(Buloxibutid) - 药物靶点：AT2R_在研适应症：新型冠状病毒感染，特发性肺纤维化，2型糖尿病_专利_临床

概要

基本信息

药物类型

小分子化药

别名

+ [3]

靶点

AT2R

作用机制

AT2R激动剂(血管紧张素II-2型受体激动剂)

治疗领域

感染呼吸系统疾病心血管疾病+ [1]

在研适应症

新型冠状病毒感染特发性肺纤维化2型糖尿病+ [2]

非在研适应症

掌腱膜挛缩症纤维化雷诺病+ [2]

原研机构

Vicore Pharma Holding AB

在研机构

Vicore Pharma AB

Emeriti Bio ABVicore Pharma Holding AB

非在研机构-

最高研发阶段临床3期

首次获批日期-

最高研发阶段(中国)-

特殊审评孤儿药 (欧盟)

序列信息

Sequence Code 15939045

关联

14

项与 Buloxibutid 相关的临床试验

NCT05831644 / Completed临床1期

A Randomized, Double-blind, Placebo-controlled, 2-way Cross-over Trial Evaluating the Effect of C21 on Endothelial Dysfunction and Safety in Subjects With Type 2 Diabetes Mellitus

This trial is a single-centre, randomized, double-blind, placebo-controlled, 2-way cross-over phase 1b trial evaluating the pharmacodynamic effect of C21 on endothelial dysfunction and safety in subjects with type 2 diabetes mellitus (T2DM).

开始日期2023-04-25

申办/合作机构

Vicore Pharma AB

NCT05830799 / Completed临床1期

A Single-centre, Open-label, Fixed-sequence Trial to Evaluate the Impact of C21 on the Exposure of CYP1A2, CYP2C9, CYP3A4 and P-gp Substrates in Healthy Volunteers

This is a single-centre, open-label, fixed-sequence trial to evaluate the impact of C21 on the exposure of CYP1A2, CYP2C9, CYP3A4 and P-gp substrates in healthy volunteers.

开始日期2023-03-29

申办/合作机构

Vicore Pharma AB

NCT05576155 / Active, not recruiting早期临床1期IIT

Sex Differences in the Dilatory Response of Compound 21

When blood pressure changes, Angiotensin II is produced and released into the bloodstream. This substance can make blood vessels smaller (i.e., vasoconstriction) by acting through Angiotensin II type I receptors (AT1R) to increase blood pressure. Or it can increase the diameter of vessels (i.e., vasodilation) through Angiotensin II type II receptors (AT2R) to decrease blood pressure. These two receptors normally work in balance to maintain blood pressure. However, excess Angiotensin II released in the bloodstream may reduce the sensitivity of AT2Rs, leading to excessive activation of AT1Rs. This results in increased constriction which plays a major role in diseases such as high blood pressure, hardening of the arteries, and heart failure. In the body, Angiotensin II production is reduced in the presence of estrogen, as seen in pre-menopausal women. Pre-menopausal women have a greater protection against cardiovascular diseases compared to age-matched males, likely due to the protective effects of estrogen. However, the extent that estrogen may impact the sensitivity of Angiotensin II receptors in pre-menopausal is unknown.
In this study, the investigators use the blood vessels in the skin as a representative vascular bed for examining mechanisms of microvascular dysfunction in humans. Using a minimally invasive technique (intradermal microdialysis for the local delivery of pharmaceutical agents), the blood vessels in a dime-sized area of the skin are studied in healthy young women and men. As a compliment to these measurements, blood is drawn from the subjects and circulating factors that may contribute to cardiovascular health are measured.

开始日期2022-10-03

申办/合作机构

University of Iowa

100 项与 Buloxibutid 相关的临床结果

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100 项与 Buloxibutid 相关的转化医学

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100 项与 Buloxibutid 相关的专利（医药）

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230

项与 Buloxibutid 相关的文献（医药）

2024-06-01·European Journal of Pharmacology

Combining brief recall and ketamine treatment prevents stress-primed methamphetamine memory reinstatement via heightening mPFC GABA activity

Article

作者: Lee, Chi-Pin ; Liao, Yi-Han ; Chan, Ya-Hsuan ; Chin, Min-Han ; Yu, Lung ; Sun, Li-Han

This study aimed to assess whether brief recall of methamphetamine (MA) memory, when combined with ketamine (KE) treatment, may prevent stress-primed MA memory reinstatement. Combining 3-min recall and KE facilitated MA memory extinction and resistance to subsequent stress-primed reinstatement. Such combination also produced glutamate metabotropic receptor 5 (mGluR5) upregulation in animals' medial prefrontal cortex (mPFC) γ-amino-butyric acid (GABA) neuron. Accordingly, chemogenetic methods were employed to bi-directionally modulate mPFC GABA activity. Following brief recall and KE-produced MA memory extinction, intra-mPFC mDlx-Gi-coupled-human-muscarinic-receptor 4 (hM4Di)-infused mice receiving compound 21 (C21) treatment showed eminent stress-primed reinstatement, while their GABA mGluR5 expression seemed to be unaltered. Intra-mPFC mDlx-Gq-coupled-human-muscarinic-receptor 3 (hM3Dq)-infused mice undergoing C21 treatment displayed MA memory extinction and resistance to stress-provoked reinstatement. These results suggest that combining a brief recall and KE treatment and exciting mPFC GABA neuron may facilitate MA memory extinction and resistance to stress-primed recall. mPFC GABA neuronal activity plays a role in mediating brief recall/KE-produced effects on curbing the stress-provoked MA seeking.

2024-03-23·Journal of Biomolecular Structure and Dynamics

Computational investigation of the impact of potential AT ₂ R polymorphism on small molecule binding

Article

作者: Rehman, Md Tabish ; Sharma, Bhanu ; Hussain, Tahir ; Khan, Mohd Azhar ; Jaiswal, Varun ; AlAjmi, Mohamed F ; Shahwan, Moayad

For more than a century, the renin-angiotensin system (RAS) has been acknowledged for playing a crucial part in the physiological control of arterial pressure, as well as sodium and fluid balance. It is now generally acknowledged that one of the receptor of RAS system i.e. angiotensin type 2 receptor (AT2R) functions as a repair system during pathophysiologic circumstances and performs a significant protective role. Efforts have been made previously to design suitable agonist and antagonist molecules to potentially modulate AT2R. One of the agonists and antagonists, named C21 and EMA401, has been studied in a number of pathological conditions. Additionally, a wide panel of single nucleotide polymorphisms (SNPs) has been reported for AT2R, which might potentially affect the efficacy of these molecules. Therefore, computational investigations have been carried out to analyze all the SNPs (1151) reported in NCBI to find potential SNPs affecting the active site of AT2R, as this domain is still unexplored. Structures of these polymorphic forms were modeled, and in silico drug interaction studies with C21 and EMA401 were carried out. The two mutants (rs868939201 and rs1042852794) that significantly affect the binding affinity as that of the wild type were subjected to molecular dynamics simulations. Our analysis of native and mutant AT2R and their complexes with C21 and EMA401 indicated that the occurrence of these mutations affects the conformation of the protein and has affected the binding of these ligand molecules. The study's findings will aid in the development of better, more versatile medications in the near future, and also in vitro and in vivo studies might be planned in accordance with recent findings.Communicated by Ramaswamy H. Sarma.

2024-03-01·Journal of Neurotrauma

Delayed Administration of an Angiotensin II Type 2 Receptor Agonist Promotes Functional Recovery of the Brain and Heart After Traumatic Brain Injury

Article

作者: Liu, Mingqi ; Gao, Chuang ; Dong, Shiying ; Tian, Yu ; Jiang, Weiwei ; Lei, Ping ; Nie, Meng ; Qian, Yu ; Jiang, Rongcai ; Yuan, Jiangyuan ; Liu, Xuanhui

Cardiac injury is a common complication following traumatic brain injury (TBI) that can lead to poor clinical outcomes. Angiotensin II type 2 receptor (AT2R) activation exerts protective roles in the brain and heart, yet its potential impact on TBI or TBI-induced cardiac deficits remains elusive. The goal of this study was to investigate the influence of AT2R activation on recovery after TBI-induced cognitive and cardiac injury using the selective nonpeptide AT2R agonist compound 21 (C21). TBI was induced by cortical impact injury in male adult C57BL/6J mice, and the mice received C21 (0.03 mg/kg, intraperitoneally) starting from 24 h after TBI and continuing once daily. C21 facilitated cognitive function recovery until 1 month after TBI. C21 alleviated blood-brain barrier leakage and brain edema and inhibited the expression of proinflammatory cytokines in the brain after 3 consecutive days of treatment. C21 improved cerebral blood flow after 1 month, although the lesion volume was not affected. C21 also reduced the expression of proinflammatory cytokines in the heart after a 3-day consecutive treatment. Meanwhile, C21 benefited cardiac function, as identified by increased left ventricular ejection fraction 1 month after TBI. In addition, C21 alleviated TBI-induced cardiac hypertrophy and fibrosis; however, blood pressure was not affected. Our results demonstrate that AT2R activation ameliorates TBI-induced neurological and cardiac deficits.

24

项与 Buloxibutid 相关的新闻（医药）

2024-05-14

·BioSpace

Vicore Expands and Strengthens its Board of Directors

STOCKHOLM, SWEDEN / ACCESSWIRE / May 14, 2024 / Vicore Pharma Holding (STO:VICO) Stockholm, May 14, 2024 - Vicore Pharma Holding AB, a clinical-stage biopharmaceutical company unlocking the potential of a new class of drug candidates, angiotensin II type 2 receptor agonists (ATRAGs), is pleased to announce the election of Hans Schikan, PharmD, as the new Chair of the Board of Directors as well as the election of two new Board members, Ann Barbier, MD, PhD and Yasir Al-Wakeel BM, BCh. Hans Schikan has been a member of the Board since 2018 and is a leader in rare disease drug development and strategy. He was previously CEO of Prosensa (Nasdaq: RNA), a company developing therapies for rare diseases including Duchenne muscular dystrophy acquired by BioMarin. He is also co-founder and Vice-Chair of Pharvaris (Nasdaq: PHVS), a clinical stage company developing therapies for the rare disease hereditary angioedema. Prior to Pharvaris and Prosensa, Hans Schikan was an executive at rare disease pioneer Genzyme. He also served on the boards of Wilson Therapeutics (Nasdaq Stockholm: WTX), acquired by Alexion, Therachon, acquired by Pfizer, and VectivBio (Nasdaq: VECT), acquired by Ironwood. "It has been a privilege to serve on the Vicore Board and I am pleased to be taking on an expanded role with the company," said Hans Schikan. "I am looking forward to leading the Board as the company seeks to drive transformational impact for patients suffering from idiopathic pulmonary fibrosis and advance its leadership in angiotensin II pathway biology and drug discovery." Ann Barbier, MD, PhD, has more than 20 years of experience in drug discovery and development in rare diseases, including rare respiratory diseases She previously served as Chief Medical Officer of Translate Bio (Nasdaq: TBIO), a biotechnology company developing drugs for rare respiratory diseases acquired by Sanofi as well as Chief Medical Officer at CAMP4 Therapeutics. "Idiopathic pulmonary fibrosis is a huge unmet medical need and the data generated by the Vicore team to date reflect disease modifying potential for patients who have limited options today," said Ann Barbier. "I am proud to join Vicore's effort to impact this disease and look forward to serving on the Board as the company advances to Phase 2b development of buloxibutid." Yasir Al-Wakeel is a leader in biotech strategic finance and business development. He is currently the CEO of a private biotech company and member of the Maxcyte (Nasdaq: MXCT) board. Yasir Al-Wakeel was previously the Chief Financial Officer and Head of Corporate Development at Kronos Bio (Nasdaq: KRON), Chief Financial and Strategy Officer at Neon Therapeutics (Nasdaq: NTGN), acquired by BioNTech, and Chief Financial Officer and Head of Corporate Development at Merrimack Pharmaceuticals (Nasdaq: MACK), leading its 1 billion USD asset sale to Ipsen. "Vicore's potential therapy for IPF is incredibly promising and I am excited to join the Vicore Board as the company seeks to expand its global footprint as it advances to late-stage development of buloxibutid," said Yasir Al-Wakeel. "I am looking forward to leveraging my experience in both strategic finance and corporate development during this important time for the company." This information was submitted for publication on May 14, 2024, at 08:00 CET. About Vicore Pharma Holding AB (publ) Vicore is an innovative clinical-stage pharmaceutical company unlocking the potential of a new class of drugs with disease-modifying potential. The company is establishing a portfolio in respiratory diseases, including idiopathic pulmonary fibrosis (IPF). Buloxibutid (C21) is a first-in-class orally available small molecule angiotensin II type 2 receptor agonist (ATRAG) currently in phase 2a development for IPF. Almee™ (an investigational medical device in clinical development) is a digital therapeutic based on cognitive behavioral therapy created to address the psychological impact of living with pulmonary fibrosis. Almee has received Breakthrough Device Designation from the FDA, reflecting its potential to have transformative impact. Using its unique expertise in ATRAG chemistry and biology, Vicore is further fueling its pipeline with several new therapies across additional potential indications. The company's shares (VICO) are listed on Nasdaq Stockholm's main market. For more information, see . Attachments Vicore Expands and Strengthens its Board of Directors SOURCE: Vicore Pharma Holding View the original press release on accesswire.com

临床2期高管变更并购

2024-04-12

·BioSpace

Vicore to Present at Upcoming April 2024 Investor Conferences

STOCKHOLM, SE / ACCESSWIRE / April 12, 2024 / Vicore Pharma Holding (STO:VICO) Stockholm, April 12, 2024 - Vicore Pharma Holding AB (publ), unlocking the potential of a new class of drug candidates, angiotensin II type 2 receptor agonists (ATRAGs), today announced participation in the following investor conferences: Kempen Life Sciences Conference Location: Amsterdam, Holland Date: April 16 Company Participants: Hans Jeppsson, CFO, and Bertil Lindmark, CMO Aktiespararna - Digital Temadag - Life Science Location: Virtual Presenter: Mikael Nygård, VP Operations and Corporate Strategy Presentation Date and Time: April 17 at 9:20 AM ET/3:20 PM CET Webcast: This information was submitted for publication on April 12, 2024, at 11:00 CET. About Vicore Pharma Holding AB (publ) Vicore is an innovative clinical-stage pharmaceutical company unlocking the potential of a new class of drugs with disease-modifying potential. The company is establishing a portfolio in respiratory diseases, including idiopathic pulmonary fibrosis (IPF). Buloxibutid (C21) is a first-in-class orally available small molecule angiotensin II type 2 receptor agonist (ATRAG) currently in phase 2a development for IPF. Almee™ (an investigational medical device in clinical development) is a digital therapeutic based on cognitive behavioral therapy created to address the psychological impact of living with pulmonary fibrosis. Almee has received Breakthrough Device Designation from the FDA, reflecting its potential to have transformative impact. Using its unique expertise in ATRAG chemistry and biology, Vicore is further fueling its pipeline with several new therapies across additional potential indications. The company's shares (VICO) are listed on Nasdaq Stockholm's main market. For more information, see . Attachments Vicore to Present at Upcoming Investor Conferences SOURCE: Vicore Pharma Holding View the original press release on accesswire.com

临床2期突破性疗法

2024-03-27

·BioSpace

Vicore Publishes the Annual Report for 2023

STOCKHOLM, SWEDEN / ACCESSWIRE / March 27, 2024 / Vicore Pharma Holding (STO:VICO) Stockholm, March 27, 2024 - Vicore Pharma Holding AB (publ), unlocking the potential of a new class of drug candidates, angiotensin II type 2 receptor agonists (ATRAGs), today announced the publication of the Annual Report for the financial year 2023. The Annual Report for the financial year 2023 is available on the company's website: About Vicore Pharma Holding AB (publ) Vicore is an innovative clinical-stage pharmaceutical company unlocking the potential of a new class of drugs with disease-modifying potential. The company is establishing a portfolio in respiratory diseases, including idiopathic pulmonary fibrosis (IPF). C21 is a first-in-class orally available small molecule angiotensin II type 2 receptor agonist (ATRAG) currently in phase 2a development for IPF. Almee™ (an investigational medical device in clinical development) is a digital therapeutic based on cognitive behavioral therapy created to address the psychological impact of living with pulmonary fibrosis. Using its unique expertise in ATRAG chemistry and biology, Vicore is further fueling its pipeline with several new therapies across additional potential indications. The company's shares (VICO) are listed on Nasdaq Stockholm's main market. For more information, see . This information is information that Vicore Pharma Holding is obliged to make public pursuant to the Securities Markets Act. The information was submitted for publication, through the agency of the contact persons set out above, at 2024-03-27 08:00 CET. Attachments Vicore Annual Report 2023 SOURCE: Vicore Pharma Holding View the original press release on accesswire.com

临床2期

100 项与 Buloxibutid 相关的药物交易

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研发状态

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
新型冠状病毒感染	临床3期	菲律宾	Vicore Pharma AB	2021-09-16
新型冠状病毒感染	临床3期	-	Vicore Pharma AB	2021-09-16
新型冠状病毒感染	临床3期	哥伦比亚	Vicore Pharma AB	2021-09-16
新型冠状病毒感染	临床3期	美国	Vicore Pharma AB	2021-09-16
新型冠状病毒感染	临床3期	印度	Vicore Pharma AB	2021-09-16
新型冠状病毒感染	临床3期	南非	Vicore Pharma AB	2021-09-16
新型冠状病毒感染	临床3期	阿根廷	Vicore Pharma AB	2021-09-16
新型冠状病毒感染	临床3期	巴西	Vicore Pharma AB	2021-09-16
新型冠状病毒感染	临床3期	捷克	Vicore Pharma AB	2021-09-16
新型冠状病毒感染	临床3期	乌克兰	Vicore Pharma AB	2021-09-16

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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


NCT04452435 (ATTRACT, ESC2022)	临床2期	新型冠状病毒感染 NT-proBNP	206	C21	(遞簾簾餘簾鏇選蓋餘齋) = 鏇範積窪範齋鹹衊淵積構廠範願繭鬱齋醖顧淵 (願鏇築簾壓齋繭鹹積壓 )	-	2022-08-29
				Placebo	(遞簾簾餘簾鏇選蓋餘齋) = 顧願鏇簾願願網廠積餘構廠範願繭鬱齋醖顧淵 (願鏇築簾壓齋繭鹹積壓 )
AIR (ERS2022)	临床2期	特发性肺纤维化	21	C21 100 mg	醖積鏇網鹹鏇淵顧積遞(糧構夢壓製製艱獵積觸) = no signals of gastro-intestinal toxicity 糧製網壓遞鹽夢鹹壓願 (遞範製艱艱窪簾構膚窪 ) 更多	积极	2022-09-04
NCT04533022 (AIR, Corporate Publications) 人工标引	临床2期	特发性肺纤维化	45	C21	(鑰製糧窪壓餘鏇鏇獵餘) = 顧膚夢遞鏇膚鹽遞衊壓壓齋襯鬱齋壓網夢膚糧 (糧壓構餘網齋簾蓋選餘 ) 更多	积极	2022-11-05
NCT04533022 (AIR, ATS2024) 人工标引	临床2期	特发性肺纤维化	46	Buloxibutid	(願壓繭築夢淵衊願鏇廠) = 鹽醖願夢獵構繭鬱簾廠簾夢艱鏇齋獵鹹鹽蓋鬱 (顧鹹簾觸壓醖築網鑰顧 ) 更多	积极	2024-04-29
ISC2015	N/A	再灌注损伤	16	Compound 21	鹹糧膚艱鏇艱窪網築觸(構醖衊餘鹹簾蓋築觸獵) = 糧鹽積餘構觸憲糧廠餘願築壓製窪簾獵遞觸遞 (窪鑰鏇顧鏇製憲憲構壓 )	-	2015-02-01
				Saline	鹹糧膚艱鏇艱窪網築觸(構醖衊餘鹹簾蓋築觸獵) = 糧鏇築製淵壓範製選窪願築壓製窪簾獵遞觸遞 (窪鑰鏇顧鏇製憲憲構壓 )
NCT04452435 (ATTRACT, Pubmed) 人工标引	临床2期	新型冠状病毒感染	106	C21	(願網襯憲積製願遞鹽夢) = 觸窪糧觸衊顧餘壓範繭積窪夢蓋獵淵壓淵憲範 (遞鹹願膚簾簾積衊衊夢 )	积极	2021-11-01
				Placebo	(願網襯憲積製願遞鹽夢) = 衊製廠齋壓願壓遞築築積窪夢蓋獵淵壓淵憲範 (遞鹹願膚簾簾積衊衊夢 )
NCT04388176 (Pubmed)	临床2期	雷诺病	20	C21 (200mg)	鹽膚願膚醖淵蓋遞簾獵(襯鏇範餘艱獵鑰網遞鑰) = 繭鹹鏇鬱憲壓範簾壓觸鹽範願觸淵壓襯範製顧 (衊糧壓鑰獵鹽鑰衊蓋鬱 ) 更多	积极	2022-07-27
				Placebo	鹽膚願膚醖淵蓋遞簾獵(襯鏇範餘艱獵鑰網遞鑰) = 製壓構範獵糧衊齋糧憲鹽範願觸淵壓襯範製顧 (衊糧壓鑰獵鹽鑰衊蓋鬱 ) 更多
NCT04452435 (ATTRACT, PRNewswire) 人工标引	临床2期	新型冠状病毒感染	106	C21	(簾願構簾憲選壓夢築淵) = Although the primary endpoint (reduction in CRP) was not different between C21 and placebo treated patients after seven days of treatment, 襯願壓網鏇觸鬱鏇鑰鬱 (齋選鏇夢淵鏇醖壓製醖 ) 更多	积极	2021-10-25
				Placebo
NCT04388176 (CTgov)	临床2期	系统性硬皮病 \| 视网膜色素变性	20	placebo (Placebo)	(簾遞夢積獵網膚鑰襯範) = 夢夢鹹襯鑰糧獵鏇膚築夢願艱鬱積願鏇願鹹蓋 (憲範網簾壓製廠顧鏇鏇, 鏇簾廠憲蓋廠簾餘淵壓 ~ 築蓋積鏇積鹹選網築遞) 更多	-	2023-05-18
				C21 (C21 200 mg)	(簾遞夢積獵網膚鑰襯範) = 鏇顧夢齋憲範廠艱膚簾夢願艱鬱積願鏇願鹹蓋 (憲範網簾壓製廠顧鏇鏇, 夢窪壓鹽構鹹選鹽遞齋 ~ 築糧製醖網醖積廠窪淵) 更多
NCT04880642 (CTgov)	临床3期	新型冠状病毒感染	272	C21 (C21 Treatment)	淵糧鏇窪膚鹽製蓋齋網(餘繭遞蓋壓夢齋獵鹹艱): Hazard Ratio (HR) = 0.98 (95.0% CI, 0.4 ~ 2.36) 更多	-	2023-12-14
				placebo (Placebo Treatment)