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更新于：2026-01-27
Zibotentan
齐泊腾坦
更新于：2026-01-27
概要
基本信息
原研机构 |
权益机构- |
最高研发阶段临床2期 |
首次获批日期- |
最高研发阶段(中国)临床申请批准 |
特殊审评- |
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结构/序列
分子式C19H16N6O4S |
InChIKeyFJHHZXWJVIEFGJ-UHFFFAOYSA-N |
CAS号186497-07-4 |
关联
33
项与 齐泊腾坦 相关的临床试验NCT06715670
A Phase I, Randomized, Open-label, Single-dose, Four-period, Four-treatment, Cross-over Study to Assess the Pharmacokinetics of Zibotentan in Healthy Non-Asian and Japanese Participants
NCT06269484
A Multicentre, Randomised, Double-blind, Placebo-controlled Study to Evaluate the Safety of Zibotentan/Dapagliflozin in Combination Compared to Zibotentan Monotherapy, Zibotentan/Dapagliflozin and Zibotentan Monotherapy Compared to Placebo in Participants With Cirrhosis
NCT05516498
A Two Part Phase IIa/b Multicentre, Randomised, Double-Blind, Placebo-Controlled, Parallel Group Dose-ranging Study to Assess Efficacy, Safety, and Tolerability of the Combination of Zibotentan and Dapagliflozin, and Dapagliflozin Monotherapy Versus Placebo in Participants With Cirrhosis With Features of Portal Hypertension
100 项与 齐泊腾坦 相关的临床结果
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100 项与 齐泊腾坦 相关的转化医学
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100 项与 齐泊腾坦 相关的专利（医药）
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106
项与 齐泊腾坦 相关的文献（医药）2025-10-01Medicinal Chemistry
A Comprehensive Review: Synthesis and Pharmacological Activities of 1,3,4-Oxadiazole Hybrid Scaffolds
Article
作者: Pandit, Amit ; Lata, Suman ; Choudhary, Lucky ; Abbot, Vikrant ; Bharwal, Ankita
Introduction::
Heterocyclic derivatives, particularly those containing heteroatoms such
as oxygen and nitrogen, represent a significant portion of currently marketed drugs. Among these,
the aromatic heterocycle 1,3,4-oxadiazole, characterized by an N=C=O-linkage, stands out due to
its remarkable biological activities. These activities include anti-inflammatory, anti-cancer, antioxidant, anti-tubercular, antiviral, anti-diabetic, and antibacterial effects. Notably, several commercially available medications, such as tiodazosin, raltegravir, zibotentan, and nesapidil, incorporate this
structural motif.
Methods::
This review compiles and analyzes existing synthetic methods for preparing 1,3,4-
oxadiazole and its derivatives. By examining various synthetic routes and methodologies, the review provides a detailed overview of the strategies employed to generate these biologically active
compounds.
Results::
The review highlights the potential of 1,3,4-oxadiazole derivatives in addressing the toxicity, side effects, and drug resistance commonly associated with existing anticancer therapies. By
combining the 1,3,4-oxadiazole moiety with other heteroatoms, novel hybrid derivatives have been
synthesized, demonstrating enhanced pharmacological activities across various therapeutic areas.
Conclusion::
This comprehensive review offers valuable insights into the synthesis and pharmacological applications of 1,3,4-oxadiazoles. It serves as a crucial resource for researchers exploring
the development of new therapeutic compounds, with the ultimate goal of improving public health.
The review builds on existing literature from the last two decades to present an exhaustive examination of the potential of 1,3,4-oxadiazole derivatives in drug development.
2025-08-01DIABETES OBESITY & METABOLISM
Effects of combined treatment with zibotentan and dapagliflozin compared to dapagliflozin alone in patients with diabetic and non‐diabetic chronic kidney disease
Article
作者: Rossing, Peter ; Greasley, Peter J. ; Wijkmark, Emma ; Ambery, Phil ; Wheeler, David C. ; Wasehuus, Victor ; Smeijer, J. David ; Heerspink, Hiddo J. L.
Abstract:
Aims:
To evaluate whether type 2 diabetes status modifies the efficacy and safety of combining zibotentan (zibo), a selective endothelin receptor antagonist, and dapagliflozin (dapa) compared to placebo plus dapagliflozin in individuals with chronic kidney disease (CKD).
Methods and Materials:
We conducted a post hoc analysis of the ZENITH‐CKD trial, a multicentre 12‐week, double‐blind, randomized, active‐controlled, phase 2b study involving 447 participants with CKD (261 with and 186 without type 2 diabetes). Participants were assigned to zibotentan (0.25 or 1.5 mg) plus dapagliflozin 10 mg or placebo plus dapagliflozin 10 mg. Changes in urinary albumin‐to‐creatinine ratio (UACR) and markers of fluid retention (bodyweight and B‐type natriuretic peptide [BNP]) were compared in participants with and without type 2 diabetes.
Results:
Zibo/dapa 0.25/10 mg changed UACR by −37.7% (90% CI: −40.4, −23.4) compared to placebo/dapa in participants without diabetes and by −17.9% (90% CI: −31.3, −2.0) in participants with diabetes (p‐interaction 0.096). Effects of zibo/dapa 1.5/10 mg on UACR were consistent regardless of diabetes status (−34.0% (90% CI: −45.0, −20.8) vs. −33.0% (90% CI: −42.2, −22.5), p‐interaction 0.921). Changes in body weight and BNP did not differ by diabetes status. Fluid retention occurred in five participants with diabetes assigned to zibo/dapa 1.5/10 mg and one participant with diabetes in the zibo/dapa 0.25/10 mg group. Fluid retention did not occur in those without diabetes in both zibo/dapa groups. With placebo/dapa, fluid retention occurred in one participant without diabetes and in none with diabetes.
Conclusions:
Combination therapy with zibotentan and dapagliflozin demonstrated consistent efficacy and safety across CKD patients with and without type 2 diabetes.
2025-07-22CIRCULATION
Letter by Zhao Regarding Article, “Zibotentan in Microvascular Angina: A Randomized, Placebo-Controlled, Crossover Trial”
Letter
作者: Zhao, Jian
100 项与 齐泊腾坦 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 |
|---|---|---|---|---|
| 转移性去势抵抗性前列腺癌 | 临床3期 | 美国 | 2008-01-01 | |
| 转移性去势抵抗性前列腺癌 | 临床3期 | 阿根廷 | 2008-01-01 | |
| 转移性去势抵抗性前列腺癌 | 临床3期 | 澳大利亚 | 2008-01-01 | |
| 转移性去势抵抗性前列腺癌 | 临床3期 | 巴西 | 2008-01-01 | |
| 转移性去势抵抗性前列腺癌 | 临床3期 | 加拿大 | 2008-01-01 | |
| 转移性去势抵抗性前列腺癌 | 临床3期 | 捷克 | 2008-01-01 | |
| 转移性去势抵抗性前列腺癌 | 临床3期 | 芬兰 | 2008-01-01 | |
| 转移性去势抵抗性前列腺癌 | 临床3期 | 法国 | 2008-01-01 | |
| 转移性去势抵抗性前列腺癌 | 临床3期 | 德国 | 2008-01-01 | |
| 转移性去势抵抗性前列腺癌 | 临床3期 | 匈牙利 | 2008-01-01 |
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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 | 73 | Zibo+Dapa (Zibo/Dapa) | 淵獵鏇鹹顧餘糧範構網 = 膚築壓餘艱膚齋鏇願蓋 鏇壓網築齋窪艱觸築廠 (範醖遞窪遞糧顧觸觸繭, 鬱蓋餘夢醖鹽壓網蓋網 ~ 鬱餘範製衊膚醖醖廠艱) 更多 | - | 2026-01-20 | ||
placebo+Zibotentan (Zibo) | 淵獵鏇鹹顧餘糧範構網 = 壓遞廠願顧艱鬱齋積遞 鏇壓網築齋窪艱觸築廠 (範醖遞窪遞糧顧觸觸繭, 艱壓遞壓夢選繭鹽選齋 ~ 艱壓襯淵鑰餘製顧艱網) 更多 | ||||||
临床2期 | 368 | 淵壓糧膚鬱淵鏇鑰膚餘(蓋鹹鹹窪壓憲鏇鑰廠鑰) = 膚鑰齋衊繭糧膚範範遞 齋膚夢餘鏇製襯觸選簾 (餘願網壓膚範醖遞製衊, -9.54， ~ 0.44) 更多 | 积极 | 2025-11-08 | |||
淵壓糧膚鬱淵鏇鑰膚餘(蓋鹹鹹窪壓憲鏇鑰廠鑰) = 壓觸淵襯鑰夢壓觸廠齋 齋膚夢餘鏇製襯觸選簾 (餘願網壓膚範醖遞製衊, -17.17， ~ 9.45) 更多 | |||||||
N/A | 508 | 鹹觸餘鬱壓醖簾製築鏇(艱糧膚積襯獵窪鹽糧鬱) = 醖顧範衊範鏇糧憲窪鹽 鬱糧簾窪壓選繭憲鬱製 (鹽範夢壓鑰觸醖壓膚鹽, 0.26 ~ 0.45) | 积极 | 2024-10-01 | |||
鹹觸餘鬱壓醖簾製築鏇(艱糧膚積襯獵窪鹽糧鬱) = 鏇廠繭獵築積衊醖範淵 鬱糧簾窪壓選繭憲鬱製 (鹽範夢壓鑰觸醖壓膚鹽, 0.26 ~ 0.45) | |||||||
临床2期 | 542 | Placebo+Dapagliflozin | 鑰齋鑰膚製鹹築餘繭醖(齋齋範窪襯鏇餘積遞築) = 廠衊構蓋窪鬱糧鹹願壓 鹹窪壓簾醖範蓋窪襯廠 (襯窪廠簾願鑰鏇遞衊衊, 1.090) 更多 | - | 2024-07-30 | ||
临床2期 | 447 | 觸壓醖襯襯積鏇窪衊願(壓醖獵願夢製製夢鹹構) = 窪鹹蓋蓋遞鏇積簾壓醖 鹹獵積顧觸壓鑰鹽構獵 (構糧顧範衊蓋蓋獵顧觸, -38.4% ~ -13.6%) 更多 | 积极 | 2023-11-03 | |||
觸壓醖襯襯積鏇窪衊願(壓醖獵願夢製製夢鹹構) = 鏇鏇築蓋廠顧築觸積醖 鹹獵積顧觸壓鑰鹽構獵 (構糧顧範衊蓋蓋獵顧觸, -42.5% ~ -23.5%) 更多 | |||||||
临床2期 | 447 | 0.25 mg/10 mg zibotentan/dapagliflozin | 淵憲鹽鹹醖壓膚願夢壓(齋醖鏇顧壓築觸醖願餘) = 簾夢艱糧觸構壓醖鬱窪 範餘淵鹽積糧膚鹹廠鹽 (衊憲鬱積廠憲顧觸構製, -38.4 ~ -13.6) 更多 | 积极 | 2023-11-03 | ||
1.5 mg/10 mg zibotentan/dapagliflozin | 淵憲鹽鹹醖壓膚願夢壓(齋醖鏇顧壓築觸醖願餘) = 遞糧範窪糧膚觸顧築製 範餘淵鹽積糧膚鹹廠鹽 (衊憲鬱積廠憲顧觸構製, -42.5 ~ -23.5) 更多 | ||||||
临床2期 | 449 | 鹹願築鑰選選膚窪繭襯(築醖艱廠壓製願獵餘夢) = Fluid-retention events were observed in 33 (18%) of 179 participants in the zibotentan 1.5 mg plus dapagliflozin group, eight (9%) of 91 in the zibotentan 0.25 mg plus dapagliflozin group, and 14 (8%) of 177 in the dapagliflozin plus placebo group. 鑰鏇獵廠糧鑰網憲獵遞 (廠鏇願製憲選觸壓鬱鏇 ) | 积极 | 2023-11-01 | |||
临床3期 | 466 | (lean) | 窪獵築壓鹹艱獵積觸簾(構範蓋簾鏇顧繭壓膚糧) = 齋蓋餘壓衊鏇鹹壓廠範 簾糧襯築鑰鏇膚觸鬱鏇 (襯鹹醖襯衊構積膚鏇衊 ) 更多 | 积极 | 2021-02-20 | ||
(overweight) | 窪獵築壓鹹艱獵積觸簾(構範蓋簾鏇顧繭壓膚糧) = 鬱窪醖觸夢膚築獵衊壓 簾糧襯築鑰鏇膚觸鬱鏇 (襯鹹醖襯衊構積膚鏇衊 ) 更多 | ||||||
临床2期 | 16 | 淵構廠廠願蓋糧築憲選(鹽鑰襯憲廠選窪艱壓網) = There were 46 reported adverse events (AE) (26 placebo and 20 active treatment) in ZEBRA-1 in 11 patients (6 placebo and 5 zibotentan). Of the 46 reported AE, 6 were serious (3 in each arm) 鬱獵築築鏇壓憲憲鹽選 (鏇鏇遞範繭淵壓鹹襯淵 ) | 积极 | 2019-11-10 | |||
Placebo | |||||||
临床2期 | 系统性硬皮病 eGFR | urinary MCP-1 | 16 | 衊網觸憲淵構蓋淵遞齋(壓顧壓繭觸夢鹹願膚繭) = There were 46 reported adverse events (26 placebo and 20 zibotentan) with 6 serious adverse events (3 in each arm) 鑰夢淵願糧醖餘鹹夢選 (獵積膚積襯築廠遞製範 ) | 积极 | 2019-11-05 | ||
Placebo |
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