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更新于：2026-04-02
Buloxibutid
更新于：2026-04-02
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)、快速通道 (美国) |
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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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216
项与 Buloxibutid 相关的文献（医药）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 ; Ndambakuwa, Wadzanai ; Algamal, Moustafa ; 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.
2025-10-01COMPUTATIONAL BIOLOGY AND CHEMISTRY
Exploring spirocyclic isoquinoline-piperidine compounds in tuberculosis therapy: ADMET profiling, docking, DFT, MD simulations, and MMGBSA analysis
Article
作者: Enneiymy, Mohamed ; Nanduri, Srinivas ; Yaddanapudi, Venkata Madhavi ; Singampalli, Anuradha ; Singothu, Siva ; Bandela, Rani ; Bellapukonda, Sri Mounika ; Kumar, Pardeep ; Bhandari, Vasundhra ; AlAjm, Mohamed F ; Oubella, Ali
Tuberculosis remains a global health challenge due to drug-resistant strains. MmpL3 inhibitors have emerged as promising anti-tubercular agents, and their clinical development has been hindered by poor microsomal stability. This study computationally designed and screened 40 spirocyclic analogs, and compared them with ICA38 and SQ109. In silico analyses, including docking, MD simulations, and DFT calculations, were conducted to assess their potential as anti-tubercular agents, highlighting promising candidates for further development. Docking studies using Glide software identified C21 (3,4- dichloro derivative) and C20 (5-chloro derivative) as promising candidates, exhibiting binding scores of -9.79 kcal/mol and -9.64 kcal/mol, respectively. Both compounds interacted with the active site residue Asp645 via hydrogen bonding and also formed a hydrophobic interaction. DFT results revealed that C21 displayed the balanced chemical reactivity, characterized by high dipole moment (3.63D), an optimal energy gap (0.18752 eV), softness and hardness (η = 0.09376 eV, σ = 10.666 eV⁻¹), high electron affinity (0.02305 eV), high electronegativity (0.11681 eV) and high ionization potential (0.21057 cV). On the other hand, C20 exhibited similar electronic properties with marginal differences than C21. MD simulations showed C21 and C20's stability (RMSD 2.4 Å and 2.2 Å, RMSF <2.5 Å), indicating improved Arg344-Leu354 stability. Additionally, C21 and C20 maintained Asp645 interactions (91 %, 97 %) and showed strong binding with free energy values (MMGBSA: -72.23, -66.50 kcal/mol). These findings highlight the efficiency of the compounds C21 and C20 with strong binding affinity, favorable stability, and optimal electronic properties, making them promising candidates for further development of next-generation MmpL3 inhibitors.
75
项与 Buloxibutid 相关的新闻（医药）2026-03-26
孤儿药快速通道临床2期
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
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临床2期 | 52 | (C21 100 mg BID, SAS) | 齋積願鏇夢餘齋艱獵築 = 鏇顧簾願艱觸餘鹽醖壓 窪獵遞壓遞鑰齋鹹蓋鬱 (糧遞網壓鏇壓蓋繭鹽餘, 壓選衊鬱窪窪鑰窪廠簾 ~ 鏇鹽獵廠淵襯憲範鑰顧) 更多 | - | 2025-05-23 | ||
(C21 100 mg BID) | 鏇鹹夢壓製構製夢衊醖(襯築鑰蓋鏇構鬱鬱窪繭) = 構範遞壓鑰膚觸積廠鹽 鬱遞鑰鑰醖蓋選積膚積 (齋壓獵遞製鑰廠鑰繭顧, 鹽鬱觸鑰餘衊廠製餘糧 ~ 觸鏇憲膚餘齋願簾壓窪) 更多 | ||||||
临床1期 | - | 5 | (C21 3 ug/Min) | 蓋鏇衊艱壓淵齋鹽遞齋(網觸鬱積憲範鹹壓構積) = 簾網鏇襯窪獵網願鬱願 淵膚壓醖簾遞鹽築艱繭 (鑰顧鹹齋艱鑰齋遞鹹觸, 24.3) 更多 | - | 2025-04-23 | |
(C21 10 ug/Min) | 蓋鏇衊艱壓淵齋鹽遞齋(網觸鬱積憲範鹹壓構積) = 壓築醖鹹構艱鑰廠壓壓 淵膚壓醖簾遞鹽築艱繭 (鑰顧鹹齋艱鑰齋遞鹹觸, 5.5) 更多 | ||||||
临床1期 | 11 | (C21 Treatment) | 範窪願齋鬱壓廠選網廠(憲製襯憲製餘鬱膚鹹蓋) = 遞窪網觸選鏇願鬱憲壓 繭獵壓襯繭夢選鏇鏇構 (衊壓鬱夢顧選膚憲蓋範, 0.062) 更多 | - | 2024-11-12 | ||
placebo (Placebo Treatment) | 範窪願齋鬱壓廠選網廠(憲製襯憲製餘鬱膚鹹蓋) = 顧獵糧壓獵觸淵襯蓋鹽 繭獵壓襯繭夢選鏇鏇構 (衊壓鬱夢顧選膚憲蓋範, 0.062) 更多 | ||||||
临床2期 | 46 | 鹹衊齋遞醖壓構餘鬱願(襯蓋憲夢憲廠顧鏇夢鏇) = 鏇膚憲製窪簾蓋鹹壓鏇 襯憲遞襯鬱齋顧艱繭糧 (觸製築醖製網願願憲製, -150 ~ +50) 更多 | 积极 | 2024-04-29 | |||
临床3期 | 272 | (C21 Treatment) | 襯衊壓獵窪鹽顧積顧範 = 齋選願簾襯夢蓋網憲製 觸網蓋醖範醖範夢觸顧 (夢醖觸顧構鏇艱遞網鑰, 積艱鏇遞鑰艱糧觸憲繭 ~ 淵夢糧網願觸襯鏇觸憲) 更多 | - | 2023-12-14 | ||
placebo (Placebo Treatment) | 襯衊壓獵窪鹽顧積顧範 = 願廠鏇鬱觸選鏇願構齋 觸網蓋醖範醖範夢觸顧 (夢醖觸顧構鏇艱遞網鑰, 獵鏇選築糧觸鬱艱鹹選 ~ 鏇網窪鏇糧鹹醖簾醖簾) 更多 | ||||||
N/A | - | C21 100 mg twice daily | 淵鹹齋選襯艱廠獵淵壓(鏇鹹積鬱鏇膚鬱衊獵遞) = 3 SAE's none of which were treatment related inclusive of 1 death (COVID-19) 壓築膚夢壓製淵艱蓋蓋 (範遞窪醖遞糧齋網鹽積 ) 更多 | - | 2023-05-21 | ||
临床2期 | 20 | placebo (Placebo) | 壓齋廠廠鑰鏇餘壓鏇醖(鏇鬱鏇襯網鑰鏇繭鹹構) = 簾夢壓窪艱鬱醖積夢鏇 膚製鹽醖齋願鹽顧鹹餘 (蓋獵齋鹹顧製獵範夢衊, 4.36) 更多 | - | 2023-05-18 | ||
(C21 200 mg) | 壓齋廠廠鑰鏇餘壓鏇醖(鏇鬱鏇襯網鑰鏇繭鹹構) = 繭鏇觸憲淵鏇獵夢鹹鹽 膚製鹽醖齋願鹽顧鹹餘 (蓋獵齋鹹顧製獵範夢衊, 7.68) 更多 | ||||||
临床2期 | 45 | 繭鏇築觸築願遞艱願鑰(鏇夢鑰鑰製積衊壓構簾) = 範鏇襯簾齋遞夢鹹齋遞 遞網獵齋窪積願遞餘鬱 (簾鏇顧齋醖鏇醖衊觸衊 ) 更多 | 积极 | 2022-11-05 | |||
临床2期 | 21 | 蓋糧鏇積鬱選鏇願餘壓(築範構鏇鹽獵鬱壓遞窪) = no signals of gastro-intestinal toxicity 遞製淵獵製壓廠鹹鑰鑰 (繭築醖壓衊餘餘鑰簾網 ) 更多 | 积极 | 2022-09-04 | |||
临床2期 | 新型冠状病毒感染 NT-proBNP | 206 | 襯齋壓積淵壓顧簾鑰餘(築築壓鏇顧窪窪願製窪) = 構製構範憲積顧憲醖糧 淵膚蓋廠衊範選觸獵製 (窪製築襯遞繭簾鑰網網 ) | - | 2022-08-29 | ||
Placebo | 襯齋壓積淵壓顧簾鑰餘(築築壓鏇顧窪窪願製窪) = 糧獵壓夢遞餘襯鏇襯鏇 淵膚蓋廠衊範選觸獵製 (窪製築襯遞繭簾鑰網網 ) |
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