维贝格龙(Vibegron) - 药物靶点：β3-adrenergic receptor_在研适应症：膀胱过度活动症综合征，尿频，急迫性尿失禁_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Vibegron (JAN/USAN)、KRP-114V、MK-4618

+ [8]

靶点

β3-adrenergic receptor

作用机制

β3-adrenergic receptor激动剂(β3-肾上腺素能受体激动剂)

治疗领域

泌尿生殖系统疾病

在研适应症

膀胱过度活动症综合征尿频急迫性尿失禁+ [3]

非在研适应症

内分泌系统疾病高血压肠易激综合征+ [1]

原研机构

Merck & Co., Inc.

在研机构

Pierre Fabre SAPierre Fabre Médicament SASUrovant Sciences Ltd.

+ [6]

非在研机构

Merck & Co., Inc.

Merck Sharp & Dohme Corp.Merck GmbH

+ [1]

最高研发阶段批准上市

首次获批日期

日本 (2018-09-21),

膀胱过度活动症

最高研发阶段(中国)临床3期

特殊审评-

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结构

分子式C26H28N4O3

InChIKeyDJXRIQMCROIRCZ-XOEOCAAJSA-N

CAS号1190389-15-1

关联

35

项与维贝格龙相关的临床试验

NCT06438861 / Not yet recruitingN/AIIT

Exploring the Additive Effect of Vibegron to Intradetrusor OnabotulinumtoxinA in Women With Refractory Overactive Bladder

Defined by the International Continence Society (ICS) as urinary "urgency, with or without urge incontinence, usually with frequency and nocturia", overactive bladder (OAB) presents as challenging syndrome to treat. OAB is a very prevalent condition, affecting between 11.8% to 16% of the population with equal impact on women and men and growing prevalence with age. OAB is associated with a significant financial burden to both patients and the health care system with a estimated cost of US $82.6 billion in 2020. Traditionally, a stepwise approach has been taken in managing OAB; starting first with lifestyle modifications, followed by anticholinergic or beta-3-agonist medications as the second line, and lastly, intradetrusor onabotulinumtoxinA injections, percutaneous tibial nerve stimulation (PTNS), and sacral neuromodulation (SNM) as third line options. Given the limitations of this stepwise approach in patients with refractory OAB, combination therapy offers patients an increasing number of treatment options but the literature surrounding the efficacy of combination therapy is somewhat limited. A 2019 systematic review revealed there were only 32 studies in the current OAB literature that explored the role of combination therapy, and the majority of these studies examined the effect of lifestyle modifications with another intervention strategy, highlighting an untapped area of research5.
To date, there has only been a single pilot study conducted in Taiwan examining the effect of intradetrusor onabotulinumtoxinA injections with the addition of mirabegron for patients with refractory OAB. This study by Wang et al. explored the therapeutic impact of adding either an anticholinergic, solifenacin, or a beta-3 agonist, mirabegron, to intradetrusor onabotulinumtoxinA injections as compared to each other as well as patients receiving onabotulinumtoxinA alone. Ninety patients were enrolled with 30 patients allocated to the solifenacin arm, 31 to the mirabegron arm, and 29 to the control group. While the baseline data among the three arms was comparable, the percentage of OAB wet in the mirabegron plus onabotulinumtoxinA group was significantly less at 3-, 6-, 9-, and 12-month intervals than the solifenacin plus onabotulinumtoxinA and the onabotulinumtoxinA alone groups. While this pilot study reveals the potential additive benefit of a beta-3 agonist to intradetrusor onabotulinumtoxinA, no further studies have been performed to date and there are no studies regarding the additive benefit of vibegron, which has a more tolerable side effect profile and is not as limited by as many contraindications as mirabegron. If vibegron can potentiate the effect of intradetrusor onabotulinumtoxinA, this presents a new treatment strategy for OAB and could offer patients an additional line of therapy before having to pursue more invasive and costly management option of sacral neuro modulation.

开始日期2024-09-01

申办/合作机构

The University of Alabama at Birmingham

NCT06417177 / Not yet recruiting早期临床1期IIT

Impact of Early Aging and Menopause on the Vascular Responses to Hypoxia

The purpose of this study is to examine hypoxic vasodilation and the role of beta-adrenergic receptors in younger premenopausal, perimenopausal, and older postmenopausal women.

开始日期2024-06-01

申办/合作机构

University of Missouri

JPRN-jRCT1011230058 / SuspendedN/A

Comparison of efficacy and safety of tamsulosinand vibegron for male lower urinary tract symptoms-Multicenter randomized crossover study- - ALPHABET study

开始日期2024-01-26

申办/合作机构-

100 项与维贝格龙相关的临床结果

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100 项与维贝格龙相关的转化医学

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100 项与维贝格龙相关的专利（医药）

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94

项与维贝格龙相关的文献（医药）

2024-03-01·Journal of pharmaceutical and biomedical analysis

Simultaneous quantification of mirabegron and vibegron in human plasma by HPLC-MS/MS and its application in the clinical determination in patients with tumors associated with overactive bladder

Article

作者: Cheng, Mengting ; Lou, Yutao ; Zhang, Yuan ; Lin, Sisi ; Bao, Meihua ; Qin, Hui ; Li, Kening ; Zhang, Yiwen ; Cao, Qin

Mirabegron and vibegron, both newly identified beta-3 adrenergic agonists, have significantly improved the quality of life for patients suffering from overactive bladder. In order to comprehensively assess the plasma exposure levels of these agents, the development of a rapid and highly sensitive bioanalytical method becomes imperative. The primary objective of this study was to establish a robust high-performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) method for the concurrent quantification of mirabegron and vibegron in human plasma. The analytes were extracted from a 100 μL plasma sample through protein precipitation, employing 300 μL of methanol. Subsequently, samples underwent separation and quantification using a Waters XBridge C₁₈ column (2.1 × 100 mm, 3.5 µm), with a mobile phase consisting of 0.1% formic acid in water and 0.1% formic acid in acetonitrile. The mass analysis was conducted using positive electrospray ionization (ESI+) operated in a multiple reaction monitoring (MRM) mode. The proposed method was meticulously validated in accordance with the guidelines set forth by the U.S. Food and Drug Administration (FDA) for bioanalytical method validation. The regression equations demonstrated exceptional linearity for both mirabegron (r² ≥ 0.994) and vibegron (r² ≥ 0.996) across the concentration range of 0.5 - 200 ng/mL. Furthermore, the assay exhibited accuracy (inter-day relative error ≤ 6.90%) and precision (inter-day coefficient of variation ≤ 8.88%). The average recoveries of the analytes were found to range from 81.94% to 102.02%, with mean matrix effects falling within the range of 89.77% to 110.58%. As a result, this method was deemed highly suitable for the precise determination of the concentrations of both mirabegron and vibegron in the context of therapeutic drug monitoring and bioequivalence studies.

2023-12-01·Cureus

Chronic Penile Pain: A Poorly Researched and Managed Life-Debilitating Condition

作者: Bailon, Rachel ; Trammel, Sabrina ; Huang, Jing ; Shah, Nishma

Chronic penile pain is a complex clinical entity with limited diagnostic criteria and treatment options. Due to limited reporting of these cases, there are no clear clinical treatments and indications for when these patients present to the clinic. This case report will highlight the diagnostic challenges encountered and the subsequent management strategies employed while working up a patient with penile pain. We present a 37-year-old male with a six-year history of debilitating penile pain, urinary frequency, and urgency that is exacerbated by sexual arousal and touch. Initial evaluations attributed the symptoms to medication side effects, leading to medication changes. Despite multiple treatments, including gabapentin, solifenacin, vibegron, and a variety of specialist consultations, the patient's condition persisted. Neurological evaluation revealed pudendal neuropathy. Medical management with pudendal nerve blocks and gabapentin did not provide lasting relief, so surgical interventions were considered. Subsequent treatment with an InterStim II device (Medtronic Inc., Minneapolis, MN) initially resulted in significant symptom improvement. Unfortunately, at the seven-month follow-up, his pain returned. Further evaluation and additional treatment options are currently under consideration. This case report highlights the diagnostic complexity and limited treatment options for chronic penile pain. It suggests that sacral neuromodulation, although lacking long-term data, may offer temporary relief in cases refractory to medical therapy. Further research is needed to enhance our understanding and management of this challenging condition.

2023-11-02·Expert review of clinical pharmacology

Clinical pharmacology of β-3 adrenergic receptor agonists for cardiovascular diseases

Article

作者: Balligand, Jean-Luc ; Michel, Lauriane Y M

INTRODUCTION:

Few agonists of the third isotype of beta-adrenergic receptors, the β3-adrenoreceptor, are currently used clinically, and new agonists are under development for the treatment of overactive bladder disease. As the receptor is expressed in human cardiac and vascular tissues, it is important to understand their beneficial (or adverse) effect(s) on these targets.

AREAS COVERED:

We discuss the most recent results of clinical trials testing the benefit and safety of β3-adrenoreceptor activation on cardiovascular outcomes in light of current knowledge on the receptor biology, genetic polymorphisms, and agonist pharmacology.

EXPERT OPINION:

While evidence from small clinical trials is limited so far, the β3-agonist, mirabegron seems to be safe in patients at high cardiovascular risk but produces benefits on selected cardiovascular outcomes only at higher than standard doses. Activation of cardiovascular β3-adrenoreceptors deserves to be tested with more potent agonists, such as vibegron.

47

项与维贝格龙相关的新闻（医药）

2024-07-01

·Firstwordpharma

EU okays Pierre Fabre’s Obgemsa to treat overactive bladder symptoms

The European Commission approved Pierre Fabre Laboratories’ Obgemsa (vibegron) for the symptomatic treatment of overactive bladder (OAB) syndrome in adults, more than three years after being cleared by the FDA. The decision follows a positive stance adopted by the European Medicines Agency's (EMA) drug advisory body in April. Eric Ducournau, CEO of Pierre Fabre said the approval “will allow European patients to benefit from a new therapeutic option for OAB,” which is estimated to affect more than 70 million people in the region. The approval was backed by findings from the Phase III EMPOWUR trial and a 52-week extension study, which showed that the 75-mg daily dose of Gemtesa significantly improved urgency, increased urination frequency, and urge urinary incontinence in patients with OAB compared with placebo.In 2022, Pierre Fabre gained an exclusive license to commercialise vibegron in the EU from Sumitomo Pharma’s subsidiary Urovant Sciences, which markets it as Gemtesa in the US. The once-daily oral drug is also approved to treat symptoms of OAB in Japan and South Korea under the name Beova, where it is marketed by Kyorin Pharmaceutical and JEIL Pharmaceutical, respectively.

临床3期上市批准引进/卖出临床结果

2024-06-28

·美通社

Pierre Fabre Laboratories宣布授予OBGEMSA™ （ vibegron ）膀胱过度活跃的欧洲上市许可。

法国卡斯特尔 2024年6月29日 /美通社/ -- 欧盟委员会（ EC ）已授权Pierre Fabre Laboratories销售OBGEMSA™ （ vibegron ），用于对症治疗成人膀胱过度活跃综合征，这是一种特别令人衰弱的疾病，影响着欧洲7000多万患者*。 2022年， Pierre Fabre Laboratories从Urovant Sciences Gmbh获得了vibegron的独家许可，用于在欧洲经济区注册和商业化这种创新的治疗方法。欧盟委员会的决定将适用于所有欧盟成员国以及冰岛、列支敦士登和挪威。 OBGEMSA™是Urovant Sciences拥有的商标。 PDF - https://mma.prnewswire.com/media/2451098/Pierre_Fabre.pdf " 我们对这一发展感到高兴，这将使欧洲患者受益于膀胱过度活跃综合征的新治疗选择，并进一步加强我们 40 多年的泌尿外科专业知识。这一决定证实了 Pierre Fabre Laboratories 致力于为患者提供创新的治疗方法，以更好地管理慢性衰弱性疾病， "Pierre Fabre Laboratories首席执行官Eric Ducournau 说。欧盟委员会的决定遵循欧洲药品管理局（ EMA ）人用药品委员会（ CHMP ）于4月25日发布的赞成意见。它是基于在膀胱过度活动症状的成年人中进行的两项关键性、多中心、双盲、随机3期研究的结果。研究RVT-901-3003 （ EMPOWUR ）评估了振子（剂量为每天75 mg ）在12周内与安慰剂和托特罗定作为阳性对照相比的有效性、耐受性和安全性。其扩展，研究RVT-901-3004 （ EMPOWUR扩展），以托特罗定为活性对照药，在52周内双盲评估了振子的长期安全性、耐受性和有效性。在这些研究中， vibegron作为β-3肾上腺素能受体（增强现实（ AR ））的新型选择性激动剂，在过度活动性膀胱综合征患者中可能发生的紧急性、排尿频率增加和尿急性尿失禁（ UUI ）的对症治疗中显示出良好的获益-风险曲线。联系人： Laurence MARCHAL laurence.marchal@pierre-fabre.com

临床3期申请上市临床成功

2024-06-28

·PRNewswire

Pierre Fabre Laboratories announce granting of European marketing authorization for OBGEMSA™ (vibegron) in overactive bladder.

CASTRES, France, June 28, 2024 /PRNewswire/ -- The European Commission (EC) has authorized the marketing of OBGEMSA™ (vibegron) by Pierre Fabre Laboratories for the symptomatic treatment of overactive bladder syndrome in adults, a particularly debilitating condition affecting over 70 million patients* in Europe. In 2022, Pierre Fabre Laboratories acquired the exclusive license for vibegron from Urovant Sciences Gmbh for the registration and commercialization of this innovative treatment in the European Economic Area. The decision of the EC will be applicable to all EU member states as well as Iceland, Liechtenstein, and Norway. OBGEMSA™ is a trademark owned by Urovant Sciences. Continue Reading View PDF Pierre Fabre Laboratories announce granting of European marketing authorization for OBGEMSA™ (vibegron) in overactive bladder. "We are delighted with this development, which will allow European patients to benefit from a new therapeutic option for overactive bladder syndrome and further strengthen our expertise of over 40 years in urology. This decision confirms Pierre Fabre Laboratories' commitment to offering patients innovative therapies that provide better management of chronic debilitating diseases," said Eric Ducournau, CEO of Pierre Fabre Laboratories. The decision of the EC follows the favorable opinion issued on April 25 by the Committee for Medicinal Products for Human Use (CHMP) of the European Medicines Agency (EMA). It is based on the results of two pivotal, multicenter, double-blind, randomized phase 3 studies in adults with overactive bladder symptoms. Study RVT-901-3003 (EMPOWUR) evaluated the efficacy, tolerability, and safety of vibegron (at a dose of 75 mg per day) over 12 weeks compared to placebo and with tolterodine as a positive control. Its extension, study RVT-901-3004 (EMPOWUR Extension), double-blindly evaluated the long-term safety, tolerability, and efficacy of vibegron over 52 weeks, with tolterodine as an active comparator. In these studies, vibegron, as a new selective agonist of beta-3 adrenergic receptors (AR), demonstrated a favorable benefit-risk profile in the symptomatic treatment of urgency, increased frequency of urination, and urge urinary incontinence (UUI) that can occur in patients with overactive bladder syndrome. Contact: Laurence MARCHAL [email protected] PDF - Logo -

临床结果上市批准引进/卖出临床3期

100 项与维贝格龙相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D10433	-	G04BD	DB14895

研发状态

批准上市

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
膀胱过度活动症综合征	欧盟	Pierre Fabre Médicament SAS	2024-06-28
膀胱过度活动症综合征	冰岛	Pierre Fabre Médicament SAS	2024-06-28
膀胱过度活动症综合征	列支敦士登	Pierre Fabre Médicament SAS	2024-06-28
膀胱过度活动症综合征	挪威	Pierre Fabre Médicament SAS	2024-06-28
尿频	美国	Urovant Sciences, Inc.	2020-12-23
急迫性尿失禁	美国	Urovant Sciences, Inc.	2020-12-23
膀胱过度活动症	日本	KYORIN Pharmaceutical Co., Ltd.	2018-09-21
膀胱过度活动症	日本	Kissei Pharmaceutical Co., Ltd.	2018-09-21

未上市

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适应症	最高研发状态	国家/地区	公司	日期
神经源性逼尿肌过度活动	临床3期	美国	Urovant Sciences Ltd.	2022-10-12
前列腺增生症	临床3期	美国	Urovant Sciences Ltd.	2019-03-26
前列腺增生症	临床3期	比利时	Urovant Sciences Ltd.	2019-03-26
前列腺增生症	临床3期	加拿大	Urovant Sciences Ltd.	2019-03-26
前列腺增生症	临床3期	匈牙利	Urovant Sciences Ltd.	2019-03-26
前列腺增生症	临床3期	立陶宛	Urovant Sciences Ltd.	2019-03-26
前列腺增生症	临床3期	波兰	Urovant Sciences Ltd.	2019-03-26
前列腺增生症	临床3期	葡萄牙	Urovant Sciences Ltd.	2019-03-26
前列腺增生症	临床3期	西班牙	Urovant Sciences Ltd.	2019-03-26
疼痛	临床2期	美国	Urovant Sciences Ltd.	2019-01-23

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临床结果

适应症

分期

评价

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT03902080 (URO-901-3005, PRNewswire) 人工标引	临床3期	膀胱过度活动症	-	Vibegron 75mg (GEMTESA)	衊窪憲簾製衊顧鹽夢築(壓遞糧製襯製網鬱壓齋) = 選醖艱簾壓範鹽窪鏇鬱淵觸鏇窪願鹽構襯範製 (糧淵廠壓艱憲襯構鬱構, 0.109) 更多	积极	2024-05-07
NCT03492281 (EMPOWUR, Pubmed) 人工标引	临床3期	膀胱过度活动症	922	Vibegron	製繭繭獵醖壓構廠範憲(簾選鑰淵窪夢憲簾鏇顧): difference = -0.5 (95% CI, -0.8 ~ -0.2) 更多	积极	2022-11-21
				Placebo
AUA2022	N/A	膀胱功能障碍 \| 脊柱裂辅助	19	Vibegron	構願獵獵壓鹽鹹鹹觸餘(齋積鏇繭網襯構獵鏇選) = 築膚繭襯憲鬱蓋襯淵餘簾網願膚選構襯構積淵 (艱鹹壓醖獵顧簾鑰鬱繭 )	-	2022-05-01
				Antimuscarinic therapy	構願獵獵壓鹽鹹鹹觸餘(齋積鏇繭網襯構獵鏇選) = 憲膚製夢膚簾遞繭觸獵簾網願膚選構襯構積淵 (艱鹹壓醖獵顧簾鑰鬱繭 )
NCT03492281 (EMPOWUR, Pubmed \| Adv Ther) 人工标引	临床3期	膀胱过度活动症	-	vibegron	憲壓觸糧醖鹽鹽淵構醖(夢願糧積衊簾選顧範醖) = 遞襯繭鹹鏇衊鹽簾襯鏇鹹窪餘積願鹽範壓觸繭 (鏇鏇繭遞醖淵淵鹹襯壓 ) 更多	积极	2021-12-18
				Placebo	憲壓觸糧醖鹽鹽淵構醖(夢願糧積衊簾選顧範醖) = 齋鑰鑰鏇糧廠襯獵製廠鹹窪餘積願鹽範壓觸繭 (鏇鏇繭遞醖淵淵鹹襯壓 ) 更多
NCT03806127 (CTgov)	临床2期	肠易激综合征	222	Placebo (Placebo)	醖壓壓遞窪餘壓醖積構(獵齋窪鹹鑰廠衊製鏇網) = 顧醖餘蓋積艱鹹襯範構壓憲構製衊壓餘網積鹽 (窪繭構選鏇鬱膚範網艱, 膚獵衊獵鹹觸鬱積艱夢 ~ 鹽憲願窪築夢願廠範鹽) 更多	-	2021-07-30
				Vibegron (Vibegron 75 mg)	醖壓壓遞窪餘壓醖積構(獵齋窪鹹鑰廠衊製鏇網) = 獵憲鏇觸遞夢鹹繭廠壓壓憲構製衊壓餘網積鹽 (窪繭構選鏇鬱膚範網艱, 壓艱鏇鑰艱齋夢齋獵繭 ~ 選衊遞顧壓餘網齋鏇衊) 更多
NCT03583372 (Pubmed \| J Urol) 人工标引	临床3期	膀胱过度活动症	506	vibegron	簾壓衊憲廠鹹窪淵築構(範壓簾壓觸積艱餘鏇艱) = 願獵範艱選鏇選構構觸範壓網製簾鑰廠願壓餘 (願鹹製憲衊鹽壓艱鑰積 ) 更多	积极	2021-05-01
				tolterodine	選壓選製齋製糧蓋艱襯(艱獵築夢夢積網廠繭憲) = 醖襯顧淵鏇廠簾蓋遞構膚襯衊鬱範築窪襯艱艱 (願餘夢窪繭壓艱膚淵簾 ) 更多
NCT03492281 (EMPOWUR, CTgov)	临床3期	膀胱过度活动症	1,530	placebo (Placebo)	築蓋鹹餘顧顧齋製網鑰(選窪鏇鹹壓淵積壓壓願) = 憲鹽壓顧願觸鬱鏇鹹製膚願鏇獵繭觸網觸網廠 (膚製簾鬱簾蓋觸範艱願, 淵鹽鏇艱築壓積憲簾齋 ~ 積築衊艱鏇積襯選顧鬱) 更多	-	2021-03-04
				Vibegron (Vibegron 75 mg)	築蓋鹹餘顧顧齋製網鑰(選窪鏇鹹壓淵積壓壓願) = 憲襯壓遞願鏇築醖鹹襯膚願鏇獵繭觸網觸網廠 (膚製簾鬱簾蓋觸範艱願, 蓋鏇夢製齋構襯窪鏇構 ~ 鹹繭顧餘繭製衊積憲獵) 更多
NCT03583372 (CTgov)	临床3期	膀胱过度活动症	506	Vibegron (Overall Vibegron 75 mg)	範艱構繭蓋築膚淵製積(齋製簾繭鑰範顧窪餘簾) = 鹹獵衊構夢壓膚衊網齋範鹹選鏇鹽範繭遞醖顧 (獵繭範壓遞製構觸選獵, 構夢獵夢蓋鏇蓋簾觸齋 ~ 遞獵淵夢蓋齋廠壓襯餘) 更多	-	2021-02-03
				Tolterodine (Overall Tolterodine ER 4 mg)	範艱構繭蓋築膚淵製積(齋製簾繭鑰範顧窪餘簾) = 壓窪齋築襯齋襯衊簾鏇範鹹選鏇鹽範繭遞醖顧 (獵繭範壓遞製構觸選獵, 遞淵壓繭獵製繭艱觸築 ~ 選簾衊鹽艱夢蓋範觸築) 更多
NCT03492281 (EMPOWUR, Pubmed \| Drugs Aging)	临床3期	膀胱过度活动症	1,463	Vibegron 75 mg	鹽窪繭積遞鏇獵積鹹選(遞糧淵獵糧夢淵艱齋願) = 觸構鑰夢鑰鹽衊艱繭鹽鹹鹽鑰簾鹹鬱襯蓋願衊 (衊鹽衊顧選鹹鬱憲夢繭 )	-	2021-02-01
				Placebo	鹽窪繭積遞鏇獵積鹹選(遞糧淵獵糧夢淵艱齋願) = 糧鬱遞襯製襯艱願範蓋鹹鹽鑰簾鹹鬱襯蓋願衊 (衊鹽衊顧選鹹鬱憲夢繭 )