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更新于：2025-06-20
Pazopanib Hydrochloride
培唑帕尼
更新于：2025-06-20
概要
基本信息
药物类型 小分子化药 |
别名 Armala、pazopanib、Pazopanib hydrochloride (JAN/USAN) + [12] |
作用方式 拮抗剂、刺激剂、抑制剂 |
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 |
权益机构 |
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)批准上市 |
特殊审评孤儿药 (美国) |
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结构/序列
分子式C21H24ClN7O2S |
InChIKeyMQHIQUBXFFAOMK-UHFFFAOYSA-N |
CAS号635702-64-6 |
关联
333
项与 培唑帕尼 相关的临床试验ChiCTR2500096689
Evaluation of efficacy and safety of pazopanib combined with TGI/CIV(nab?Paclitaxel+ gemcitabine + isocyclophosphamide/cyclophosphamide +Irinotecan + vinorelbine) in the treatment for children or adolescents with recurrent/refractory rhabdomyosarcoma ——an open-label, single-arm, single-center,phase II clinical trial
NCT04199026
Pilot Trial of an Implantable Microdevice for In Vivo Drug Sensitivity Testing in Patients With Sarcomas
NCT06816771
Evaluation of Efficacy and Safety of Pazopanib Combined with TGI/CIV(nab⁃Paclitaxel+ Gemcitabine + Ifosfamide/cyclophosphamide +Irinotecan + Vinorelbine) in the Treatment for Children or Adolescents with Recurrent/refractory Rhabdomyosarcoma--an Open-label, Single-arm, Single-cente,phase II Clinical Trial
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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3,740
项与 培唑帕尼 相关的文献（医药）2025-12-31ANNALS OF MEDICINE
A novel glycogene-related signature for prognostic prediction and immune microenvironment assessment in kidney renal clear cell carcinoma
Article
作者: Zhao, Danni ; Cui, Hanxiao ; Ren, Xueting ; Zhao, Xuyan ; Kang, Huafeng ; Li, Zihao ; Liu, Peinan ; Lin, Shuai ; Zhou, Mingjing
BACKGROUND:
Kidney Renal Clear Cell Carcinoma (KIRC) is a prevalent urinary malignancies worldwide. Glycosylation is a key post-translational modification that is essential in cancer progression. However, its relationship with prognosis, tumour microenvironment (TME), and treatment response in KIRC remains unclear.
METHOD:
Expression profiles and clinical data were retrieved from The Cancer Genome Atlas and Gene Expression Omnibus databases. Consensus clustering, Cox regression, and LASSO regression analyses were conducted to develop an optimal glycogene-related signature. The prognostic relevance of this molecular signature was rigorously analyzed, along with its connections to tumour microenvironment (TME), tumour mutation burden, immune checkpoint activity, cancer-immunity cycle regulation, immunomodulatory gene expression patterns, and therapeutic response profiles. Validation was performed using real-world clinical specimens, quantitative PCR (qPCR), and immunohistochemistry (IHC), supported by cohort analyses from the Human Protein Atlas (HPA) database.
RESULTS:
A glycogene-associated prognostic scoring system was established to categorize patients into risk-stratified subgroups. Patients in the high-risk cohort exhibited significantly poorer survival outcomes (p < 0.001). By incorporating clinicopathological variables into this framework, we established a predictive nomogram demonstrating strong calibration and a concordance index (C-index) of 0.78. The high-risk subgroup displayed elevated immune infiltration scores (p < 0.001), upregulated expression of immune checkpoint-related genes (p < 0.05), and an increased frequency of somatic mutations (p = 0.043). The risk score positively correlated with cancer-immunity cycle activation and immunotherapy-related signals. The high-risk groups also showed associations with T cell exhaustion, immune-activating genes, chemokines, and receptors. Drug sensitivity analysis revealed that low-risk patients were more sensitive to sorafenib, pazopanib, and erlotinib, whereas high-risk individuals responded better to temsirolimus (p < 0.01). qPCR and IHC analyses consistently revealed distinct expression patterns of MX2 and other key genes across the risk groups, further corroborated by the HPA findings.
CONCLUSION:
This glycogene-based signature provides a robust tool for predicting prognosis, TME characteristics, and therapeutic responses in KIRC, offering potential clinical utility in patient management.
2025-09-01JOURNAL OF CHEMICAL THERMODYNAMICS
Molecular interaction and esterase activity of bovine serum albumin with Pazopanib using multi-spectroscopic techniques and molecular docking
作者: Jalan, Ankita ; Moyon, N. Shaemningwar ; Patar, Madhumita
This work delves into the binding dynamics of a promising anti-cancer drug Pazopanib (PZB) with bovine serum albumin (BSA), a mammalian plasma protein carrier with incredible ligand-binding properties.PZB is a tyrosine kinase inhibitor (TKI) used as a monotherapy against advanced renal cell carcinoma, soft tissue sarcoma, and liver fibrosis.Drug-albumin interactions vary with concentration, affecting drug efficacy and toxicity.Herein, we have investigated the binding mechanism of PZB with BSA at higher drug concentrations (5 x 10-6 mol/kg - 4 x 10-5 mol/kg) than albumin (3 x 10-6 mol/kg) using techniques like absorption, steady-state fluorescence, FRET, FT-IR, synchronous fluorescence, CD, and mol. docking.The intrinsic BSA fluorescence quenches with gradual increase in concentration of PZB via static quenching.The binding constant was found to be moderate (6.497 x 104 mol -1.kg) and it has only one binding site.The Forster distance (r) indicated probable transfer of energy between the donor BSA and acceptor PZB.The major interacting forces are hydrophobic forces and hydrogen bonding.Conformational change in the protein framework was revealed from synchronous fluorescence, FT-IR, and CD studies.Competitive binding experiments as well as docking studies suggest that PZB binds to site I (subdomain IIA) of BSA.The increase in kinetic parameters reveals that the catalytic efficiency of BSA is enhanced on PZB interaction.
2025-08-01INTERNATIONAL JOURNAL OF BIOCHEMISTRY & CELL BIOLOGY
Deciphering the molecular heterogeneity of soft tissue sarcoma by integrating multiomics and single cell sequence
Article
作者: Luo, Peng ; Jiang, Aimin ; Jiang, Hao ; Zhang, Haixiang ; Wu, Chunbiao ; Wei, Wei
BACKGROUND:
Soft tissue sarcoma is a highly malignant tumor with extensive heterogeneity across multiple omics. However, a comprehensive multi-omics subtyping system has not yet been established.
METHODS:
We integrated sarcoma multi-omics data, including clinical information, transcriptome expression profiles, DNA methylation, and somatic mutations. Using ten advanced clustering algorithms, we identified robust subtypes and validated the reproducibility of our analysis in two independent external datasets. We also identified subtype-specific treatment strategies and analyzed the differences in microenvironments between subtypes using single-cell data.
RESULTS:
Based on multi-omics subtyping, we identified two novel sarcoma molecular subtypes, named sarcoma multi-omics subtype 1 (SAMS1) and SAMS2. SAMS2 exhibited a poorer prognosis, with significantly activated Myc, glycolysis, and Wnt beta-catenin signaling pathways. SAMS2 was characterized by a lower abundance of immune cell infiltration and anti-tumor immunity deficiency, which owned a lower response rate to immunotherapy but was sensitive to certain targeted drugs, including pazopanib, axitinib, thapsigargin, and elesclomol. MK886 and NU1025 were identified as effective therapeutic targets for the SAMS2. In SAMS2-like tumor epithelial cells, HOXB13/COL16A1 and BASP1 regulated epithelial-mesenchymal transition. We found that WNT7B was highly expressed in STS and was associated with poor patient prognosis, suggesting its potential as a novel therapeutic target for STS patients.
CONCLUSION:
The STS molecular subtyping system based on multi-omics data effectively distinguishes patients with poor prognosis. The subtyping results are robust and reliable, providing new insights for the precise diagnosis and treatment of these patients.
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 |
|---|---|---|---|
| 转移性肾细胞癌 | 日本 | 2014-03-17 | |
| 软组织肿瘤 | 日本 | 2012-09-28 | |
| 肉瘤 | 美国 | 2012-04-26 | |
| 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 | |
| 软组织肉瘤 | 欧盟 | 2010-06-14 | |
| 软组织肉瘤 | 冰岛 | 2010-06-14 | |
| 软组织肉瘤 | 列支敦士登 | 2010-06-14 | |
| 软组织肉瘤 | 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 |
|---|---|---|---|---|
| 输卵管癌 | 临床3期 | 美国 | 2009-05-26 | |
| 输卵管癌 | 临床3期 | 美国 | 2009-05-26 | |
| 输卵管癌 | 临床3期 | 中国 | 2009-05-26 | |
| 输卵管癌 | 临床3期 | 中国 | 2009-05-26 | |
| 输卵管癌 | 临床3期 | 日本 | 2009-05-26 | |
| 输卵管癌 | 临床3期 | 日本 | 2009-05-26 | |
| 输卵管癌 | 临床3期 | 澳大利亚 | 2009-05-26 | |
| 输卵管癌 | 临床3期 | 澳大利亚 | 2009-05-26 | |
| 输卵管癌 | 临床3期 | 奥地利 | 2009-05-26 | |
| 输卵管癌 | 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 | 40 | (High-risk gene signature group) | 簾膚蓋繭鹽廠繭齋願願(鑰蓋顧顧糧範築憲遞積) = 製壓窪窪簾遞餘壓鹹壓 齋觸構夢鬱獵簾鹽獵願 (選繭廠獵構鬱艱鹹積窪, 3.7 ~ 10.0) | 积极 | 2025-05-30 | ||
(Low-risk gene signature group) | 簾膚蓋繭鹽廠繭齋願願(鑰蓋顧顧糧範築憲遞積) = 鏇築壓鬱餘夢獵壓淵衊 齋觸構夢鬱獵簾鹽獵願 (選繭廠獵構鬱艱鹹積窪, 6.5 ~ NR) | ||||||
临床2期 | 32 | 鹽鑰齋觸鹽鏇構鬱憲鑰 = 糧憲夢繭繭選鬱蓋憲艱 遞餘餘夢顧襯繭繭網鬱 (廠窪願製簾鏇艱構鏇鏇, 網廠齋獵範構鏇獵鑰鑰 ~ 鏇遞構壓窪鹹獵壓襯鹽) 更多 | - | 2025-05-02 | |||
N/A | 1,573 | 鬱糧簾鹽餘壓糧憲憲壓(窪鹽糧襯憲繭範廠網鏇) = 33% 齋鬱簾憲糧糧襯憲蓋窪 (膚廠壓窪窪糧餘顧壓築 ) 更多 | 积极 | 2025-03-21 | |||
Other TKIs | |||||||
临床2期 | 51 | 願廠廠遞簾蓋選醖餘鹽(壓膚簾選願選網餘淵醖) = 糧餘遞壓選選遞淵鏇獵 獵獵壓鏇構膚壓膚簾觸 (鹽襯鹽衊襯膚遞製糧願 ) 更多 | 积极 | 2024-09-15 | |||
临床2期 | 1 | (Pazopanib) | 觸膚繭網淵遞衊獵齋範 = 夢壓艱艱顧構繭鹹鑰窪 築壓壓艱夢積齋淵憲醖 (醖製鏇鬱觸鏇鑰糧蓋廠, 餘窪遞獵範遞壓遞鹹憲 ~ 製憲醖選觸鏇築鏇鹹簾) 更多 | - | 2024-08-09 | ||
Placebo (for Pazopanib) (Placebo) | 觸膚繭網淵遞衊獵齋範 = 顧獵鹽鏇襯淵觸繭鹹鏇 築壓壓艱夢積齋淵憲醖 (醖製鏇鬱觸鏇鑰糧蓋廠, 願範遞衊遞築窪醖艱蓋 ~ 餘範積範網艱獵繭淵憲) 更多 | ||||||
临床3期 | 转移性肾细胞癌 一线 | 129 | 鏇艱膚構夢鹹鬱衊獵簾(鹹簾鏇糧繭淵選簾選鏇) = 膚鏇築選廠構繭鏇觸鏇 鏇鹹壓繭糧繭襯壓鹽鏇 (襯糧鑰窪鹹膚衊襯構遞, 20.2 ~ 44.1) 更多 | 不佳 | 2024-07-25 | ||
鏇艱膚構夢鹹鬱衊獵簾(鹹簾鏇糧繭淵選簾選鏇) = 憲鏇蓋築範衊鹹鹹餘積 鏇鹹壓繭糧繭襯壓鹽鏇 (襯糧鑰窪鹹膚衊襯構遞, 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) | 鹹衊獵壓鹽獵鹹積觸願(齋淵艱廠膚網願範廠衊) = 膚鹽觸鹽齋餘齋廠蓋窪 鑰製願鹽齋醖壓鬱膚膚 (鹽網顧顧夢願製衊遞鏇, 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) | 鹹衊獵壓鹽獵鹹積觸願(齋淵艱廠膚網願範廠衊) = 衊築艱遞齋獵鑰鹽糧積 鑰製願鹽齋醖壓鬱膚膚 (鹽網顧顧夢願製衊遞鏇, 77.0 ~ 91.2) 更多 | ||||||
N/A | 肉瘤 新辅助 | 10 | Neoadjuvant Pazopanib with Radiation Therapy | 鬱夢醖構鬱醖製廠鑰網(憲鹹夢艱窪獵憲鏇獵衊) = 廠壓艱鏇衊壓範觸遞齋 鹽願鏇齋遞範夢蓋範鑰 (夢鏇鹽醖製選遞願壓膚 ) 更多 | 积极 | 2024-05-24 | |
临床3期 | 129 | 築衊淵鬱築範淵窪壓膚(範壓製餘膚衊築積網蓋) = 衊窪醖膚壓顧膚壓壓餘 蓋廠夢鬱願醖範壓蓋糧 (醖遞鹹鹹廠襯窪鏇鏇襯, 17.9 ~ 41.7) 更多 | 不佳 | 2024-03-26 | |||
Placebo | 築衊淵鬱築範淵窪壓膚(範壓製餘膚衊築積網蓋) = 憲糧積鑰鏇選膚蓋襯鹽 蓋廠夢鬱願醖範壓蓋糧 (醖遞鹹鹹廠襯窪鏇鏇襯, 13.3 ~ 36.2) 更多 | ||||||
临床1/2期 | 20 | 願遞網齋選窪淵憲醖鏇(顧窪鏇獵蓋鏇鬱鹽鹽餘) = 膚顧獵鏇鹽衊憲網選繭 齋鏇淵齋獵築鑰蓋淵遞 (網顧鬱壓壓夢蓋衊餘網, 52 ~ 96) 更多 | 积极 | 2024-02-26 |
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