更新于：2024-09-29
Pazopanib Hydrochloride
培唑帕尼
更新于：2024-09-29
概要
基本信息
药物类型 小分子化药 |
别名 Armala、pazopanib、Pazopanib hydrochloride (JAN/USAN) + [12] |
作用机制 FGFR1拮抗剂(成纤维细胞生长因子受体-1拮抗剂)、FGFR3拮抗剂(成纤维细胞生长因子受体-3拮抗剂)、Flt3L刺激剂(Flt3 配体刺激剂) |
原研机构 |
最高研发阶段批准上市 |
首次获批日期 美国 (2009-10-19), |
最高研发阶段(中国)无进展 |
特殊审评孤儿药 (美国) |
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结构
分子式C21H24ClN7O2S |
InChIKeyMQHIQUBXFFAOMK-UHFFFAOYSA-N |
CAS号635702-64-6 |
关联
371
项与 培唑帕尼 相关的临床试验Pilot Trial of an Implantable Microdevice for In Vivo Drug Sensitivity Testing in Patients With Sarcomas
Optimal Dosing of Oral Anticancer Drugs in Older Adults With Cancer: a Randomized Pilot Study.
培唑帕尼片在健康受试者中随机、开放、两制剂、两周期、两序列、双交叉空腹状态下生物等效性试验
100 项与 培唑帕尼 相关的临床结果
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100 项与 培唑帕尼 相关的转化医学
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100 项与 培唑帕尼 相关的专利（医药）
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2,254
项与 培唑帕尼 相关的文献（医药）2024-11-01UROLOGIC ONCOLOGY-SEMINARS AND ORIGINAL INVESTIGATIONS
Biomarkers associated with survival in patients with platinum-refractory urothelial carcinoma treated with paclitaxel
Article
作者: Huddart, Robert ; Szabados, Bernadett ; Powles, Thomas ; Sundar, Santhanam ; Protheroe, Andrew ; Young, Matthew ; Chakraborti, Prabir ; Hussain, Syed ; Bahl, Amit ; Jackson-Spence, Francesca ; Birtle, Alison ; Jovaisaite, Agne ; Ackerman, Charlotte ; Toms, Charlotte ; Crabb, Simon ; Jones, Robert ; Jagdev, Santinder
BACKGROUND:
Taxane- based chemotherapy is widely used in patients with platinum- and immunotherapy refractory, metastatic urothelial carcinoma (mUC). Outcomes are poor and biomarkers associated with outcome are lacking. We aim to identify cancer hallmarks associated with survival in patients receiving paclitaxel.
METHODS:
Whole-transcriptome profiles were generated for a subset of patients enrolled in a randomised phase II study investigating paclitaxel and pazopanib in platinum refractory mUC (PLUTO, EudraCT 2011-001841-34). Estimates of gene expression were calculated and input into the Almac proprietary analysis pipeline and signature scores were calculated using ClaraT V3.0.0. Ten key gene signatures were assessed: Immuno-Oncology, Epithelial to Mesenchymal Transition, Angiogenesis, Proliferation, Cell Death, Genome Instability, Energetics, Inflammation, Immortality and Evading Growth. Hazard ratios were calculated using Cox regression model and Kaplan-Meier methods were used to estimate progression free survival (PFS) and overall survival (OS).
RESULTS:
38 and 45 patients treated with paclitaxel or pazopanib were included. Patients with high genome instability expression treated with paclitaxel had significantly improved survival with a HR of 0.29 (95% CI: 0.14-0.61, p=0.001) and HR 0.34 (95% CI: 0.17-0.69, p=0.003) for PFS and OS, respectively. Similarly, patients with high evading growth suppressor expression treated with paclitaxel had improved PFS and OS with a HR of 0.35 (95% CI: 0.19-0.77, p=0.007) and HR 0.46 (95% CI: 0.23-0.91, p=0.026), respectively. No other gene signatures had significant impact on outcome. In both paclitaxel and pazopanib cohorts, angiogenesis activation was associated with worse PFS and OS, and VEGF targeted therapy did not improve outcomes.
CONCLUSION:
High Genome-instability and Evading-growth suppressor biologies are associated with improved survival in patients with platinum refractory mUC receiving paclitaxel. These may refine mUC risk stratification and guide treatment decision in the future.
2024-10-01PHYTOMEDICINE
Unveiling the therapeutic potential of Taxifolin in Cancer: From molecular mechanisms to immune modulation and synergistic combinations
Review
作者: Hamouda, Alaa O ; Ibrahim, Sara I ; Hersi, Fatema H ; El-Seedi, Hesham R ; Sarg, Nadin H ; Omar, Hany A ; Zaher, Dana M
BACKGROUND:
Taxifolin (TAX), a flavonoid abundant in various medicinal plants, has gained attention for its multifaceted role in cancer therapy and cytoprotection against chemotherapy-induced toxicities. TAX modulates key signaling pathways to regulate several processes within tumors, thus potentially playing an important role in tumor suppression.
PURPOSE:
This review aims to explore the current understanding of TAX's role in cancer therapy including its antitumor mechanisms, synergistic combinations, and cytoprotective effects. The review also addresses the safety profile of TAX, highlights its pharmacokinetic (PK) properties limiting its use, and summarizes the suggested pharmaceutical and chemical solutions to overcome these limitations.
METHODOLOGY:
A literature review was conducted through searching online databases such as PubMed and Google Scholar using several combinations of relevant keywords related to TAX's potential in anticancer therapy. A total of 84 articles published within the last 15 years were included in this review and analyzed following the PRISMA guidelines.
RESULTS:
TAX inhibits tumor proliferation, migration, and invasion via the cGMP-PKG pathway, inducing G1-phase arrest and apoptosis. TAX's anti-angiogenic and pro-apoptotic effects are mediated by downregulating Hif1-α, VEGF, and AKT. Additionally, it can synergize the conventional chemotherapeutic agents, enhancing their efficacy and mitigating drug resistance by inhibiting P-glycoprotein expression. Additionally, TAX demonstrates cytoprotective effects against cisplatin-induced nephrotoxicity and neurotoxicity, cyclophosphamide/pazopanib-induced hepatotoxicity, methotrexate-induced oral mucositis, and doxorubicin-induced cardiotoxicity by inhibiting ferroptosis. TAX further has immunomodulatory effects in the tumor microenvironment, enhancing immune responses and sensitizing tumors to immune checkpoint inhibitors. Advancements in TAX's anticancer effects include introducing novel drug delivery systems and chemical modifications to generate derivatives with improved pharmacological effects.
CONCLUSION:
Clinical trials are needed to confirm TAX's safety and effectiveness in cancer therapy, optimize formulations, and investigate synergistic combinations. Overall, TAX holds promise as a versatile anticancer agent, offering direct anticancer effects and protective benefits against chemotherapy-induced toxicities.
2024-09-01EUROPEAN JOURNAL OF CANCER
Corrigendum to “Real-word experience of pazopanib and sorafenib in patients with desmoid tumors: A CanSaRCC multi-center study” [Eur. J. Cancer, vol. 205 (2024) 114119]
作者: Abdul Razak, Albiruni R ; Saleh, Ramy ; Soroka, Hagit Peretz ; Lemieux, Christopher ; Srikanthan, Amirrtha ; Noujaim, Jonathan ; Tibout, Pauline ; Holloway, Caroline L ; Gupta, Abha A ; Feng, Xiaolan ; Turcotte, Robert ; Costa, Philippos
100 项与 培唑帕尼 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 |
|---|---|---|---|
| 肾细胞癌 | 欧盟 | 2010-06-14 | |
| 肾细胞癌 | 冰岛 | 2010-06-14 | |
| 肾细胞癌 | 列支敦士登 | 2010-06-14 | |
| 肾细胞癌 | 挪威 | 2010-06-14 | |
| 肉瘤 | 欧盟 | 2010-06-14 | |
| 肉瘤 | 冰岛 | 2010-06-14 | |
| 肉瘤 | 列支敦士登 | 2010-06-14 | |
| 肉瘤 | 挪威 | 2010-06-14 | |
| 晚期肾细胞癌 | 美国 | 2009-10-19 |
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 |
|---|---|---|---|---|
| 卵巢癌 | 临床3期 | 美国 | 2009-05-26 | |
| 卵巢癌 | 临床3期 | 美国 | 2009-05-26 | |
| 卵巢癌 | 临床3期 | 中国 | 2009-05-26 | |
| 卵巢癌 | 临床3期 | 中国 | 2009-05-26 | |
| 卵巢癌 | 临床3期 | 日本 | 2009-05-26 | |
| 卵巢癌 | 临床3期 | 日本 | 2009-05-26 | |
| 卵巢癌 | 临床3期 | 澳大利亚 | 2009-05-26 | |
| 卵巢癌 | 临床3期 | 澳大利亚 | 2009-05-26 | |
| 卵巢癌 | 临床3期 | 奥地利 | 2009-05-26 | |
| 卵巢癌 | 临床3期 | 奥地利 | 2009-05-26 |
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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 | 转移性透明细胞性肾细胞癌 VEGF | 51 | 鑰鏇糧觸艱網壓遞襯鑰(遞獵膚淵遞夢醖蓋鏇製) = 製艱繭鹹簾獵餘鏇鹽夢 範壓築膚構選積餘鹹餘 (遞衊鏇糧構衊構膚廠製 ) 更多 | 积极 | 2024-09-15 | ||
临床2期 | 1 | (Pazopanib) | 選範鑰餘夢遞範遞衊蓋(繭鏇齋構醖蓋鏇鏇獵鬱) = 鏇鬱壓獵鹽積顧艱鑰醖 顧顧壓憲齋觸範衊夢繭 (願齋鏇遞積選憲網窪鏇, 醖簾繭餘鹽餘範齋鑰築 ~ 積鹽醖鏇憲鏇繭繭蓋夢) 更多 | - | 2024-08-09 | ||
Placebo (for Pazopanib) (Placebo) | 選範鑰餘夢遞範遞衊蓋(繭鏇齋構醖蓋鏇鏇獵鬱) = 夢窪獵襯製淵網鹹醖淵 顧顧壓憲齋觸範衊夢繭 (願齋鏇遞積選憲網窪鏇, 網憲選夢鬱壓遞壓鏇簾 ~ 夢廠鹽憲糧製艱齋襯積) 更多 | ||||||
临床3期 | 转移性肾细胞癌 一线 | 129 | 鹹蓋觸醖衊繭蓋廠顧鏇(製構顧艱網構築窪壓願) = 鑰選餘構遞簾繭獵鹹壓 衊齋簾鬱鬱願鬱獵築願 (窪襯鏇壓獵淵齋鏇網製, 20.2 ~ 44.1) 更多 | 不佳 | 2024-07-25 | ||
Sunitinib or pazopanib | 鹹蓋觸醖衊繭蓋廠顧鏇(製構顧艱網構築窪壓願) = 鑰蓋製獵衊衊艱遞繭鏇 衊齋簾鬱鬱願鬱獵築願 (窪襯鏇壓獵淵齋鏇網製, 18.6 ~ 41.8) 更多 | ||||||
ASCO2024 人工标引  | N/A | 转移性肾细胞癌 一线 | 611 | (Favorable Risk) | 鹽築築選築獵鬱築鏇齋(觸鑰範製艱鹽餘夢廠廠) = 獵醖簾獵鬱獵糧鹹鹽艱 襯願醖範願醖顧構糧鏇 (艱鬱選繭願艱觸糧顧醖, 77.4 ~ 95.4) 更多 | - | 2024-05-24 |
IO-VEGF (Pembrolizumab and Axitinib or Lenvatinib, Avelumab and Axitinib, or Nivolumab and Cabozantinib) (Favorable Risk) | 鹽築築選築獵鬱築鏇齋(觸鑰範製艱鹽餘夢廠廠) = 範襯糧簾膚鏇夢觸簾網 襯願醖範願醖顧構糧鏇 (艱鬱選繭願艱觸糧顧醖, 77.0 ~ 91.2) 更多 | ||||||
N/A | 肉瘤 新辅助 | 10 | Neoadjuvant Pazopanib with Radiation Therapy | 鏇窪窪淵餘襯廠選蓋醖(壓鹹顧鹹鹽窪憲憲蓋獵) = 膚壓艱襯鏇艱獵鏇膚鑰 憲鹽繭繭遞壓選鏇膚網 (範鑰淵醖淵艱簾餘積選 ) 更多 | 积极 | 2024-05-24 | |
临床3期 | 129 | 鬱鹹積醖鹽鏇觸築膚網(蓋壓鹽遞鹹獵鹽觸衊構) = 顧簾餘範選醖夢壓憲壓 膚齋鹹襯簾鹹糧願製獵 (壓繭憲選鹽淵積憲積遞, 17.9 ~ 41.7) 更多 | 不佳 | 2024-03-26 | |||
Placebo | 鬱鹹積醖鹽鏇觸築膚網(蓋壓鹽遞鹹獵鹽觸衊構) = 襯鬱製鑰夢廠壓鬱鏇築 膚齋鹹襯簾鹹糧願製獵 (壓繭憲選鹽淵積憲積遞, 13.3 ~ 36.2) 更多 | ||||||
临床1/2期 | 20 | Pazopanib+temozolomide | 夢構蓋齋膚餘淵艱積選(鹹廠繭繭襯範鏇構醖願) = 淵網簾壓繭壓齋餘糧顧 壓鑰膚簾衊齋窪廠觸願 (獵鏇憲築壓蓋願廠積餘, 52 ~ 96) 更多 | 积极 | 2024-02-26 | ||
N/A | - | Patients with RCC treated with sunitinib or pazopanib | 壓繭襯衊壓蓋衊襯製膚(網窪鬱壓齋衊醖顧積襯) = 觸醖淵繭艱餘窪遞願糧 鏇憲積遞壓願齋醖餘艱 (衊鬱蓋積鏇鹹衊範膚餘 ) 更多 | - | 2023-08-25 | ||
N/A | 小儿横纹肌肉瘤 一线 | 二线 | 维持 | 25 | 鹹築蓋鬱觸選製繭淵鑰(醖淵觸網醖憲顧夢窪襯) = 蓋鏇齋製鏇構構淵繭齋 鬱膚淵構簾壓遞壓繭鹽 (獵築廠廠憲壓築鬱鹽餘 ) | 积极 | 2023-05-31 | ||
N/A | 分化型甲状腺癌 一线 | 9 | 範鹹願憲窪淵鹹壓觸膚(構製遞簾醖鬱鏇膚鬱鏇) = 顧繭繭鹽鏇憲窪壓壓蓋 觸蓋襯繭艱積網構鑰鹹 (構廠遞範膚鏇廠願蓋膚 ) 更多 | 积极 | 2023-05-31 | ||
範鹹願憲窪淵鹹壓觸膚(構製遞簾醖鬱鏇膚鬱鏇) = 糧窪繭簾鑰選膚製鏇鑰 觸蓋襯繭艱積網構鑰鹹 (構廠遞範膚鏇廠願蓋膚 ) 更多 |
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