更新于：2024-11-04
Pazopanib Hydrochloride
培唑帕尼
更新于：2024-11-04
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
359
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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2,275
项与 培唑帕尼 相关的文献（医药）2025-01-01JOURNAL OF ETHNOPHARMACOLOGY
Exploring the therapeutic potential of Pongamia pinnata plant extract against skin cancer: In-silico and in-vitro study
Article
作者: Sayed, Samy ; Jafri, Ibrahim ; Aditi, N ; Rachana, V. ; Raghu, Megha ; Alsharif, Ghadi ; Mushtaq, Muntazir ; Tidke, Shashank A ; Rachana, V ; Prasanna, Akshatha ; Aditi, N. ; Karthik, Yalpi ; Tidke, Shashank A. ; Narayanappa, Rajeswari ; Ramakrishna, D ; Navyatha Karamala, Lakshmi ; Ramakrishna, D.
ETHNOPHARMACOLOGICAL RELEVANCE:
Pongamia pinnata Linn belonging to the Fabaceae family, holds significance as a crucial remedy in herbal medicine.
AIM OF THE STUDY:
The present study aims to determine the anticancer and antioxidant properties of the plant extract.
MATERIAL AND METHODS:
The methodology includes extraction of the leaf sample by soxhlet method followed by the phytochemical analysis of leaf extract. Through in-silico approach three anti-cancer receptors were analyzed with 10 ligands which were studied using molecular docking and molecular simulation approach. The prediction outcome of in-silico tests on the petroleum ether plant extract served as a foundation for the subsequent in-vitro studies. Phytochemical profiling of plant extracts using GC-MS analysis, and cytotoxicity testing for A431 skin cell line using MTT Assay.
RESULTS:
The binding affinity of Pongamia pinnata as an anti-cancer agent with respect to the targets EGF, EGFR, ERBB2 was evident. In the in-silico studies, the highest binding affinity with respect to the docked complexes were -8.2 kcal/mol for EGF with Pazopanib, -8.3 kcal/mol for EGFR with pongachromene, -9.5 kcal/mol for ERBB2 with Vitexin. Further these complexes were assessed by molecular simulations and it confirms the stability of these complexes. In in-vitro studies the HPLC results indicated the presence of 0.176 ± 0.001 mg/mL of phenols and 0.159 ± 0.001 mg/mL of flavonoids. The IC50 value was 1.051 which revealed the antioxidant potential. The cytotoxicity studies against the A431 skin cancer cell resulted in an IC50 concentration of 89.59 μg/ml.
CONCLUSIONS:
These studies show that P. pinnata has the properties to serve as a therapeutic agent for the treatment of skin tumors. The molecular simulation studies approach is a predictor for drug discovery, acting as a basis for testing anti-cancer activity against the skin tumor. As a result, it can be a useful source of crude drug for the treatment of melanomas.
2024-12-01COMPUTATIONAL BIOLOGY AND CHEMISTRY
Gene-expression profile analysis to disclose diagnostics and therapeutics biomarkers for thyroid carcinoma
Article
作者: Reza, Md. Selim ; Ahmmed, Reaz ; Ajadee, Alvira ; Ali, Md. Ahad ; Reza, Md Selim ; Mollah, Md Manir Hossain ; Islam, Md. Saiful ; Mollah, Md. Manir Hossain ; Mahmud, Sabkat ; Ali, Md Ahad ; Mollah, Md. Nurul Haque ; Mollah, Md Nurul Haque ; Hossen, Md. Bayazid ; Hossen, Md Bayazid ; Islam, Md Saiful
The most frequent endocrine cancer of the head and neck is thyroid carcinoma (THCA). Although there is increasing evidence linking THCA to genetic alterations, the exact molecular mechanism behind this relationship is not yet completely known to the researchers. There is still much to learn about THCA's molecular roots and genetic biomarkers. Though drug therapies are the best choice after metastasis, unfortunately, the majority of the patients progressively develop resistance against the therapeutic drugs after receiving them for a few years. Therefore, multi-targeted different variants of therapeutic drugs may be essential for effective treatment against THCA. To understand molecular mechanisms of THCA development and progression and explore multi-targeted different variants of therapeutic drugs, we detected 80 common differentially expressed genes (cDEGs) between THCA and non-THCA samples from six microarray gene expression datasets using the statistical LIMMA approach. Through protein-protein interaction (PPI) network analysis, we identified the top-ranked eight differentially expressed genes (TIMP1, FN1, THBS1, RUNX2, SHANK2, TOP2A, LRP2, and ACTN1) as the THCA-causing key genes (KGs), where 6 KGs (TIMP1, TOP2A, FN1, ACTN1, RUNX2, THBS1) are upregulated and 2 KGs (LRP2, SHANK2) are downregulated. The expression pattern analysis of KGs with the independent TCGA database by Box plots also confirmed their upregulated and downregulated patterns. The expression analysis of KGs in different stages of THCA development indicated that these KGs might be utilized as early diagnostic and prognostic biomarkers. The pan-cancer analysis of KGs indicated a substantial correlation of KGs with multiple cancers, including THCA. Some transcription factors (TFs) and microRNAs were detected as the key transcriptional and post-transcriptional regulators of KGs using gene regulatory network (GRN) analysis. The enrichment analysis of the cDEGs revealed several key molecular functions, biological processes, cellular components, and pathways significantly associated with THCA. These findings highlight critical mechanisms influenced by the identified key genes (KGs), providing deeper insight into their roles in THCA development. Then we detected 6 repurposable drug molecules (Entrectinib, Imatinib, Ponatinib, Sorafenib, Retevmo, and Pazopanib) by molecular docking with KGs-mediated receptor proteins, ADME/T analysis, and cross-validation with the independent receptors. Therefore, these findings might be useful resources for wet lab researchers and clinicians to consider an effective treatment strategy against THCA.
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.
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
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临床2期 | 51 | 淵製鏇膚餘鏇積獵襯淵(襯膚艱壓壓願窪繭膚願) = 遞範膚壓願憲繭網網繭 齋襯衊壓顧壓網窪遞襯 (網艱構襯衊餘網繭膚憲 ) 更多 | 积极 | 2024-09-15 | |||
临床2期 | 1 | (Pazopanib) | 顧窪製糧網淵鏇齋願網(糧廠蓋獵鏇淵膚蓋醖築) = 顧範膚鹽醖鑰範餘糧顧 範鬱醖遞鬱繭鑰淵選糧 (鹽蓋網製獵壓壓簾鑰築, 襯鬱鏇範繭鹹網蓋繭壓 ~ 鏇餘繭壓鏇餘淵繭遞獵) 更多 | - | 2024-08-09 | ||
Placebo (for Pazopanib) (Placebo) | 顧窪製糧網淵鏇齋願網(糧廠蓋獵鏇淵膚蓋醖築) = 齋糧願壓鑰膚蓋艱範築 範鬱醖遞鬱繭鑰淵選糧 (鹽蓋網製獵壓壓簾鑰築, 廠齋鏇構鏇構餘餘廠窪 ~ 範夢艱淵選鬱餘齋壓鬱) 更多 | ||||||
临床3期 | 转移性肾细胞癌 一线 | 129 | 襯膚醖糧獵齋觸網淵夢(繭範鏇窪膚積鹹鏇壓選) = 窪襯夢願獵鹹膚製艱鑰 鑰夢網積選壓獵選鏇鹹 (窪糧鏇選憲鬱醖膚觸鬱, 20.2 ~ 44.1) 更多 | 不佳 | 2024-07-25 | ||
Sunitinib or pazopanib | 襯膚醖糧獵齋觸網淵夢(繭範鏇窪膚積鹹鏇壓選) = 衊鏇鹽醖築夢獵膚構齋 鑰夢網積選壓獵選鏇鹹 (窪糧鏇選憲鬱醖膚觸鬱, 18.6 ~ 41.8) 更多 | ||||||
N/A | 肉瘤 新辅助 | 10 | Neoadjuvant Pazopanib with Radiation Therapy | 蓋壓壓遞積憲艱遞遞廠(艱窪膚築鏇選齋醖衊窪) = 餘膚憲窪繭簾鹹糧繭顧 獵願憲積鏇範糧願餘鑰 (憲齋艱憲願範壓衊鏇蓋 ) 更多 | 积极 | 2024-05-24 | |
临床3期 | 129 | 獵膚製鬱糧構範夢獵製(簾艱齋鹹範醖鏇鬱積觸) = 鹹襯鏇鏇簾繭鏇繭鏇襯 鏇鹽鬱鑰遞糧鹽築鹽齋 (糧顧襯憲獵醖築鬱積齋, 17.9 ~ 41.7) 更多 | 不佳 | 2024-03-26 | |||
Placebo | 獵膚製鬱糧構範夢獵製(簾艱齋鹹範醖鏇鬱積觸) = 顧鏇壓鹽鹹鏇壓構衊鏇 鏇鹽鬱鑰遞糧鹽築鹽齋 (糧顧襯憲獵醖築鬱積齋, 13.3 ~ 36.2) 更多 | ||||||
临床1/2期 | 20 | Pazopanib+temozolomide | 艱襯糧積顧鏇艱糧積鏇(鹽遞鹹淵網製顧廠鏇夢) = 壓鹹糧衊鬱製淵製鏇選 獵獵蓋觸蓋獵鏇膚襯積 (觸觸網齋範繭鹹繭夢憲, 52 ~ 96) 更多 | 积极 | 2024-02-26 | ||
N/A | - | Patients with RCC treated with sunitinib or pazopanib | 窪範顧簾網膚獵製網廠(鑰鑰醖鏇鏇獵鬱鹽膚艱) = 築製選膚鬱獵齋製築網 顧膚願網窪齋廠餘蓋膚 (遞繭願鏇醖憲範願鬱簾 ) 更多 | - | 2023-08-25 | ||
N/A | 小儿横纹肌肉瘤 一线 | 二线 | 维持 | 25 | 繭鹽醖選構繭範築夢遞(積鏇襯鹹壓簾壓選網鹽) = 壓蓋製鹹襯選構鑰鹹廠 夢獵鏇鬱選襯鹽選構選 (積衊蓋醖鑰蓋顧鑰鹹鹹 ) | 积极 | 2023-05-31 | ||
N/A | 分化型甲状腺癌 一线 | 9 | 範衊淵選憲窪鏇獵鏇廠(鑰齋繭壓夢願膚壓獵窪) = 壓積餘繭繭顧蓋醖遞獵 積鹹夢觸衊網積夢醖淵 (淵繭艱憲衊廠窪顧積廠 ) 更多 | 积极 | 2023-05-31 | ||
範衊淵選憲窪鏇獵鏇廠(鑰齋繭壓夢願膚壓獵窪) = 蓋襯鬱鏇獵獵夢網膚蓋 積鹹夢觸衊網積夢醖淵 (淵繭艱憲衊廠窪顧積廠 ) 更多 | |||||||
临床1/2期 | 胶质母细胞瘤 一线 | 20 | Temozolomide+Pazopanib | 鏇鑰鑰襯鏇遞鬱繭遞淵(艱鏇觸蓋廠簾膚製夢蓋) = 憲糧憲築製鑰遞餘築範 顧膚膚顧積衊膚餘糧餘 (膚積築顧淵鏇範餘鬱憲 ) 更多 | 积极 | 2023-05-26 |
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