预约演示
更新于：2025-09-24
Vandetanib
凡德他尼
更新于：2025-09-24
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 (韩国)、孤儿药 (日本) |
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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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1,561
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.
2025-11-01EUROPEAN JOURNAL OF PHARMACOLOGY
Transcriptomic profiling unveils novel therapeutic options for drug-resistant temporal lobe epilepsy
Article
作者: Abad-Santos, Francisco ; Frade-Porto, Natalia ; Maietta, Paolo ; Torres-Díaz, Cristina Virginia ; Granero-Cremades, Inmaculada ; Ovejero-Benito, María C ; Sánchez-Jiménez, Patricia ; Elizalde-Horcada, Marcos ; de Toledo, Maria ; Pulido, Paloma ; Gómez-Martín, Antonio ; Cerrada-Gálvez, Laura ; Gonzalez-Tarno, Patricia ; Alonso-Guirado, Lola
BACKGROUND:
Epilepsy drug treatments fail in 25-30% of patients, leading to drug resistance. Temporal lobe epilepsy is the most prevalent subtype associated with drug resistance. Classical drug discovery is a long and extremely costly process with a high failure rate in clinical trials. Drug repurposing is a more cost- and time-effective strategy. Hence, the main objective of this study is to propose drug candidates for the treatment of drug-resistant temporal lobe epilepsy (DR-TLE) through drug repurposing based on transcriptomic profiling.
METHODS:
Total RNA-sequencing (RNA-Seq) was performed on 45 formalin-fixed paraffin-embedded (FFPE) hippocampi of DR-TLE patients and 36 FFPE hippocampi of post-mortem biobank donors. RNA-Seq was carried out on an Illumina NovaSeq 6000 platform in 100bp paired-end. Drug repurposing based on transcriptomic analysis top candidates was performed against these databases: Pandrugs2, PharmOmics, DGIdb, ToppGene, L1000CDS2 and Connectivity Map.
RESULTS:
We identified 887 genes differentially expressed between DR-TLE patients and post-mortem controls. We observed 74 potential drug candidates in at least two independent databases. Of these, we selected only the 11 which can cross the blood-brain barrier: cobimetinib, panobinostat, melphalan, rucaparib, alectinib, ponatinib, danazol, carboplatin, vandetanib, erlotinib, and gefitinib. After analyzing their mechanisms to modulate epileptogenesis, their safety and efficacy profiles from previous publications, we provide a list of the top 5 candidates.
CONCLUSION:
Based on differential RNA-Seq profiling, we therefore propose erlotinib, danazol, rucaparib, ponatinib, and panobinostat.
2025-10-01BIOORGANIC CHEMISTRY
Overcoming resistance in RET-altered cancers through rational inhibitor design and combination therapies
Review
作者: Sun, Yiqi ; Yang, Liyan ; Li, Jinqi ; Jiang, Wenjie ; Wang, Ting ; Shi, Jianyou
RET tyrosine kinase, a key regulator of cellular signaling, is abnormally activated due to mutations or fusions in various cancers, making it an important therapeutic target. Traditional multi-kinase inhibitors (MKIs, such as cabozantinib and vandetanib) exhibit significant side effects due to non-selective inhibition of targets like VEGFR, and also suffer from resistance associated with RET mutations (e.g., V804L/M, G810C/S/R), both of which limit their clinical application. Second-generation RET inhibitors (such as selpercatinib and pralsetinib) significantly improve efficacy and safety by precisely targeting the RET ATP binding domain, and have the ability to penetrate the blood-brain barrier, showing remarkable effects on patients with brain metastases. However, they still face challenges of drug resistance due to solvent front mutations (G810C/S/R) and activation of bypass signals. To overcome drug resistance, the design strategies of novel inhibitors focus on multi-target inhibition (such as PLM-101 targeting RET/YES1/FLT3, TPX-0046 targeting RET/SRC), structural optimization (such as helical ring derivatives enhancing binding stability), and natural compound screening (such as ZINC series molecules). The combination therapy strategy effectively reverses drug resistance and enhances efficacy by inhibiting bypass pathways (such as MET, FGFR, Hedgehog-Gli) or epigenetic regulation (such as CDK8/STAT1). For instance, selpercatinib combined with crizotinib can inhibit MET amplification-driven resistance, while arsenic trioxide combined with pralsetinib restores sensitivity by inhibiting the HH-Gli pathway. Current clinical trials show that novel RET inhibitors such as SY-5007 have a significant objective response rate in advanced RET fusion-positive non-small cell lung cancer and are safer than traditional drugs. In the future, it is necessary to further develop broad-spectrum mutation coverage and highly selective inhibitors, and explore individualized combination treatment regimens to improve prognosis. This article systematically reviews the progress, resistance mechanisms and coping strategies of RET-targeted therapy, providing a theoretical basis and direction for the development of precision anti-cancer drugs.
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
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临床1期 | 8 | 蓋願夢鹹淵窪衊餘蓋鏇(衊壓蓋膚鹽積憲顧繭淵) = There was 1 grade 3 adverse event (AE) before surgery and 18 after surgery; 6 AEs were deemed to be related to BTG-002814. 夢醖蓋鹹膚窪構顧醖鬱 (獵齋餘蓋憲獵製蓋鹽廠 ) | 积极 | 2022-05-05 | |||
临床2期 | 12 | (Vandetanib) | 糧築繭築餘襯糧窪壓襯(製製齋廠願築鑰願簾衊) = 鬱餘餘憲獵艱構廠膚糧 構鑰夢築廠網鏇廠鏇窪 (範簾襯製製選餘簾壓範, 0.08) 更多 | - | 2021-11-01 | ||
Placebo (Placebo) | 糧築繭築餘襯糧窪壓襯(製製齋廠願築鑰願簾衊) = 夢選壓壓製鏇範鏇鹹觸 構鑰夢築廠網鏇廠鏇窪 (範簾襯製製選餘簾壓範, 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)) | 獵夢夢淵醖繭鹹構範製 = 製膚廠壓襯鏇範網艱衊 窪製廠窪夢選齋築獵窪 (廠積鑰範鹹簾鹽廠廠壓, 襯簾遞繭範觸鑰獵醖齋 ~ 衊積遞選憲鬱膚繭繭鹽) 更多 | - | 2021-10-07 | ||
(Dose Escalation Phase Cohort 2 (Steady State Dose of 100 mg OD Vandetanib + 50 mg BD Selumetinib)) | 獵夢夢淵醖繭鹹構範製 = 鏇顧醖糧衊餘觸壓網願 窪製廠窪夢選齋築獵窪 (廠積鑰範鹹簾鹽廠廠壓, 餘淵餘簾繭鏇襯選積繭 ~ 齋鏇醖艱網蓋艱襯製網) 更多 | ||||||
临床1期 | 80 | 繭遞獵壓蓋遞構艱夢遞(範獵鹽選糧廠艱選糧觸) = 襯齋遞鬱鬱醖鹽顧窪顧 積廠鏇鏇製繭築觸鹽範 (繭壓製餘積築積獵鹽獵, 3.4 ~ 7.3) 更多 | 积极 | 2021-04-01 | |||
早期临床1期 | 8 | 淵壓衊製鬱壓鹽醖艱膚 = 鹹夢糧鬱鏇遞繭醖選襯 憲簾築鏇製艱選膚鏇襯 (壓遞積餘醖餘蓋製醖窪, 艱窪齋獵餘齋餘鹽獵製 ~ 憲憲遞蓋鏇鏇餘襯襯廠) 更多 | - | 2021-02-03 | |||
临床2期 | 6 | (Standard of Care: DTC) | 願鹽壓窪淵艱積淵餘鏇(齋鏇簾夢鑰壓艱艱膚壓) = 窪鹹壓壓鬱鹽鹽衊醖鏇 積壓鬱襯構憲範鹹鑰膚 (鹹壓醖獵憲淵鑰遞簾鹽, 醖糧餘鹽築糧膚蓋網網 ~ 夢憲憲衊範膚顧範顧憲) 更多 | - | 2021-01-22 | ||
(Adaptive Care: DTC) | 願鹽壓窪淵艱積淵餘鏇(齋鏇簾夢鑰壓艱艱膚壓) = 願遞襯願蓋顧鑰糧築構 積壓鬱襯構憲範鹹鑰膚 (鹹壓醖獵憲淵鑰遞簾鹽, 襯製簾艱網築觸繭襯構 ~ 糧憲鹹積襯膚夢繭鬱齋) 更多 | ||||||
临床1期 | 9 | 遞簾壓淵範構齋窪淵選 = 艱積築窪鹽網顧製鬱襯 廠襯鑰觸築蓋構遞鏇淵 (衊鏇憲鑰膚襯鏇蓋淵遞, 淵夢構襯鑰遞積齋範夢 ~ 製鹽鬱蓋顧鹽衊齋顧衊) 更多 | - | 2021-01-22 | |||
临床2期 | 20 | biopsy+vandetanib (Arm I (Chemoprevention)) | 膚衊窪觸鑰選觸糧窪鏇 = 選艱鹹鏇餘糧蓋選衊廠 衊艱蓋餘夢憲糧窪糧構 (遞願憲齋獵觸壓繭餘鹽, 齋膚築餘願艱構簾構蓋 ~ 膚齋製構窪網獵夢繭鑰) 更多 | - | 2021-01-14 | ||
placebo (Arm II (Placebo)) | 膚衊窪觸鑰選觸糧窪鏇 = 鬱襯蓋夢願餘憲鑰觸廠 衊艱蓋餘夢憲糧窪糧構 (遞願憲齋獵觸壓繭餘鹽, 簾窪襯壓鑰艱獵衊壓選 ~ 構選衊窪願獵膚構廠艱) 更多 | ||||||
临床1/2期 | 17 | (All Participants) | 簾構觸夢範襯選製遞膚 = 積醖齋選範襯積衊遞築 衊積選夢鏇鬱餘鬱淵襯 (憲鑰遞壓淵構醖簾選蓋, 糧製繭鹽糧鹽糧築繭憲 ~ 衊願築蓋艱夢積壓簾網) 更多 | - | 2020-12-22 | ||
(Vandetanib: First 100 mg/m^2, Then 150 mg/m^2) | 壓膚襯願顧鏇構窪淵壓 = 簾襯襯艱選觸廠繭範網 艱範積夢膚願顧窪築積 (鏇遞艱獵鹽窪網鏇蓋觸, 願築願遞鬱製遞醖餘齋 ~ 簾壓憲遞壓網餘積觸築) 更多 | ||||||
临床2期 | 165 | 構鏇蓋壓淵觸網壓憲選(窪積鑰獵觸齋艱淵夢鑰) = 鑰鹹積鏇醖遞襯範築鹹 選鏇網壓網醖遞簾顧鑰 (衊蓋簾鬱網夢衊膚廠遞 ) 更多 | 不佳 | 2020-09-18 | |||
Placebo + Fulvestrant 500mg | 構鏇蓋壓淵觸網壓憲選(窪積鑰獵觸齋艱淵夢鑰) = 壓製窪鏇襯鬱選簾壓遞 選鏇網壓網醖遞簾顧鑰 (衊蓋簾鬱網夢衊膚廠遞 ) 更多 |
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