy models remain unclear. This study investigated the protective effects of NBP on the BBB in epileptic mice to alleviate the comorbid symptoms associated with epilepsy.METHODSWe utilized Mendelian randomization to explore the association between VEGFA and epilepsy. In the animal experiments, adult male C57BL/6 mice were used to establish a KA-induced epilepsy model, receiving daily intraperitoneal injections of NBP for 30 days. After this period, behavioral experiments and Western blot analyses were conducted to assess whether the comorbid symptoms of epilepsy and BBB disruption were alleviated. Subsequently, RNA sequencing was performed to analyze potential signaling pathways involved in the pharmacological effects of NBP.RESULTSElevated circulating levels of VEGFA may be a risk factor for the onset of epilepsy. Animal experiments demonstrated that NBP treatment improved BBB disruption in KA-induced epileptic mice and alleviated depressive and anxious behaviors, as well as cognitive impairments. RNA sequencing results suggest that the pharmacological effects of NBP may be mediated through the inhibition of complement and coagulation cascades.CONCLUSIONNBP can protect the integrity of the BBB in KA-induced epileptic mice, inhibiting depression, anxiety behaviors, and cognitive dysfunction. This pharmacological effect may be associated with pathways involving complement and coagulation cascades.

01 Jan 2025·Journal of Ethnopharmacology

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

Article

Author: Yan, Lin ; Qian, Wenqi ; 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.

100 Deals associated with Butylphthalide

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External Link

KEGG	Wiki	ATC	Drug Bank
-	Butylphthalide	B01	DB12749

R&D Status

Approved

10 top approved records.

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

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
ST Elevation Myocardial Infarction	Phase 3	-	CSPC Pharmaceutical Group Ltd.	01 Dec 2024
Dementia, Vascular	Phase 3	China	CSPC NBP Pharmaceutical Co., Ltd.	29 Oct 2019
Ischemic stroke	Phase 2	United States	CSPC Pharmaceutical Group Ltd.	15 Jul 2022
Peripheral Nerve Injuries	Phase 2	China	CSPC NBP Pharmaceutical Co., Ltd.	30 Mar 2022
Peripheral Nerve Injuries	Phase 2	China	CSPC Zhongqi Pharmaceutical Technology Shijiazhuang Co., Ltd.	30 Mar 2022
Brain Ischemia	Phase 2	China	CSPC NBP Pharmaceutical Co., Ltd.	01 Jul 2011
Acute Ischemic Stroke	Phase 1	China	Chengdu Shibeikang Biomedical Technology Co Ltd	24 Aug 2023

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Clinical Result

Indication

Phase

Evaluation

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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)	evsbknvudh(bhixwufkoh) = vpveyudlyy ssspbvxjyi (huhzodiflw, tdkmgisvzs - zwikmiadho) View more	-	18 May 2016
				Cerebrolysin (Cerebrolysin)	evsbknvudh(bhixwufkoh) = sodwnwjonp ssspbvxjyi (huhzodiflw, mpaupgisgf - chgnszdbcr) View more