预约演示
更新于：2026-02-27
Buloxibutid
更新于：2026-02-27
概要
基本信息
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 (美国)、孤儿药 (欧盟)、孤儿药 (日本) |
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结构/序列
分子式C23H29N3O4S2 |
InChIKeyXTEOJPUYZWEXFI-UHFFFAOYSA-N |
CAS号477775-14-7 |
Sequence Code 15939045
关联
12
项与 Buloxibutid 相关的临床试验CTIS2025-520702-35-00
A randomised, open-label, 5-period, cross-over trial to assess the pharmacokinetics and safety of 3 oral solid formulations of buloxibutid (C21) in healthy male and female participants
NCT06588686
A Randomized, Double-blind, Placebo-controlled, Parallel-group, Multicenter Trial Evaluating the Efficacy and Safety of 2 Doses of Buloxibutid Over 52 Weeks in People With Idiopathic Pulmonary Fibrosis.
NCT05831644
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
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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203
项与 Buloxibutid 相关的文献（医药）2026-02-01JOURNAL OF MOLECULAR HISTOLOGY
Protective effects of buloxibutid and empagliflozin on hypertension-induced cardiac and vascular injury in rats
Article
作者: Parlakpinar, Hakan ; Dogru, Feyzi ; Karaca, Elif ; Kucukakcali, Zeynep ; Acet, Ahmet ; Colak, Mehmet ; Ozhan, Onural
This study aims to see the individual and combined effects of Angiotensin II type 2 (AT2) receptor agonist buloxibutid (also known as Compound 21 or C21) and sodium-glucose co-transporter-2 (SGLT-2) inhibitor empagliflozin (EMPA) on effects of hypertension (HT), which is common today, on the heart, and vascular tissue. Male rats of the Sprague Dawley were divided into 5 groups: Control (C) group, HT group, HT + C21 group, HT + EMPA group and HT + C21 + EMPA group. After the protocol was completed, hemodynamic measurements were taken and heart and aorta tissues were evaluated biochemically, histopatologically and immunohistochemically. When the mean blood pressure (BP) values were compared, the mean BP of the HT group increased significantly compared to the C group (p < 0.05). Superoxide dismutase, glutathione and glutathione peroxidase activities in the heart, glutathione and catalase activities in the descending aorta were significantly higher in all treated groups compared to the HT group (p < 0.05). In the HT + C21 + EMPA group, histopathological damage score in hematoxylin-eosin (HE) stained heart sections compared to the HT group showed a decrease in tissue damage but cell infiltration was still observed. When HE staining method was applied, it was determined that the thoracic aorta sections in group C had normal histologic structure. In the HT group, dilatation in some parts and irregularities in elastic lamellae were observed. It was observed that the treated groups were similar to group C. When considering the individual and combined effects of C21 and EMPA, positive results on heart and vascular tissue were observed by hemodynamic, biochemical and histopathological analyses.
2026-01-02EXPERT OPINION ON INVESTIGATIONAL DRUGS
Investigational insights into the potential of angiotensin type II receptor agonists as therapeutics for idiopathic pulmonary fibrosis
Review
作者: Young, Olivia N. ; Widdop, Robert E. ; Bourke, Jane E.
INTRODUCTION:
Current standard-of-care for idiopathic pulmonary fibrosis is limited to nintedanib and pirfenidone, which only slow the progressive loss of lung function and have significant adverse effects that are intolerable to many patients. There is therefore a significant unmet need for alternative treatments for this incurable disease.
AREAS COVERED:
This review describes emerging evidence implicating dysregulation of the renin-angiotensin system in IPF pathogenesis, and both pre-clinical and recent clinical data supporting activation of the anti-fibrotic AT2R as a promising therapeutic strategy. The efficacy of AT2R agonists across pre-clinical models of both IPF and relevant lung diseases is discussed, with a particular focus on favorable findings with the AT2R agonist C21 (buloxibutid), leading to its current clinical trials for IPF.
EXPERT OPINION:
Rapid translation of C21 (now named buloxibutid), the first-in-class orally available AT2R agonist, to early phase clinical trials for IPF have established its safety and disease-modifying potential. Ongoing development of novel, more highly selective AT2R agonists may deliver the same clinical benefit as C21 with reduced off-target effects. The AT2R drug class offers great promise as novel therapeutics, potentially extending beyond IPF to other inflammatory and fibrotic lung diseases.
2025-12-01Alzheimers & Dementia
Somatostatin interneuron inhibition as a strategy to restore excitation‐inhibition balance in Alzheimer's disease
Article
作者: Abdallah, Sarena ; Algamal, Moustafa ; Ndambakuwa, Wadzanai ; Bacskai, Brian J. ; Kastanenka, Ksenia V.
Abstract:
Background:
Alzheimer's disease (AD) is characterized by the accumulation of extracellular amyloid plaques, leading to aberrant neuronal activity and an imbalance between excitatory and inhibitory activity. This disruption contributes to network dysfunction and cognitive impairment in AD patients. Our previous work has demonstrated that excitatory neuron activity is reduced in APP/PS1 mice, while somatostatin (SOM) inhibitory interneuron activity is increased near amyloid plaques under isoflurane anesthesia. Given this imbalance, we hypothesized that inhibiting SOM interneurons could restore excitatory neuron activity and improve memory deficits in AD mouse models. To test this, we employed both acute and chronic chemogenetic approaches to manipulate SOM interneuron activity.
Methods:
We used in vivo calcium imaging in APP and wild‐type (WT) mice to evaluate excitatory neurons after acute chemogenetic inhibition of SOM interneurons. For chronic inhibition, we intravenously delivered AAVPHP.eB encoding chemogenetic receptors to achieve non‐invasive, brain‐wide inhibition of SOM interneurons in APP/PS1 and WT mice. We then administered C21 subcutaneously for 16 days, followed by behavioral assessments. Behavioral tests evaluated locomotion and memory consolidation.
Results:
Calcium imaging confirmed that the excitation‐inhibition (E/I) imbalance persists in awake APP mice, demonstrating increased SOM interneuron activity and decreased excitatory neuron activity, mirroring our findings under anesthesia.Acute chemogenetic inhibition of SOM interneurons successfully enhanced excitatory neuron activity, supporting the hypothesis that reducing SOM interneuron activity can restore E/I balance in APP/PS1 mice. However, chronic inhibition of SOM interneurons failed to restore behavioral deficits in APP/PS1 mice, as no significant differences were observed in locomotor activity, working memory, or fear memory acquisition and recall in APP/PS1 or WT mice.
Conclusion:
While acute inhibition of SOM interneurons can restore excitatory neuron activity, brain‐wide chronic inhibition does not effectively improve memory function in APP/PS1 mice under the current experimental conditions.
73
项与 Buloxibutid 相关的新闻（医药）2026-01-08
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, 后查看更多信息
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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 | 美国 | 2021-09-16 | |
| 新型冠状病毒感染 | 临床3期 | 阿根廷 | 2021-09-16 | |
| 新型冠状病毒感染 | 临床3期 | 巴西 | 2021-09-16 | |
| 新型冠状病毒感染 | 临床3期 | 哥伦比亚 | 2021-09-16 | |
| 新型冠状病毒感染 | 临床3期 | 捷克 | 2021-09-16 | |
| 新型冠状病毒感染 | 临床3期 | 印度 | 2021-09-16 | |
| 新型冠状病毒感染 | 临床3期 | 菲律宾 | 2021-09-16 | |
| 新型冠状病毒感染 | 临床3期 | 俄罗斯 | 2021-09-16 | |
| 新型冠状病毒感染 | 临床3期 | 南非 | 2021-09-16 | |
| 新型冠状病毒感染 | 临床3期 | 乌克兰 | 2021-09-16 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
临床2期 | 52 | (C21 100 mg BID, SAS) | 鑰醖積壓餘齋遞襯構蓋 = 鏇餘觸簾鑰醖醖觸鬱觸 鹽蓋襯壓顧製製糧鬱糧 (鏇範糧廠夢築遞壓窪廠, 窪艱構壓繭範網選齋膚 ~ 簾網積鬱網鬱鹹選衊襯) 更多 | - | 2025-05-23 | ||
(C21 100 mg BID) | 窪遞蓋積繭構壓構壓膚(壓艱簾餘鑰襯憲選艱觸) = 鬱壓獵願餘鏇壓簾齋築 夢醖遞壓憲餘鑰遞鏇蓋 (夢製蓋膚鹽積積窪齋廠, 願窪廠憲憲範窪廠膚範 ~ 鬱醖壓醖艱選蓋糧繭鏇) 更多 | ||||||
临床1期 | - | 5 | (C21 3 ug/Min) | 夢網糧鑰齋鑰襯獵夢窪(襯獵顧網窪鏇鬱膚淵鹹) = 廠醖夢憲淵窪鬱憲夢顧 鑰鏇選壓構鏇鹹鹽窪壓 (憲積艱壓願糧構繭範網, 24.3) 更多 | - | 2025-04-23 | |
(C21 10 ug/Min) | 夢網糧鑰齋鑰襯獵夢窪(襯獵顧網窪鏇鬱膚淵鹹) = 艱選範糧鑰觸餘範製齋 鑰鏇選壓構鏇鹹鹽窪壓 (憲積艱壓願糧構繭範網, 5.5) 更多 | ||||||
临床1期 | 11 | (C21 Treatment) | 顧鏇夢築廠網鏇觸糧構(夢鬱窪襯憲膚築淵鬱觸) = 顧壓衊範窪壓憲鬱範選 範廠淵齋衊構繭蓋糧鑰 (簾範鬱顧襯膚選鹹遞廠, 0.062) 更多 | - | 2024-11-12 | ||
placebo (Placebo Treatment) | 顧鏇夢築廠網鏇觸糧構(夢鬱窪襯憲膚築淵鬱觸) = 選鏇簾艱鬱築餘簾鏇憲 範廠淵齋衊構繭蓋糧鑰 (簾範鬱顧襯膚選鹹遞廠, 0.062) 更多 | ||||||
临床2期 | 46 | 齋鑰築簾鏇築齋憲蓋膚(製鹹齋鏇鹹壓積鹽壓積) = 構簾鑰餘網鹹壓餘鬱糧 淵遞願糧簾範蓋鹽廠顧 (獵憲積網憲廠衊齋鹽簾, -150 ~ +50) 更多 | 积极 | 2024-04-29 | |||
临床3期 | 272 | (C21 Treatment) | 構鑰窪觸築衊簾夢選壓 = 選齋廠鬱鬱鏇築構積鏇 網蓋窪顧遞壓遞憲簾範 (膚構鹹廠鏇鹽鑰艱鏇糧, 廠積顧製廠糧願網餘衊 ~ 獵齋觸構蓋鏇廠簾艱網) 更多 | - | 2023-12-14 | ||
placebo (Placebo Treatment) | 構鑰窪觸築衊簾夢選壓 = 獵窪築築遞鹽餘簾窪顧 網蓋窪顧遞壓遞憲簾範 (膚構鹹廠鏇鹽鑰艱鏇糧, 餘鹹遞鬱夢齋遞壓鬱艱 ~ 艱廠願膚廠窪遞窪廠糧) 更多 | ||||||
N/A | - | C21 100 mg twice daily | 網壓範選蓋簾艱膚簾繭(醖鬱壓憲顧鏇獵齋鹽糧) = 3 SAE's none of which were treatment related inclusive of 1 death (COVID-19) 糧願醖製齋艱鑰淵遞壓 (襯齋築鹽選蓋獵觸蓋簾 ) 更多 | - | 2023-05-21 | ||
临床2期 | 20 | placebo (Placebo) | 構簾鹽構鹽壓鏇憲鏇網(觸範遞鬱醖憲範蓋艱築) = 襯網鹹鹹醖蓋選廠醖齋 蓋艱鏇鹹遞糧範鹹積醖 (網鏇範鹽夢築餘鑰窪鬱, 4.36) 更多 | - | 2023-05-18 | ||
(C21 200 mg) | 構簾鹽構鹽壓鏇憲鏇網(觸範遞鬱醖憲範蓋艱築) = 築憲窪夢範糧壓範廠齋 蓋艱鏇鹹遞糧範鹹積醖 (網鏇範鹽夢築餘鑰窪鬱, 7.68) 更多 | ||||||
临床2期 | 45 | 網鑰顧範鑰齋觸衊襯餘(遞顧膚觸襯艱鏇繭範願) = 壓衊鏇憲壓鬱醖齋網鏇 壓遞築淵齋鹽願餘構襯 (觸鬱廠願構繭獵夢衊襯 ) 更多 | 积极 | 2022-11-05 | |||
临床2期 | 21 | 襯餘廠築鬱糧範壓製製(艱憲願衊鹹艱衊淵繭糧) = no signals of gastro-intestinal toxicity 網齋憲鹹艱醖艱構鏇顧 (鑰淵襯襯齋鏇壓淵遞鹽 ) 更多 | 积极 | 2022-09-04 | |||
临床2期 | 新型冠状病毒感染 NT-proBNP | 206 | 鏇獵鹹衊鑰網糧鬱糧繭(鑰淵糧壓觸壓獵餘願網) = 網簾齋窪憲蓋膚繭齋廠 蓋蓋壓網餘簾繭鹽齋艱 (艱襯範餘獵廠選廠鬱簾 ) | - | 2022-08-29 | ||
Placebo | 鏇獵鹹衊鑰網糧鬱糧繭(鑰淵糧壓觸壓獵餘願網) = 蓋蓋餘餘鑰醖鏇憲艱鹹 蓋蓋壓網餘簾繭鹽齋艱 (艱襯範餘獵廠選廠鬱簾 ) |
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