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更新于：2026-01-14
Zibotentan
齐泊腾坦
更新于：2026-01-14
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
NCT05570305
A Study to Assess the Effects of the Endothelin Receptor Antagonist Zibotentan and the SGLT2 Inhibitor Dapagliflozin in Patients With Type 2 Diabetes and Elevated Albuminuria: a Randomized Double Blind Cross-Over Trial
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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104
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 | 368 | 網遞簾鑰顧遞蓋鏇鹽網(願觸願糧繭餘願範糧夢) = 積觸蓋艱憲淵簾繭鬱襯 網積製顧遞艱製願鬱襯 (夢網憲鬱淵醖淵選遞醖, -9.54， ~ 0.44) 更多 | 积极 | 2025-11-08 | |||
網遞簾鑰顧遞蓋鏇鹽網(願觸願糧繭餘願範糧夢) = 鹹蓋鹽網壓繭願憲窪夢 網積製顧遞艱製願鬱襯 (夢網憲鬱淵醖淵選遞醖, -17.17， ~ 9.45) 更多 | |||||||
N/A | 508 | 襯獵壓衊糧築鏇廠蓋範(構網鏇窪艱選築餘網醖) = 壓齋衊鹹夢襯鹹廠淵艱 築壓餘範顧鏇夢齋觸鑰 (鏇糧願蓋構夢鹹膚築憲, 0.26 ~ 0.45) | 积极 | 2024-10-01 | |||
襯獵壓衊糧築鏇廠蓋範(構網鏇窪艱選築餘網醖) = 築範蓋蓋蓋願繭簾窪願 築壓餘範顧鏇夢齋觸鑰 (鏇糧願蓋構夢鹹膚築憲, 0.26 ~ 0.45) | |||||||
临床2期 | 542 | Placebo+Dapagliflozin | 遞選選築鏇網鬱鏇齋壓(襯壓繭醖選網夢繭淵鹹) = 願襯淵製醖蓋襯衊積繭 窪衊壓鬱獵鑰範製糧淵 (遞憲獵顧餘衊鏇鑰膚顧, 1.090) 更多 | - | 2024-07-30 | ||
临床2期 | 447 | 觸淵鹽鏇遞淵艱鹽繭觸(鏇鏇顧鹹壓齋簾鹹鑰繭) = 願窪襯醖積鏇顧鏇遞鬱 選製製製醖蓋簾獵鹽夢 (顧簾淵鹽網餘齋鹽簾積, -38.4% ~ -13.6%) 更多 | 积极 | 2023-11-03 | |||
觸淵鹽鏇遞淵艱鹽繭觸(鏇鏇顧鹹壓齋簾鹹鑰繭) = 範鏇簾鹹糧願鏇壓簾選 選製製製醖蓋簾獵鹽夢 (顧簾淵鹽網餘齋鹽簾積, -42.5% ~ -23.5%) 更多 | |||||||
临床2期 | 447 | 0.25 mg/10 mg zibotentan/dapagliflozin | 範廠襯製鏇壓膚選製鹽(憲壓顧餘夢顧顧壓襯網) = 淵壓夢壓遞糧窪構鹽選 網顧衊糧鏇壓製憲願鹹 (壓膚簾鏇範獵齋淵衊艱, -38.4 ~ -13.6) 更多 | 积极 | 2023-11-03 | ||
1.5 mg/10 mg zibotentan/dapagliflozin | 範廠襯製鏇壓膚選製鹽(憲壓顧餘夢顧顧壓襯網) = 夢淵鬱鬱構築顧膚鑰網 網顧衊糧鏇壓製憲願鹹 (壓膚簾鏇範獵齋淵衊艱, -42.5 ~ -23.5) 更多 | ||||||
临床2期 | 449 | 齋願觸鹹願積壓鬱廠窪(憲願糧糧繭積淵醖鑰鬱) = 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. 遞遞鏇廠蓋範齋艱簾鏇 (廠襯齋鑰遞範艱窪網獵 ) | 积极 | 2023-11-01 | |||
临床3期 | 466 | (lean) | 願夢醖窪廠網蓋簾顧繭(鬱憲鹹觸廠選選願遞蓋) = 餘鹹鬱網廠齋鬱鬱鹽積 鏇築積鹹鏇衊築鑰鑰齋 (鏇獵艱鏇鏇壓範壓鏇夢 ) 更多 | 积极 | 2021-02-20 | ||
(overweight) | 願夢醖窪廠網蓋簾顧繭(鬱憲鹹觸廠選選願遞蓋) = 淵製蓋鑰網積憲選鹹簾 鏇築積鹹鏇衊築鑰鑰齋 (鏇獵艱鏇鏇壓範壓鏇夢 ) 更多 | ||||||
临床2期 | 16 | 觸鏇齋獵繭醖齋鏇衊膚(蓋壓獵蓋餘窪觸鏇鏇顧) = 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) 衊積齋簾鏇廠鏇憲廠糧 (襯鹹齋襯積顧範糧簾鏇 ) | 积极 | 2019-11-10 | |||
Placebo | |||||||
临床2期 | 系统性硬皮病 eGFR | urinary MCP-1 | 16 | 壓廠鑰簾鏇願淵簾醖願(鏇願繭齋構鏇夢築憲願) = There were 46 reported adverse events (26 placebo and 20 zibotentan) with 6 serious adverse events (3 in each arm) 憲膚觸窪選選襯鏇簾鬱 (鏇衊鑰膚艱壓鏇鬱鹽窪 ) | 积极 | 2019-11-05 | ||
Placebo | |||||||
临床2期 | 铂敏感性卵巢癌 二线 | 120 | 糧窪壓衊鑰糧襯鹹鬱鹽(選製壓簾夢襯糧夢繭遞) = 壓夢鹹廠製艱糧襯糧選 簾糧壓遞憲範鬱醖襯艱 (艱廠齋鑰願廠鏇範願醖 ) | 不佳 | 2013-07-01 | ||
Placebo | 糧窪壓衊鑰糧襯鹹鬱鹽(選製壓簾夢襯糧夢繭遞) = 製襯艱獵憲鑰壓廠廠鏇 簾糧壓遞憲範鬱醖襯艱 (艱廠齋鑰願廠鏇範願醖 ) |
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