预约演示
更新于：2025-05-22
Dapoxetine Hydrochloride
盐酸达泊西汀
更新于：2025-05-22
概要
基本信息
权益机构- |
最高研发阶段批准上市 |
首次获批日期 英国 (2008-12-17), |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构/序列
分子式C21H24ClNO |
InChIKeyIHWDIQRWYNMKFM-BDQAORGHSA-N |
CAS号129938-20-1 |
关联
119
项与 盐酸达泊西汀 相关的临床试验CTR20250283
评价盐酸达泊西汀片在中国成年健康男性受试者中的一项单中心、随机、开放、空腹和餐后条件下单次给药、两制剂、两周期交叉的生物等效性研究
CTR20250171
盐酸达泊西汀片在中国成年健康男性受试者中的一项单中心、随机、开放、空腹和餐后单次给药、两制剂、两序列、两周期交叉的生物等效性研究
CTR20250263
山东济坤生物制药有限公司研制的盐酸达泊西汀片与参比制剂在中国健康受试者中进行的单中心、随机、开放、两制剂、空腹和餐后、单次给药、两周期、双交叉设计的生物等效性研究
100 项与 盐酸达泊西汀 相关的临床结果
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100 项与 盐酸达泊西汀 相关的转化医学
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100 项与 盐酸达泊西汀 相关的专利（医药）
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437
项与 盐酸达泊西汀 相关的文献（医药）2025-06-01BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR BASIS OF DISEASE
Both carvedilol and cimetidine alleviate cisplatin-induced nephrotoxicity via downregulating OCT2
Article
作者: Jiao, Xiaoyan ; Wu, Huan ; Ning, Yichun ; Sun, Zhaoxing ; Ji, Ji ; Yu, Xiaofang ; Ding, Xiaoqiang ; Cheng, Xin ; Xu, Xiaoliang ; Lu, Min
BACKGROUND:
Cisplatin is a common chemotherapy agent for solid tumors but severe nephrotoxicity limits its application, with no effective pharmacological treatments. Organic cation transporter 2 (OCT2) is involved in cisplatin uptake in kidneys. This study aimed to find drugs with promising clinical applications that could prevent cisplatin-induced acute kidney injury (Cis-AKI) by inhibiting OCT2.
METHODS:
The mRNA level of OCT2 was examined in human induced pluripotent stem cells (iPSCs) from Cis-AKI patients and paired non-AKI patients. The association between OCT2 and Cis-AKI was investigated by HEK293FT cells and kidney organoids. We screened potential compounds exhibiting protective effects against Cis-AKI in US Food and Drug Administration-approved drugs through virtual screening and activity screening. Subsequently, we determined the effects of these compounds on OCT2 expression, cisplatin uptake, and apoptosis in cells, kidney organoids and mice. A549 and HeLa cells were adopted to observe the influence of drugs on the anti-tumor function of cisplatin.
RESULTS:
Compared to non-AKI patients, the OCT2 mRNA levels of iPSCs from Cis-AKI patients were elevated. OCT2 exhibits similar expression patterns in kidney organoids and human kidney tissues. Furthermore, the overexpression of OCT2 in kidney organoids and HEK293FT cells exacerbated the injury caused by cisplatin. Carvedilol and cimetidine were identified as potent OCT2 inhibitors by drug screening. Further analysis revealed that the pretreatment of carvedilol or cimetidine downregulated OCT2, reduced cisplatin uptake, and alleviated cisplatin-induced apoptosis, but the combination of the two drugs didn't further improve these outcomes. Additionally, carvedilol and cimetidine didn't compromise the cisplatin-induced cell death in A549 and HeLa cells.
CONCLUSION:
Our study confirmed that carvedilol and cimetidine exert protective effects against Cis-AKI by inhibiting OCT2, without altering the anti-tumor effects of cisplatin.
2025-04-22ACS Omega
Unraveling the Anticancer Potential of SSRIs in Prostate Cancer by Combining Computational Systems Biology and In Vitro Analyses
Article
作者: AlJarrah, Hashem ; Jaradat, Esraa ; Bardaweel, Sanaa K. ; Hajjo, Rima
Selective serotonin reuptake inhibitors (SSRIs) are known to have anticancer activity against different types of cancer. In this study, an integrative informatics approach was applied to identify compound and genetic perturbations that produce similar effects to SSRIs to formulate systems biology hypotheses and identify biological pathways involved in the putative anticancer effects of SSRIs in prostate cancer. An 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay assessed the antiproliferative effects of SSRIs and drug combinations. Cell death mechanisms were studied using annexin V-FITC/PI staining, and the cell cycle analysis was carried out by counterstaining with propidium iodide. Relative gene expression was assessed using a real-time polymerase chain reaction (PCR). Computational results hypothesized that SSRIs could potentially exert anticancer effects in prostate cancer cell lines by modulating apoptotic and tumorigenesis pathways and significantly inhibiting the growth of prostate cancer cells in a time and concentration-dependent manner. The combination of SSRIs with cisplatin, 5-fluorouracil, and raloxifene resulted in either synergistic or additive effects. SSRIs resulted in a significant increase in the early and late apoptotic activity in PC3 cells. Dapoxetine, paroxetine, and sertraline resulted in cell cycle arrest at the G0/G1 phase. Treatment with either dapoxetine or paroxetine decreases the expression of Bcl-2, CASP8, DR5, and VEGF. At the same time, sertraline decreases the expression of Bcl-2 and VEGF and increases the expression of CASP8 and DR5. Results revealed that SSRIs can potentially act as antiproliferative agents against prostate cancer cells, and their activity is mediated through different signaling pathways.
2025-04-01SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY
Identification of Phosphodiesterase type 5 inhibitors (PDE5is) analogues using surface-enhanced Raman scattering and machine learning algorithm
Article
作者: Huang, Jiadong ; He, Hongyuan ; Li, Yujing ; Luan, Yujing
Phosphodiesterase type 5 inhibitors (PDE5is), primarily used for the treatment of erectile dysfunction, have been severely misused in recent years, posing a threat to public health and safety. This study developed a method that combines Surface-enhanced Raman spectroscopy (SERS) with machine learning algorithms to rapidly identify different PDE5is types. A total of 948 SERS spectra from 79 PDE5is were collected using gold nanoparticles (AuNPs) as the enhancement agent, and dimensionality reduction was performed through principal component analysis (PCA). Subsequently, six traditional machine learning models, partial least squares discriminant analysis (PLS-DA), orthogonal partial least squares discriminant analysis (OPLS-DA), support vector machines (SVM), k-nearest neighbors (KNN), random forest (RF), and multilayer perceptron (MLP) were applied for data classification and identification. Results showed that the MLP model achieved the highest classification accuracy of 99.65 %, with only 1.82 % of the samples misclassified from thiosildenafil to sildenafil analogues, significantly outperforming the other models. This method offers a rapid, cost-effective, and accurate alternative for the detection of PDE5is in health foods, with implications for improving regulatory oversight and public health safety.
100 项与 盐酸达泊西汀 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 |
|---|---|---|---|
| 早泄 | 奥地利 | 2008-12-17 | |
| 早泄 | 比利时 | 2008-12-17 | |
| 早泄 | 保加利亚 | 2008-12-17 | |
| 早泄 | 克罗地亚 | 2008-12-17 | |
| 早泄 | 塞浦路斯 | 2008-12-17 | |
| 早泄 | 捷克 | 2008-12-17 | |
| 早泄 | 爱沙尼亚 | 2008-12-17 | |
| 早泄 | 芬兰 | 2008-12-17 | |
| 早泄 | 法国 | 2008-12-17 | |
| 早泄 | 德国 | 2008-12-17 | |
| 早泄 | 希腊 | 2008-12-17 | |
| 早泄 | 匈牙利 | 2008-12-17 | |
| 早泄 | 爱尔兰 | 2008-12-17 | |
| 早泄 | 意大利 | 2008-12-17 | |
| 早泄 | 立陶宛 | 2008-12-17 | |
| 早泄 | 卢森堡 | 2008-12-17 | |
| 早泄 | 马耳他 | 2008-12-17 | |
| 早泄 | 荷兰 | 2008-12-17 | |
| 早泄 | 波兰 | 2008-12-17 | |
| 早泄 | 葡萄牙 | 2008-12-17 |
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 |
|---|---|---|---|---|
| 性功能障碍 | 临床3期 | 美国 | 2010-04-01 | |
| 性功能障碍 | 临床3期 | 阿根廷 | 2010-04-01 | |
| 性功能障碍 | 临床3期 | 澳大利亚 | 2010-04-01 | |
| 性功能障碍 | 临床3期 | 比利时 | 2010-04-01 | |
| 性功能障碍 | 临床3期 | 加拿大 | 2010-04-01 | |
| 性功能障碍 | 临床3期 | 法国 | 2010-04-01 | |
| 性功能障碍 | 临床3期 | 马来西亚 | 2010-04-01 | |
| 性功能障碍 | 临床3期 | 墨西哥 | 2010-04-01 | |
| 性功能障碍 | 临床3期 | 波兰 | 2010-04-01 | |
| 性功能障碍 | 临床3期 | 俄罗斯 | 2010-04-01 |
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临床结果
临床结果
适应症
分期
评价
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N/A | - | 鏇範獵膚鹽鏇淵鹽衊遞(醖糧鑰醖製鏇窪鹹築製) = 網衊繭網鑰夢齋構廠壓 淵顧鹹齋顧壓鏇獵願簾 (壓顧遞選廠願積醖鬱蓋, 23.0 ~ 400.0) | 积极 | 2024-05-01 | |||
OLNP-05 | 鏇範獵膚鹽鏇淵鹽衊遞(醖糧鑰醖製鏇窪鹹築製) = 鏇醖鑰觸夢願糧顧鑰醖 淵顧鹹齋顧壓鏇獵願簾 (壓顧遞選廠願積醖鬱蓋, 140.0 ~ 410.0) | ||||||
临床3期 | 495 | Placebo | 窪願築壓衊窪遞製襯餘(獵齋鹹構襯夢願製衊製) = Incidence of TEAEs was 20.0% and 29.6% in placebo- and dapoxetine-treated subjects, respectively (P = 0.0135) 繭鹽觸選膚艱範築夢醖 (遞蓋鹹鏇餘夢築窪襯鑰 ) 更多 | 积极 | 2013-09-01 | ||
临床3期 | 495 | Placebo (PDE5I + Placebo (Baseline)) | 製遞壓廠願糧選網憲製(蓋網廠憲憲鹽獵鬱簾廠) = 襯網艱鬱餘鏇簾觸簾醖 遞艱鏇築膚夢鬱簾簾壓 (選鹹獵壓繭窪製壓製糧, 0.53) | - | 2012-11-04 | ||
Placebo (PDE5I + Placebo (Week 12)) | 製遞壓廠願糧選網憲製(蓋網廠憲憲鹽獵鬱簾廠) = 積鹽製鑰構蓋壓齋繭廠 遞艱鏇築膚夢鬱簾簾壓 (選鹹獵壓繭窪製壓製糧, 3.54) |
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