Though intravenous thrombolysis has been shown to improve symptoms in acute ischemic stroke patients, the recanalization rate remains low (22.6%) and only around 30% of patients benefit from the treatment. Recently, endovascular thrombectomy using stent retrievers or catheters has proven to be more effective, with a success rate of nearly 80%. However, only 50% of patients experience clinical improvement, highlighting the need for new treatment strategies to enhance outcomes. Current guidelines recommend maintaining systolic blood pressure (BP) below 180 mmHg after thrombectomy, but there is a lack of evidence regarding optimal blood pressure management post-reperfusion.
Four randomized clinical trials, including the OPTIMAL-BP trial, have examined blood pressure control following thrombectomy. Meta-analyses showed that intensive BP lowering did not reduce symptomatic hemorrhage and was associated with worse functional outcomes at 3 months. Specifically, lowering BP too aggressively after successful reperfusion could worsen outcomes by reducing perfusion to the ischemic penumbra. Therefore, this study will investigate whether a more targeted blood pressure elevation strategy could improve patient prognosis compared to standard BP control in those with post-thrombectomy systolic BP below 140 mmHg.
This is a prospective, randomized, open-label trial with blinded endpoint assessment (PROBE) design, aimed at comparing intensive and standard BP control strategies in acute ischemic stroke patients. Participants will be randomized 1:1 into either an intensive BP control group (targeting a 20% systolic BP increase, capped at 180 mmHg) or a standard BP control group (systolic BP below 180 mmHg).

Start Date01 Dec 2024

Sponsor / Collaborator

Yonsei University

NCT06635707

/ Not yet recruitingNot ApplicableIIT

The Study on the Efficacy and Safety of Using Urapidil Alone or in Combination With Esmolol for the Treatment of Acute Hypertensive Intracerebral Hemorrhage: A Prospective, Open-label, Observational, Multicenter Research

The objective of this study is to investigate the efficacy and safety of urapidil monotherapy versus the combination of esmolol in treating participants with acute hypertensive intracerebral hemorrhage through a prospective, open-label, observational, multicenter clinical trial, aiming to provide guidance for clinicians in formulating rational treatment plans.

Start Date01 Nov 2024

Sponsor / Collaborator

Qianfoshan Hospital of Shandong Province

CTR20232398

/ CompletedNot Applicable

乌拉地尔缓释胶囊（30mg）在中国健康受试者中空腹和餐后给药条件下随机、开放、单剂量、两序列、两周期、双交叉生物等效性试验

[Translation] A randomized, open-label, single-dose, two-sequence, two-period, double-crossover bioequivalence study of urapidil sustained-release capsules (30 mg) in Chinese healthy subjects under fasting and fed conditions

主要目的：按有关生物等效性试验的规定，选择科研製薬株式会社为持证商的乌拉地尔缓释胶囊（商品名：Ebrantil；规格：30mg）为参比制剂，对石家庄四药有限公司生产的受试制剂乌拉地尔缓释胶囊（规格：30mg）进行空腹和餐后给药人体生物等效性试验，比较受试制剂中药物的吸收速度和吸收程度与参比制剂的差异是否在可接受的范围内，评估两种制剂在空腹和餐后给药条件下的生物等效性。次要目的：观察健康志愿受试者口服受试制剂乌拉地尔缓释胶囊（规格：30mg）和参比制剂乌拉地尔缓释胶囊（商品名：Ebrantil；规格：30mg）的安全性。

[Translation]

Main purpose: According to the regulations on bioequivalence testing, select urapidil sustained-release capsules (trade name: Ebrantil; specification: 30mg) of R&D Manufacturing Co., Ltd. as the licensee as the reference preparation. The test preparation urapidil sustained-release capsules (specification: 30 mg) produced by the company were subjected to human bioequivalence tests when administered on an empty stomach and after meals to compare whether the absorption speed and extent of the drug in the test preparation were different from the reference preparation. The two formulations were evaluated for bioequivalence within the acceptable range under fasting and postprandial dosing conditions. Secondary purpose: To observe the safety of the test preparation urapidil sustained-release capsules (specification: 30mg) and the reference preparation urapidil sustained-release capsules (trade name: Ebrantil; specification: 30mg) taken orally by healthy volunteer subjects.

Start Date29 Aug 2023

Sponsor / Collaborator

Shijiazhuang No. 4 Pharmaceutical Co., Ltd.

100 Clinical Results associated with Urapidil

100 Translational Medicine associated with Urapidil

100 Patents (Medical) associated with Urapidil

1,085

Literatures (Medical) associated with Urapidil

01 Dec 2025·European Journal of Trauma and Emergency Surgery

Urapidil as a neuroprotective agent: targeting hypoxia, inflammation, and oxidative stress in traumatic brain injury

Article

Author: Bindal, Ahmet ; Ozmen, Ozlem ; Imeci, Orhan ; Tepebasi, Muhammet Yusuf ; Sevuk, Mehmet Abdulkadir ; Yildirim, Burak ; Asci, Halil ; Karabacak, Pınar ; Ilhan, Ilter

Abstract:

Purpose:

One of the important causes of morbidity and mortality in the world is traumatic brain injury (TBI), which is a process that triggers damaging mechanisms such as inflammation, oxidative stress, and apoptosis. The results of current pharmaceutical methods are not enough, and researches into new therapy modalities are needed. This study aimed to evaluate the neuroprotective effects of Urapidil (Ura), which is an alpha-1 adrenergic receptor antagonist with serotonergic activity, in a TBI model and investigating signaling pathways like high mobility group box 1 (HMGB1), BCL2-interacting protein 3-like (BNIP3L), and hypoxia-inducible factor-1 alpha (HIF1α).

Methods:

Thirty-two rats were divided into four groups: control, TBI, TBI + Ura0.5 (0.5 mg/kg), TBI + Ura5 (5 mg/kg) groups. Tissue integrity and expressions of tumor necrosis factor-alpha (TNF-α), caspase-3 (Cas-3), tyrosine hydroxylase (TH), HIF1α, BNIP3L, and HMGB1 were assessed. Ura’s biochemical oxidative stress indicators were also assessed.

Results:

Ura treatment at both doses, significantly decreased histopathological findings, BNIP3L, HMGB1, and HIF1α expressions, TNF-α, Cas-3, TH immunexpressions, and TOS and OSI levels, and elevated TAS levels compared to TBI group. These results show that Ura regulates molecular pathways related to TBI, including neuroinflammation, mitochondrial dysfunction, and hypoxia.

Conclusion:

Ura shows promising tissue-protective effects in TBI by targeting inflammation, oxidative stress, and apoptosis. This study provides a new perspective on the need for further development of Ura for therapeutic use.

01 May 2025·British Journal of Pharmacology

α‐Adrenoreceptor blocker phentolamine inhibits voltage‐gated sodium channels via the local anaesthetic binding site

Article

Author: Lampert, Angelika ; Hausmann, Ralf ; Stingl, Julia ; Toklucu, Idil ; Sudha Bhagavath Eswaran, Vishal ; Kesdoğan, Aylin Bilge ; Körner, Jannis ; Gaebler, Arnim Johannes ; Bott, Raya Atlanta

Abstract:

Background and Purpose:

Phentolamine is a non‐selective α‐adrenoreceptor antagonist used to reverse local anaesthesia, for example, during dental procedures when a vasoconstrictor is co‐applied. Phentolamine‐mediated vasodilation leads to faster clearance of injected drugs. Previous electrophysiological studies hypothesized that phentolamine acts as a modulator of voltage‐gated sodium channels, which could conflict with its indication as local anaesthetic reversal agent.

Experimental Approach:

We performed manual and high throughput patch‐clamp recordings on HEK and CHO cells expressing NaV1.7 and NaV1.5. We investigated the effects of phentolamine on sodium channel biophysics and the additive impact of phentolamine on cells preconditioned with the local anaesthetic mexiletine. We used site‐directed mutagenesis, homology modelling and drug docking to identify phentolamine's binding site. We compared the effect on sodium channels with other clinically established α‐adrenoreceptor antagonists.

Key Results:

Phentolamine inhibits NaV1.7 in HEK and CHO cells with an IC50 value of 72 and 57 μM and NaV1.5 in CHO cells with an IC50 of 27 μM. Phentolamine enhances the tonic block induced by the local anaesthetic mexiletine. Phentolamine binds to sodium channels at the local anaesthetic receptor site. The α‐adrenoreceptor antagonists alfuzosin, urapidil and phenoxybenzamine show lower potency on NaV1.5 and NaV1.7 in patch‐clamp recordings.

Conclusions and Implications:

Phentolamine blocks voltage‐gated sodium channels via the local anaesthetic receptor site. This may conflict with its current indication as an antidote for local anaesthetics. We propose alternative α‐adrenoreceptor antagonists as possible candidates for local anaesthetic reversal because these are less potent inhibitors of both cardiac and neuronal voltage‐gated sodium channels.

01 Apr 2025·ECOTOXICOLOGY AND ENVIRONMENTAL SAFETY

Five-month real-ambient PM2.5 exposure impairs learning in Brown Norway rats: Insights from multi omics-based analysis

Article

Author: Zhao, Wenjie ; Xu, Yanfeng ; Xiong, Yi ; Sun, Xiuping ; Han, Yunlin ; Song, Chenchen ; Zhou, Li ; Zhao, Lianlian ; Shan, Shan ; Guo, Jianguo ; Guo, Jindan ; Yang, Hu ; Zhang, Ling ; Zhang, Boxiang

PM_2.5, recognized as a potential pathogenic factor for nervous system diseases, remains an area with many unknowns, particularly regarding its effects on human health. After five-month real-ambient PM_2.5 exposure, we observed no significant pathological damage to the lung, liver, spleen, or kidney tissues. However, PM_2.5 exposure led to neuronal degeneration in the hippocampal CA1 region of Brown Norway (BN) rats. The level of IL-6, IL-13, IL-1β, IL-12, IL-4, GRO/KC, MIP-1α, CM-CSF significantly increased in lung lavage fluid (P < 0.05 for all). Notably, we detected a slight impairment in spatial learning ability, as evidenced by the Barnes maze training outcomes. There were no significant changes in the bacterial community in lung lavage fluid (P = 0.621), but the bacterial community in the gut significantly changed (P < 0.001), with more species identified (P < 0.05). The metabolomic analysis revealed 147 and 149 significantly changed metabolites in the pulmonary system and serum, respectively (P < 0.05). PM_2.5 exposure caused a decrease in Nervonic acid (NA) in both the lung and serum, which likely contributed to spatial learning impairment (P < 0.01). The correlation between lung metabolites, gut bacterial species, and serum metabolites indicated that PM_2.5 exposure likely impaired spatial learning through the lung-gut-brain axis pathway. Lung and serum metabolic disorders and intestinal microbial imbalance occurred in BN rats post-five-month real-ambient PM_2.5 exposure. There were two potential ways that PM_2.5 exposure caused the decline of spatial learning ability in wild-type BN rats: (1) PM_2.5 exposure led to a significant decrease of neuroprotective Nervonic acid in lung and serum metabolites. (2) PM_2.5 exposure likely led to reduced spatial learning ability through the lung-gut-brain axis.

News (Medical) associated with Urapidil

23 Dec 2020

·www.geneonline.com

China’s Hasten Biopharmaceutic Acquires Five Non-Core Assets from Japan’s Takeda

Continuing its divestiture strategy since January 2019, Takeda has planned on releasing non-core assets to focus on creating innovative therapies and developments on Gastroenterology (GI), Rare Diseases, Plasma-Derived Therapies, Oncology, and Neuroscience, the 5 chosen areas that are essential to its long-term growth strategy. After the divestiture with Celltrion in early December, Takeda struck up another deal with Hasten Biopharmaceutic, a company funded by Feidong County of Hefei City, China and established by Ray Capital Management Limited. Takeda is letting go of five prescription drugs, including cardiovascular and metabolism products that are mainly sold in China in exchange for around 322 million. The portfolio of select drugs generated 109.5 million net sales in 2019, mostly contributed by cardiovascular drug Ebrantil, one of the products sold to Hasten. As per the contract, the employees who are dedicated to the commercial support of these products will also be transferred to Hasten. As for the manufacturing and supply agreement, Takeda will continue to manufacture and supply the divested products to Hasten. The agreement is estimated to close by June 30, 2021, and until then, Takeda will have the full right of these products. For future use of proceeds, Takeda will firstly reduce its debt and then facilitate the R&D and expand its manufacturing capacity of these five core business areas. “This announcement marks continued progress on our commitment to simplify our global portfolio and remain focused on investing in our growth drivers, and research and development pipeline,” said Costa Saroukos, Chief Financial Officer, Takeda. “We remain committed to expansion in China with more than 15 planned approvals over the next five years. By continuing to execute and deliver on Takeda’s financial commitments, including paying down debt and focusing on our highly innovative portfolio, we can sustain our long-term growth and continue to deliver life-transforming treatments for patients worldwide.” For the past two years, Takeda has exceeded its $10 billion non-core asset divestiture target. Here are some of the divestiture agreements in 2020. March 2: Sold 30 prescription pharmaceuticals and over-the-counter (OTC) products in Near East, Middle East, and African countries within its Growth and Emerging Markets Business Unit (GEM BU) to Acino for 200 million March 2: Sold 18 select OTC and prescription pharmaceutical assets in Brazil, Mexico, Argentina, Colombia, Ecuador, Panama, and Peru to Hypera Pharma for 825 million March 4: Sold 20 OTC and prescription pharmaceutical products exclusively in Russia, Georgia, and several countries from within the Commonwealth of Independent States to STADA Arzneimittel AG for 660 million. April 24: Sold 110 select OTC and prescription pharmaceutical assets in Europe to Orifarm for 670 million September 8: Sold non-core prescription pharmaceutical products sold predominantly in Europe and Canada to Cheplapharm for 562 million. December 1: Sold 18 pharmaceutical products and OTC products in the Asia Pacific to Celltrion for 278 million.

Acquisition

100 Deals associated with Urapidil

External Link

KEGG	Wiki	ATC	Drug Bank
D01333	Urapidil	C02CA06	DB12661

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Dysuria	Japan	Kaken Pharmaceutical Co., Ltd.	11 Nov 1999
Urination Disorders	Japan	Kaken Pharmaceutical Co., Ltd.	30 Jun 1995
Hypertension	Japan	Kaken Pharmaceutical Co., Ltd.	20 Sep 1988

Clinical Result

Indication

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


ESC2018	Not Applicable	Acute Coronary Syndrome \| Heart Failure \| Hypertension	30	Urapidil treatment group	vngtxrbrjc(pwkwntijgi) = pwqkayhttr fgjmejmaov (hpjfzrogat ) View more	-	26 May 2018
				Nitroglycerin treatment group	vngtxrbrjc(pwkwntijgi) = sqykqqlyeh fgjmejmaov (hpjfzrogat ) View more
2252 (AUA2012)	Not Applicable	Calculus, Ureteral Adjuvant	80	Urapidil (30 mg/day)	dccdhkrazi(hflwrpbhjs) = npcfayvqus mwppxktuop (lcfgyacjng ) View more	Positive	01 Apr 2012
				Placebo	dccdhkrazi(hflwrpbhjs) = qppsfhtfdm mwppxktuop (lcfgyacjng ) View more

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