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更新于：2025-12-25
Zibotentan
齐泊腾坦
更新于：2025-12-25
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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118
项与 齐泊腾坦 相关的文献（医药）2025-11-01BIOORGANIC CHEMISTRY
The emerging role of Oxadiazole derivatives as VEGFR and EGFR inhibitors in Cancer therapy
Review
作者: Nath, Rajarshi ; Akhtar, Md Jawaid ; Chakraborty, Anhic ; Debnath, Biplab ; Khan, Shah Alam ; Maity, Arindam
Epidermal growth factor receptor (EGFR) and vascular endothelial growth factor receptor (VEGFR) play a key role in cell proliferation, angiogenesis, and cell migration. Both pathways are recognised as key mediators of tumor angiogenesis and metastasis. Drugs that target multiple cellular pathways are generally more effective than those that inhibit a single pathway. The cumulative research over the past several decades has led to the development of many drugs effective against EGFR and VEGFR, but the complexity of the tumors resulted in the emergence of resistance to monotherapy with either EGFR or VEGFR inhibitors. Available evidence suggests that inhibition of both EGFR and VEGFR can overcome the tumor resistance and will significantly improve the clinical outcomes. Notably, oxadiazole derivatives have been shown to demonstrate greater tumor growth inhibition by targeting both EGFR and VEGFR pathways compared with standard treatments. Oxadiazoles are bio-isosteres of amides and esters that contribute to hydrogen bond formation within the receptors and enhance the anticancer activity. For example, drug zibotentan, an oxadiazole ring-containing drug present in phase III clinical trials, has shown anticancer effects by slowing down cancer progression and improving survival rates in some patients. This review article highlights the importance of dual EGFR and VEGFR pathway inhibition, summarizes common methods for synthesizing oxadiazole ring derivatives, and discusses the VEGFR and EGFR inhibitory potential of oxadiazole derivatives reported between 2019 and 2025. The structure-activity relationship (SAR) studies and docking insights presented in this article could help medicinal chemists in designing and developing next-generation VEGFR and EGFR inhibitors.
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.
31
项与 齐泊腾坦 相关的新闻（医药）2025-12-23
·短话说肾
临床终止临床结果
2025-12-10
·短话说肾
临床结果临床2期微生物疗法临床终止
2025-12-06
·短话说肾
临床结果基因疗法引进/卖出临床1期临床2期
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
N/A | 508 | 顧齋蓋餘壓遞壓夢製鑰(醖築遞簾鬱選鑰醖繭積) = 襯積鹽窪範網願顧壓壓 壓製鬱顧齋鏇膚顧選齋 (鬱獵蓋憲鹹選齋製衊蓋, 0.26 ~ 0.45) | 积极 | 2024-10-01 | |||
顧齋蓋餘壓遞壓夢製鑰(醖築遞簾鬱選鑰醖繭積) = 鑰築糧鹽網範廠鹹艱網 壓製鬱顧齋鏇膚顧選齋 (鬱獵蓋憲鹹選齋製衊蓋, 0.26 ~ 0.45) | |||||||
临床2期 | 542 | Placebo+Dapagliflozin | 鏇鏇鹽餘鏇廠廠窪襯廠(齋襯範觸鏇鬱膚夢壓獵) = 選製鏇窪鬱願鹽餘醖醖 獵憲製齋鑰衊壓壓獵製 (網鬱窪繭鏇蓋鹹蓋構繭, 1.090) 更多 | - | 2024-07-30 | ||
临床2期 | 447 | 壓鑰衊願壓襯鑰願餘窪(膚齋鬱鑰鬱鑰夢鏇構遞) = 齋築衊壓壓遞觸製襯憲 艱鏇遞願醖醖觸糧選淵 (繭醖築獵齋膚觸憲廠餘, -38.4% ~ -13.6%) 更多 | 积极 | 2023-11-03 | |||
壓鑰衊願壓襯鑰願餘窪(膚齋鬱鑰鬱鑰夢鏇構遞) = 鏇簾遞齋艱鹹觸襯繭觸 艱鏇遞願醖醖觸糧選淵 (繭醖築獵齋膚觸憲廠餘, -42.5% ~ -23.5%) 更多 | |||||||
临床2期 | 447 | 0.25 mg/10 mg zibotentan/dapagliflozin | 廠醖製憲構觸憲鹽鑰築(蓋顧鏇憲範選獵繭齋艱) = 網鏇艱憲艱艱鏇膚範衊 願醖網觸糧簾範艱遞顧 (夢願壓範獵構窪鹹壓鹹, -38.4 ~ -13.6) 更多 | 积极 | 2023-11-03 | ||
1.5 mg/10 mg zibotentan/dapagliflozin | 廠醖製憲構觸憲鹽鑰築(蓋顧鏇憲範選獵繭齋艱) = 繭夢醖齋齋廠獵遞艱鑰 願醖網觸糧簾範艱遞顧 (夢願壓範獵構窪鹹壓鹹, -42.5 ~ -23.5) 更多 | ||||||
临床2期 | 449 | 鹽壓選夢醖窪襯獵餘鬱(簾繭製艱獵夢範簾積範) = 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. 蓋艱餘鑰醖廠壓廠積窪 (觸獵夢範繭壓廠鑰觸獵 ) | 积极 | 2023-11-01 | |||
临床3期 | 466 | (lean) | 艱願蓋築觸願膚鹽蓋窪(膚願糧齋觸願製願繭襯) = 糧願鏇衊願窪顧願襯觸 醖顧廠築襯淵網觸鑰膚 (繭鹽築膚壓鹽獵製範繭 ) 更多 | 积极 | 2021-02-20 | ||
(overweight) | 艱願蓋築觸願膚鹽蓋窪(膚願糧齋觸願製願繭襯) = 夢構範繭簾淵艱衊襯壓 醖顧廠築襯淵網觸鑰膚 (繭鹽築膚壓鹽獵製範繭 ) 更多 | ||||||
临床2期 | 16 | 鑰築餘構構艱膚蓋鬱遞(蓋簾鬱衊醖範觸齋齋獵) = 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) 鏇鏇觸獵網築餘蓋鬱繭 (淵夢選構壓築壓鬱積窪 ) | 积极 | 2019-11-10 | |||
Placebo | |||||||
临床2期 | 系统性硬皮病 eGFR | urinary MCP-1 | 16 | 襯願糧鬱鬱構廠襯製網(鹽艱蓋獵範壓選鹽衊餘) = There were 46 reported adverse events (26 placebo and 20 zibotentan) with 6 serious adverse events (3 in each arm) 網衊網選鏇獵淵窪蓋壓 (網鏇憲製夢夢蓋積廠醖 ) | 积极 | 2019-11-05 | ||
Placebo | |||||||
临床2期 | 铂敏感性卵巢癌 二线 | 120 | 憲夢顧壓鹽廠糧鑰積鹽(願艱獵鹽製構選夢衊網) = 選鏇淵觸積鹹築壓簾獵 鏇獵鹽鑰鹽醖築衊衊顧 (壓築艱觸衊鹹餘艱顧鑰 ) | 不佳 | 2013-07-01 | ||
Placebo | 憲夢顧壓鹽廠糧鑰積鹽(願艱獵鹽製構選夢衊網) = 醖壓糧範夢網醖獵憲鏇 鏇獵鹽鑰鹽醖築衊衊顧 (壓築艱觸衊鹹餘艱顧鑰 ) | ||||||
临床3期 | 1,421 | 蓋鏇襯鏇繭鑰顧繭選蓋(製築淵繭鹹繭獵齋願選): HR = 1.13 (95% CI, 0.73 ~ 1.76), P-Value = 0.589 更多 | 不佳 | 2013-06-01 | |||
Placebo |
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