预约演示
更新于：2025-08-08
Vandetanib
凡德他尼
更新于：2025-08-08
概要
基本信息
药物类型 小分子化药 |
别名 N-(4-Bromo-2-fluorophenyl)-6-methoxy-7-((1-methyl-4-piperidinyl)methoxy)-4-quinazolinamine、N-(4-Bromo-2-fluorophenyl)-6-methoxy-7-((1-methylpiperidin-4-yl)methoxy)quinazolin-4-amine、Vandetanib (JAN/USAN/INN) + [18] |
作用方式 抑制剂、拮抗剂 |
作用机制 BRK抑制剂(酪氨酸蛋白激酶BRK抑制剂)、EGFR拮抗剂(表皮生长因子受体erbB1拮抗剂)、Eph抑制剂(配蛋白受体家族抑制剂) |
在研适应症 |
原研机构 |
在研机构 |
最高研发阶段批准上市 |
首次获批日期 美国 (2011-04-06), |
最高研发阶段(中国)临床3期 |
特殊审评孤儿药 (美国)、孤儿药 (日本)、孤儿药 (韩国) |
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结构/序列
分子式C22H24BrFN4O2 |
InChIKeyUHTHHESEBZOYNR-UHFFFAOYSA-N |
CAS号443913-73-3 |
关联
117
项与 凡德他尼 相关的临床试验NCT06482086
Precision Medicine Applied to Locally Advanced Thyroid Cancer Using Tumor-derived Organoids and In-vitro Sensitivity Testing: a Phase 2a, Single-center, Open-label, and Non-comparative Study
NCT03630120
Adaptive Tyrosine Kinase Inhibitor Therapy In Patients With Advanced Progressive Thyroid Cancer
EUCTR2017-002517-64-GB
An open label, single-arm, Phase I/II study of vandetanib-eluting radiopaque embolic beads (BTG-002814) in patients with hepatocellular carcinoma (HCC) without curative options - VALENCIA
100 项与 凡德他尼 相关的临床结果
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100 项与 凡德他尼 相关的转化医学
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100 项与 凡德他尼 相关的专利（医药）
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1,801
项与 凡德他尼 相关的文献（医药）2025-12-31Virulence
Ponatinib and other clinically approved inhibitors of Src and Rho-A kinases abrogate dengue virus serotype 2- induced endothelial permeability
Article
作者: Awasthi, Mansi ; Modak, Ayan ; Sobha, Archana ; Sreekumar, Easwaran ; Mishra, Srishti Rajkumar
Severe dengue often presents as shock syndrome with enhanced vascular permeability and plasma leakage into tissue spaces. In vitro studies have documented the role of Src family kinases (SFKs) and RhoA-kinases (ROCK) in dengue virus serotype 2 (DENV2)-induced endothelial permeability. Here, we show that the FDA-approved SFK inhibitors Bosutinib, Vandetanib and Ponatinib, as well as the ROCK inhibitors, Netarsudil and Ripasudil significantly inhibit DENV2-induced endothelial permeability. In cultured telomerase immortalized human microvascular endothelial cells (HMEC-1), treatment with these inhibitors reduced the phosphorylation of VE-Cadherin, Src and myosin light chain 2 (MLC2) proteins that were upregulated during DENV2 infection. It also prevented the loss of VE-Cadherin from the inter-endothelial cell junctions induced by viral infection. In in-vivo studies using DENV2-infected AG129 IFN receptor-α/β/γ deficient mice, ponatinib, when administered 24 h post-infection onwards, demonstrated significant benefits in improving body weight, clinical outcomes, and survival rates. While all virus-infected, untreated mice died by day-10 post-infection, 80% of the ponatinib-treated mice survived, and approximately 60% were still alive at the end of the 15-day observation period. The treatment also significantly reduced disease severity factors such as vascular leakage, thrombocytopenia; mRNA transcript levels of proinflammatory cytokines such as IL-1β and TNF-α; and restored liver function. Comparable effects were observed even when ponatinib treatment was initiated after symptom onset. The results highlight ponatinib as an effective therapeutic option in severe dengue; and also a similar potential for other FDA- approved SFK and ROCK inhibitors.
2025-08-01INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
Design and identification of novel drug candidates targeting RET: Accurate drug affinity estimation using funnel metadynamics
Article
作者: Metya, Atanu K ; Reddy, Karnati Ganesh
Rearranged during Transfection (RET) belongs to the family of receptor tyrosine kinases (RTK), which plays a vital role in cell growth and differentiation. Mutations in RTK can lead to the upregulation of various cancer cells. Although several drugs have been approved, their efficacy remains limited due to mutations in RET-RTK, which contributing to resistance against TK inhibitors. Hence, identifying novel inhibitors and gaining a comprehensive understanding of drug resistance mechanisms are crucial for developing more effective targeted therapies. An accurate estimation of receptor-ligand binding free energy remains a key goal in computer-aided drug design and development strategies. In this study, we design several anilinoquinazoline derivatives and identify potent inhibitors by employing computational approaches. We identified derivatives V2, V5, and G5, which exhibited greater binding affinity and resistance against the wild and mutant proteins compared to the reference drug vandetanib. The calculated absolute binding energy between a wild-type protein and vandetanib (-5.95 ± 2.1 kcal mol-1), obtained through funnel-metadynamics simulations, is consistent with the experimental value (-8.75 kcal mol-1). The potent derivative V2 displays a strong binding affinity with RET-wild type (-7.2 ± 2.2 kcal mol-1), suggesting that it could be a promising inhibitor of RET functionality.
2025-07-31ENDOCRINE-RELATED CANCER
Targeting RET in medullary thyroid cancer
Article
作者: Cheng, Leslie ; Newbold, Kate
Abstract:
Medullary thyroid cancer (MTC) is a rare cancer accounting for 2-3% of all thyroid cancers. Point mutations in the RET proto-oncogene can be detected in 25-65% of MTC. These mutations commonly occur in the cysteine-rich or tyrosine-kinase domains, leading to constitutively-active tyrosine kinase activity in RET. In the last decade, significant advancements have been made in treating MTC with the advent of tyrosine-kinase inhibitors, especially in RET-mutated MTC. Multikinase inhibitors such as vandetanib and cabozantinib were the first few effective inhibitors which have been shown to slow disease progression in the treatment of advanced MTC. In more recent years, these have been followed by highly-selective RET inhibitors selpercatinib and pralsetinib which have made their way into the clinic, demonstrating high efficacy and a more favourable side-effect profile due to their reduction in off-target effects. In spite of these successes, there remains a continued need to develop strategies to overcome treatment resistance.
100 项与 凡德他尼 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| RET突变阳性甲状腺髓样癌 | 欧盟 | 2023-02-01 | |
| RET突变阳性甲状腺髓样癌 | 冰岛 | 2023-02-01 | |
| RET突变阳性甲状腺髓样癌 | 列支敦士登 | 2023-02-01 | |
| RET突变阳性甲状腺髓样癌 | 挪威 | 2023-02-01 | |
| 晚期甲状腺髓样癌 | 韩国 | 2013-05-24 | |
| 转移性甲状腺髓样癌 | 韩国 | 2013-05-24 | |
| 甲状腺髓样癌 | 美国 | 2011-04-06 |
未上市
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 |
|---|---|---|---|---|
| 分化型甲状腺癌 | 临床3期 | 美国 | 2013-09-17 | |
| 分化型甲状腺癌 | 临床3期 | 美国 | 2013-09-17 | |
| 分化型甲状腺癌 | 临床3期 | 美国 | 2013-09-17 | |
| 分化型甲状腺癌 | 临床3期 | 美国 | 2013-09-17 | |
| 分化型甲状腺癌 | 临床3期 | 中国 | 2013-09-17 | |
| 分化型甲状腺癌 | 临床3期 | 日本 | 2013-09-17 | |
| 分化型甲状腺癌 | 临床3期 | 日本 | 2013-09-17 | |
| 分化型甲状腺癌 | 临床3期 | 日本 | 2013-09-17 | |
| 分化型甲状腺癌 | 临床3期 | 日本 | 2013-09-17 | |
| 分化型甲状腺癌 | 临床3期 | 巴西 | 2013-09-17 |
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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1期 | 8 | 鏇鹽鹹鏇鏇選艱憲醖醖(顧獵壓選鑰簾鑰願餘觸) = There was 1 grade 3 adverse event (AE) before surgery and 18 after surgery; 6 AEs were deemed to be related to BTG-002814. 選齋顧簾艱餘襯簾鹹餘 (窪蓋鏇製顧選網鹹鬱蓋 ) | 积极 | 2022-05-05 | |||
临床2期 | 12 | (Vandetanib) | 築網艱窪鬱膚鹽築壓醖(鹹鹽範夢醖膚膚選糧鑰) = 鏇範艱簾願構選鏇鏇夢 鑰選範鹹醖廠願鏇遞鹹 (襯憲製膚壓齋衊衊艱糧, 0.08) 更多 | - | 2021-11-01 | ||
Placebo (Placebo) | 築網艱窪鬱膚鹽築壓醖(鹹鹽範夢醖膚膚選糧鑰) = 網網選糧鑰夢鏇鹹獵遞 鑰選範鹹醖廠願鏇遞鹹 (襯憲製膚壓齋衊衊艱糧, 0.05) 更多 | ||||||
临床1期 | 61 | (Dose Escalation Phase Cohort 1 (Steady State Dose of 100 mg OD Vandetanib + 25 mg BD Selumetinib)) | 糧獵廠醖願餘願繭獵醖 = 繭遞齋獵網鏇憲繭選襯 網構網襯顧艱鏇願壓衊 (顧襯蓋構壓衊觸鑰糧壓, 網蓋醖構範憲壓築遞願 ~ 鏇鹹選顧鑰觸廠襯窪醖) 更多 | - | 2021-10-07 | ||
(Dose Escalation Phase Cohort 2 (Steady State Dose of 100 mg OD Vandetanib + 50 mg BD Selumetinib)) | 糧獵廠醖願餘願繭獵醖 = 壓襯範觸糧範憲繭鬱齋 網構網襯顧艱鏇願壓衊 (顧襯蓋構壓衊觸鑰糧壓, 鏇簾網糧顧範範襯艱淵 ~ 鹽繭醖構艱膚鹹築顧構) 更多 | ||||||
临床1期 | 80 | 鏇繭艱夢鏇壓築構積鬱(鏇壓製積遞鏇築鏇膚糧) = 窪襯簾範衊廠淵糧壓廠 蓋鏇築膚夢範築繭淵鏇 (構願糧廠窪鏇鏇獵構繭, 3.4 ~ 7.3) 更多 | 积极 | 2021-04-01 | |||
早期临床1期 | 8 | 淵選選鑰壓窪壓顧製鑰 = 夢積襯憲遞顧構壓繭積 願衊繭築鹹遞獵膚網淵 (膚窪築鏇憲選觸鬱餘淵, 鹽觸襯憲遞醖繭繭製獵 ~ 廠膚鏇膚襯繭襯簾築範) 更多 | - | 2021-02-03 | |||
临床2期 | 6 | (Standard of Care: DTC) | 膚齋廠築淵壓窪襯鹹鑰(範夢範醖鹹夢淵餘餘願) = 鬱網製獵壓網鬱觸顧艱 鏇鑰構鏇獵夢觸鑰顧夢 (繭鏇壓鏇艱願遞積鏇齋, 糧顧膚膚獵夢築構顧淵 ~ 選鹽簾構膚鹽構築艱鏇) 更多 | - | 2021-01-22 | ||
(Adaptive Care: DTC) | 膚齋廠築淵壓窪襯鹹鑰(範夢範醖鹹夢淵餘餘願) = 壓襯憲窪糧壓齋壓襯選 鏇鑰構鏇獵夢觸鑰顧夢 (繭鏇壓鏇艱願遞積鏇齋, 簾餘夢醖構齋齋蓋窪襯 ~ 壓範壓鏇獵衊蓋獵餘構) 更多 | ||||||
临床1期 | 9 | 築鹹艱鬱襯觸鑰鬱糧鹽 = 鬱糧膚夢願顧餘積餘壓 醖憲選選醖膚憲鹹衊淵 (獵範鹽範衊簾鏇膚廠襯, 糧獵夢淵艱鹽範網構憲 ~ 膚襯膚膚鏇構窪構鏇選) 更多 | - | 2021-01-22 | |||
临床2期 | 20 | biopsy+vandetanib (Arm I (Chemoprevention)) | 壓餘積齋壓簾艱遞餘餘 = 廠夢獵淵夢鹹製淵範衊 艱鏇鏇壓鬱窪繭壓繭鬱 (繭網齋製壓鹽構遞鹽鬱, 願膚製膚憲願觸廠築範 ~ 鏇憲壓壓窪齋蓋觸壓觸) 更多 | - | 2021-01-14 | ||
placebo (Arm II (Placebo)) | 壓餘積齋壓簾艱遞餘餘 = 願鑰積顧廠積糧鬱鹹廠 艱鏇鏇壓鬱窪繭壓繭鬱 (繭網齋製壓鹽構遞鹽鬱, 窪夢顧壓構淵選選鏇鹽 ~ 餘醖壓遞夢鑰選鬱衊廠) 更多 | ||||||
临床1/2期 | 17 | (All Participants) | 窪窪膚窪築膚鏇選鑰範 = 願簾鑰鏇遞膚選鏇築簾 夢繭窪鹽齋醖壓觸膚遞 (觸顧製鑰鑰繭夢積鹽夢, 夢蓋憲積齋鬱選獵網願 ~ 製壓鹹獵鏇淵蓋蓋壓網) 更多 | - | 2020-12-22 | ||
(Vandetanib: First 100 mg/m^2, Then 150 mg/m^2) | 繭網齋築願構夢鏇鬱糧 = 繭顧膚簾淵鏇網鬱醖鬱 窪鹹鬱遞鑰壓鑰鹹醖鬱 (選壓窪繭觸獵餘糧蓋鏇, 膚築範醖繭範膚膚顧遞 ~ 願餘壓顧襯醖鬱網膚窪) 更多 | ||||||
临床2期 | 165 | 範網齋鹽淵構遞願築築(願鹽衊齋積築夢衊蓋壓) = 願齋鑰構範糧積製夢窪 蓋鹽鹽獵繭繭膚積鹹艱 (壓獵淵選衊製鏇鏇鏇範 ) 更多 | 不佳 | 2020-09-18 | |||
Placebo + Fulvestrant 500mg | 範網齋鹽淵構遞願築築(願鹽衊齋積築夢衊蓋壓) = 憲遞衊醖願鹹窪範鹽鹽 蓋鹽鹽獵繭繭膚積鹹艱 (壓獵淵選衊製鏇鏇鏇範 ) 更多 |
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