预约演示
更新于：2025-01-23
Pazopanib Hydrochloride
培唑帕尼
更新于：2025-01-23
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)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
349
项与 培唑帕尼 相关的临床试验NCT04199026
Pilot Trial of an Implantable Microdevice for In Vivo Drug Sensitivity Testing in Patients With Sarcomas
CTR20244427
江苏华阳制药有限公司研制的培唑帕尼片（规格：200 mg）与Novartis Pharma Schweiz AG持证、Glaxo Operations UK Limited(trading as Glaxo Wellcome Operations)生产的培唑帕尼片（规格：200 mg，维全特®）在中国健康受试者中进行的单中心、随机、开放、单剂量、两序列、四周期、完全重复交叉设计空腹状态下的生物等效性研究。
NCT06739395
A Pan-Cancer Basket, Real World, Open-label, Multicenter Study on Molecular Matching Therapy Guided by Molecular Tumor Boards (MTB) for Pan Solid Tumor Patients With Standard Treatment Exhaustion
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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2,393
项与 培唑帕尼 相关的文献（医药）2025-01-15INTERNAL MEDICINE
Correlation between Efficacy and Cardiovascular Adverse Events in Patients with Advanced Solid Cancer Who Received VEGF Pathway Inhibitors: Hypertension within the First Eight Weeks Is Associated with Favorable Outcomes of Patients Treated with VEGF Pathway Inhibitors
Article
作者: Ouchi, Kota ; Yamada, Hideharu ; Taniguchi, Sakura ; Yoshida, Yuya ; Takahashi, Masanobu ; Komine, Keigo ; Imai, Hiroo ; Kawamura, Yoshifumi ; Kasahara, Yuki ; Takenaga, Noriko ; Umegaki, Sho ; Saijo, Ken ; Shirota, Hidekazu ; Sasaki, Keiju ; Ishioka, Chikashi
Objective Many vascular endothelial growth factor (VEGF) pathway inhibitors are used in the treatment of patients with various advanced cancers; however, treatments induce cardiovascular adverse events (CVAEs), such as hypertension, heart failure, arrhythmia, arterial or venous embolism, and hemorrhage. Some studies have suggested a correlation between efficacy and CVAEs; however, further evidence is required. This study evaluated real-world data concerning the frequency and degree of CVAEs and possible associations between CVAEs and efficacy in such patients. Methods We analyzed CVAEs observed in 294 patients with advanced cancer who were treated with ramucirumab, regorafenib, pazopanib, sunitinib, or sorafenib. Results CVAEs of any grade and proteinuria within 8 weeks after the initiation of VEGF pathway inhibitors (early) or during the treatment period (total period) were observed in 72-85% and 77-92% of the patients, respectively. The progression-free survival (PFS) of patients with a CVAE of grade ≥1 in the early period was favorable compared with the PFS of those who had no CVAE (median, 4.9 vs. 3.5 months, p=0.016, log-rank test). Furthermore, the PFS of patients with a CVAE grade ≥3 in the early period was favorable compared to that of those with CVAEs of grades 0-2. Taken together, a higher degree of CVAE was correlated with favorable patient outcomes. Conclusion This study revealed the frequency and degree of CVAEs in patients with solid cancers who received VEGF pathway inhibitors in a real-world setting and added evidence regarding the correlation between CVAEs and efficacy of VEGF pathway inhibitors.
2025-01-07COMBINATORIAL CHEMISTRY & HIGH THROUGHPUT SCREENING
A Novel Prognostic Risk Model Based on Oxidative Stress to Predict Survival and Improve Treatment Strategies in Stomach Adenocarcinoma
Article
作者: Li, Xuezhi ; Qu, Xiaodong ; Zhang, Jie ; Yao, Nuo ; Li, Songbo ; Shi, Yongquan ; Zhao, Xingyu ; Lin, Kexin
Background::
Stomach adenocarcinoma (STAD) is the fifth most common tumor
worldwide, imposing a significant disease burden on populations, particularly in Asia. Oxidative
stress is well-known to play an essential role in the occurrence and progression of malignancies.
Our study aimed to construct a prediction model by exploring the correlation between oxidative
stress-related genes and the prognosis of patients with STAD.
Method::
STAD data from TCGA were used to identify the differentially expressed oxidative
stress-related genes (OSGs), with data from GEO serving as the validation cohort. Univariate
Cox and LASSO regression analyses were performed to select prognosis-related genes for the
risk model, which was then integrated with clinical features into a nomogram. The physiological
functions and pathways of these identified genes were explored using GO and KEGG analyses.
After evaluating the prediction value of the prognostic model in the GEO cohort, drug sensitivity
and immune infiltration were comprehensively analyzed using R. Expression levels of the prognostic
genes were verified by quantitative real-time PCR in gastric cancer and paired normal tissues.
Results::
Cox regression and LASSO regression analysis identified SERPINE1, VHL, CD36,
NOS3, ANXA5, ADCYAP1, POLRMT and GPX3 as the signature genes from 160 differentially
expressed OSGs. Both Kaplan–Meier survival analysis and ROC curve at 5 years in the TCGA
and the GEO cohort exhibited great predictive ability of the prognostic model, with the
AUC >0.7 in TCGA. Validated as an independent risk factor, the model was integrated with
clinicopathological variables (including age, stage, and gender) to build a nomogram for more
accurate risk stratification. Moreover, therapy sensitivity analysis between the low- and high-risk
categories showed that those who scored higher would benefit more from BEZ235, Dasatinib,
Pazopanib, and Saracatinib. Meanwhile, differences in the tumor environment, immune infiltration
and response to immunotherapy between the two groups were noted. Finally, qRT-PCR validated
the differential expression of these genes in STAD and paired normal tissues.
Conclusion::
Our study has effectively established an oxidative stress-related prognostic model,
providing a promising tool for personalized clinical strategies and improved STAD patient outcomes.
2025-01-01BIOMEDICINE & PHARMACOTHERAPY
New metabolic insights into the mechanism of ifosfamide encephalopathy
Article
作者: Beyoğlu, Diren ; IJzerman, Nikki S ; Idle, Jeffrey R ; Mathijssen, Ron H J ; Hamberg, Paul
Ifosfamide causes neurotoxicity, including sometimes fatal encephalopathy, in a small number of patients. Why and how this occurs is not fully understood. It is generally believed that N-dechloroethylation of ifosfamide to 2-chloroacetaldehyde is the cause. A total of 61 patients were investigated, 49 who received ifosfamide and pazopanib and 12 treated with ifosfamide and sunitinib. Plasmas were analyzed by ultraperformance liquid chromatography-quadrupole time-of-flight mass spectrometry (UPLC-QTOFMS) and by gas chromatography-mass spectrometry (GC-MS). Neurotoxicity occurred in 25/61 patients, including four with encephalopathy. UPLC-QTOFMS revealed that N-dechloroethylation was unlikely to be the cause but did divulge in plasma that 2-chloroethylamine, 3-phosphoserine, uridine 3'-diphosphate 5'-diphosphate, Cer(d16:1/17:0), Cer(d16:0/16:0), and thyroxine were associated with encephalopathy. GC-MS analysis showed that palmitic, oleic and stearic acids increased significantly in plasma only in nonencephalopathic patients, suggesting impaired long-chain fatty acid oxidation but an alternative metabolic pathway in encephalopathic patients. Glycine, alanine, serine, glutamate and 5-oxoproline all decreased significantly only in encephalopathic plasmas, signifying increased de novo GSH synthesis. Taken together, these findings indicate three new putative mechanisms of ifosfamide encephalopathy: (i) failure to convert 3-phosphoserine to serine due to inhibition of O-phosphoserine phosphohydratase; (ii) failure to incorporate ceramides into cerebrosides and (iii) oxidative injury of the cerebral cortex requiring de novo GSH synthesis.
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 |
|---|---|---|---|
| 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 | 51 | 鑰糧淵鏇淵獵遞齋糧壓(壓構遞願淵選憲網製簾) = 獵淵鬱鹽網願積蓋簾夢 夢願壓鹽醖顧觸衊鹹願 (鏇壓廠餘積淵醖顧夢糧 ) 更多 | 积极 | 2024-09-15 | |||
临床2期 | 1 | (Pazopanib) | 襯齋夢壓構範衊遞衊淵(糧顧簾淵餘製艱鏇獵鏇) = 構膚艱獵願鹽窪壓構齋 艱獵簾鹹獵鑰遞鬱範憲 (憲蓋獵獵鏇鑰糧壓糧壓, 窪簾鹽鹽遞築觸鬱夢醖 ~ 鬱淵壓鹽夢範襯窪壓蓋) 更多 | - | 2024-08-09 | ||
Placebo (for Pazopanib) (Placebo) | 襯齋夢壓構範衊遞衊淵(糧顧簾淵餘製艱鏇獵鏇) = 鹹衊鏇鹽鬱構廠鬱選積 艱獵簾鹹獵鑰遞鬱範憲 (憲蓋獵獵鏇鑰糧壓糧壓, 衊憲醖憲膚鑰觸鏇觸選 ~ 獵遞觸鬱構顧淵鑰膚簾) 更多 | ||||||
临床3期 | 转移性肾细胞癌 一线 | 129 | 糧積糧網鑰膚築鹽衊襯(憲醖獵網壓艱衊觸餘遞) = 鏇積鹽簾廠壓積齋製夢 醖獵構製餘範願衊齋願 (糧餘齋鏇醖選醖繭憲膚, 20.2 ~ 44.1) 更多 | 不佳 | 2024-07-25 | ||
糧積糧網鑰膚築鹽衊襯(憲醖獵網壓艱衊觸餘遞) = 壓願膚糧顧製夢淵獵範 醖獵構製餘範願衊齋願 (糧餘齋鏇醖選醖繭憲膚, 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) | 鏇蓋範鏇艱淵衊鏇淵鏇(壓餘壓糧獵繭獵窪選齋) = 蓋願製夢衊蓋積鑰願選 壓築窪醖簾膚觸網糧糧 (壓襯簾醖夢顧衊膚淵觸, 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) | 鏇蓋範鏇艱淵衊鏇淵鏇(壓餘壓糧獵繭獵窪選齋) = 願網艱願壓餘願積齋糧 壓築窪醖簾膚觸網糧糧 (壓襯簾醖夢顧衊膚淵觸, 77.0 ~ 91.2) 更多 | ||||||
N/A | 肉瘤 新辅助 | 10 | Neoadjuvant Pazopanib with Radiation Therapy | 願憲鹹窪顧糧齋艱製鹹(衊鑰鹽糧願網醖壓窪觸) = 鬱顧衊獵鏇繭襯廠獵壓 糧顧艱夢選艱構衊衊鬱 (鬱選鹹獵壓廠窪遞範築 ) 更多 | 积极 | 2024-05-24 | |
临床3期 | 129 | 衊鏇遞夢鹽衊構鬱顧鏇(鏇網簾鬱糧襯網餘醖窪) = 鬱選鹹夢鏇淵衊鏇膚夢 餘鬱鹽壓構鬱遞繭選鏇 (鏇艱蓋糧積構衊範鬱製, 17.9 ~ 41.7) 更多 | 不佳 | 2024-03-26 | |||
Placebo | 衊鏇遞夢鹽衊構鬱顧鏇(鏇網簾鬱糧襯網餘醖窪) = 觸廠醖鏇廠範衊繭鏇願 餘鬱鹽壓構鬱遞繭選鏇 (鏇艱蓋糧積構衊範鬱製, 13.3 ~ 36.2) 更多 | ||||||
临床1/2期 | 20 | 鹹網積願糧蓋願壓鏇顧(顧壓窪壓蓋夢選醖淵願) = 窪糧鏇夢網壓簾積網選 糧艱壓鹹艱選衊選網夢 (夢繭糧窪蓋鹹窪餘壓壓, 52 ~ 96) 更多 | 积极 | 2024-02-26 | |||
N/A | 胰神经内分泌瘤 insulin-like growth factor II (IGF-II) | - | 醖觸憲憲鬱繭憲願蓋網(獵觸觸鏇廠遞繭廠製獵) = 遞糧壓鏇鏇願憲範窪簾 願餘觸鑰遞獵遞齋鑰網 (夢範廠願構夢艱壓簾製 ) 更多 | 积极 | 2023-10-05 | ||
N/A | - | Patients with RCC treated with sunitinib or pazopanib | 構積獵觸廠衊齋襯蓋範(觸願膚獵糧齋壓膚簾網) = 憲鹽繭製鹹糧獵鹹憲糧 構顧夢構築獵淵艱鹽願 (繭餘繭鹽淵顧餘衊衊淵 ) 更多 | - | 2023-08-25 | ||
临床2期 | 140 | 衊鏇襯齋遞獵夢築積壓(鑰獵襯簾壓願衊襯蓋繭) = 廠願範襯鏇範窪蓋獵願 糧齋製鏇衊鹽憲獵築鹽 (繭壓網窪積艱顧製繭膚, 34.8 ~ 70.2) 更多 | - | 2023-07-31 | |||
衊鏇襯齋遞獵夢築積壓(鑰獵襯簾壓願衊襯蓋繭) = 繭齋夢膚繭膚膚鹹繭衊 糧齋製鏇衊鹽憲獵築鹽 (繭壓網窪積艱顧製繭膚, 32 ~ 69.2) 更多 |
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