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更新于：2025-06-23
Tadalafil
他达拉非
更新于：2025-06-23
概要
基本信息
简介他达拉非（Tadalafil）是一种磷酸二酯酶5型（PDE5）抑制剂药物，商标名为“Cialis”，与西地那非（Viagra）和伐地那非（Levitra）同属一类药物。他达拉非于2003年11月21日首次获得FDA批准用于治疗勃起功能障碍（ED）。它由ICOS Corporation制药公司开发，由Eli Lilly and Company销售。除了获得勃起功能障碍的批准外，他达拉非还获得了FDA批准用于治疗良性前列腺增生症（BPH）和肺动脉高压（PAH）。 |
药物类型 小分子化药 |
别名 Tadalafil (JAN/USP/INN)、Tadalafil Film Coated Tablets(Akums)、他达那非 + [30] |
靶点 |
作用方式 抑制剂 |
作用机制 PDE5A抑制剂(磷酸二酯酶-5A抑制剂) |
最高研发阶段批准上市 |
首次获批日期 澳大利亚 (2002-10-23), |
最高研发阶段(中国)批准上市 |
特殊审评孤儿药 (美国)、优先审评 (中国) |
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结构/序列
分子式C22H19N3O4 |
InChIKeyWOXKDUGGOYFFRN-IIBYNOLFSA-N |
CAS号171596-29-5 |
关联
503
项与 他达拉非 相关的临床试验CTR20251410
他达拉非片在中国健康受试者中单剂量、两制剂、两周期、两序列、随机、开放、自身交叉的空腹和餐后状态下生物等效性试验
NCT04762082
A Single Dose Randomized Five-Way Crossover Pharmacokinetics (PK) Study of Tadalafil Semi-Chewable (Gummy) Formulations in Healthy Volunteers
NCT06968962
A Multicenter, Randomized, Controlled, Double-blind, and Non-inferiority Clinical Trial to Compare the Efficacy of Sequential to Initial Combination Therapy in Patients With Pulmonary Arterial Hypertension
100 项与 他达拉非 相关的临床结果
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100 项与 他达拉非 相关的转化医学
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100 项与 他达拉非 相关的专利（医药）
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4,776
项与 他达拉非 相关的文献（医药）2025-12-31RENAL FAILURE
The role of endothelin receptor antagonists in kidney disease
Review
作者: Lin, Haishan ; Zheng, Lingqian ; Liang, Yuyang ; Zhou, Tianbiao ; Ma, Xiaoting ; Chen, Wenmin
Kidney diseases are among the most prevalent conditions worldwide, impacting over 850 million individuals. They are categorized into acute kidney injury and chronic kidney disease. Current preclinical and clinical trials have demonstrated that endothelin (ET) is linked to the onset and progression of kidney disease. In kidney diseases, pathological conditions such as hyperglycemia, acidosis, insulin resistance, and elevated angiotensin II levels lead to an increase in ET. This elevation activates endothelin receptor type A, resulting in harmful effects like proteinuria and a reduced glomerular filtration rate (GFR). Therefore, to slow the progression of kidney disease, endothelin receptor antagonists (ERAs) have been proposed as promising new therapies. Numerous studies have demonstrated the efficacy of ERAs in significantly reducing proteinuria and improving GFR, thereby slowing the progression of kidney diseases. This review discusses the mechanisms of action of ERAs in treating kidney disease, their efficacy and safety in preclinical and clinical studies, and explores future prospects for ERAs.
2025-12-11Aging Male
Predictive value of systemic inflammatory response index in patients with erectile dysfunction on tadalafil unresponsive patients
Article
作者: Sobay, Resul
BACKGROUND:
Erectile dysfunction (ED) is a common disorder that significantly impacts quality of life, and phosphodiesterase type 5 inhibitors (PDE5is) such as tadalafil are one of the primary treatments. However, some patients remain unresponsive, necessitating further investigation.
OBJECTIVE:
To investigate the association between systemic inflammatory response index (SIRI) and tadalafil unresponsiveness in erectile dysfunction patients.
METHODS:
A total of 106 male patients who applied to the Andrology outpatient clinic with ED complaints between January and June 2024 were included in the study. Patients were started on daily tadalafil 5 mg therapy, and response was assessed after one month using the International Index of Erectile Function Erectile Function domain (IIEF-EF). SIRI values, calculated using neutrophil, monocyte, and lymphocyte counts, were compared between tadalafil-responsive and unresponsive groups.
RESULTS:
Tadalafil unresponsiveness was observed in 48.1% of patients. Non-responders had significantly higher mean age(57.44 ± 12.52 vs. 47.22 ± 11.49, p < 0.001), BMI(27.22 ± 3.17 vs. 25.85 ± 2.92, p = 0.023), and SIRI values(1.33 ± 0.82 vs. 1.02 ± 0.40, p = 0.016) compared to responders. Multivariate analysis identified age(OR = 1,641, p = 0.001) and SIRI(OR = 2.420, p = 0.014) as independent predictors of tadalafil failure. ROC curve analysis revealed a SIRI cutoff of 1.03 (AUC = 0.617) with 69.1% sensitivity and 61.2% specificity.
CONCLUSION:
Findings suggest that systemic inflammation plays a key role in ED pathophysiology and may impair PDE5i efficacy.
2025-09-01JOURNAL OF MOLECULAR STRUCTURE
Synthesis, spectroscopic, theoretical and computational investigations of novel indole fused tris-heterocyclic compounds: as high portentous antimicrobial agents
作者: Joshi, Shrinivas Dattatraya ; Anjanayya, Govinda ; Mathada, Basavarajaiah Suliphuldevarada ; Adole, Vishnu Ashok ; Bashetti, Nivedita Rajashekhar ; Mangalawede, Shailendra Shivand ; Hiremath, Murigendra Basayya ; Gani, Ramesh Sabu ; Bonagiri, Rajesh
In the human microbiome, bacteria seem to be far more prevalent than viruses, fungi, and protozoa, and bacterial illnesses are also common.As a result, microbial resistance poses serious problems for public health.Since growing bacterial and fungal resistance to antimicrobial medicines poses a serious danger to global public health, the development of novel antimicrobial medications is both urgently needed and crucial.Through spectroscopic examination, new indole fused tris heterocyclic compounds including triazole, thiazole,pyrrole and oxadiazole were clarified.We evaluated the compounds′ in vitro antibacterial and antifungal efficacy using the agar diffusion technique.After checking the pharmacokinetic features and ADME in silico predictions, the made compounds were put through mol. docking studies and DFT calculationsThe compounds such as 10 a,11,13,14,and 17 displayed a significant antimicrobial activity against selected microbial pathogens.The docking study revealed that all the compounds have showed very good docking score against Escherichia coli.and compound 10b and 14 showed reasonable binding modes in the active site of the enzyme.In silico predictions of ADME and pharmacokinetic parameters indicated that few compounds appear to possess high pharmacol. activity, they demonstarte good absorption, permiability and oral bioavailability.The antibacterial and antifungal activity of indole fused tris heterocyclic compounds, including 10a, 13, 14, and 17, demonstrated significant antimicrobial efficacy.Docking studies, ADME, and pharmacokinetic parameters further support the results.The results indicate that compounds 10a, 13, 14, and 17 represent a promising avenue for the development of new antimicrobial drugs.
100 项与 他达拉非 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 |
|---|---|---|---|
| 前列腺增生症 | 美国 | 2011-10-06 | |
| 家族性肺动脉高压 | 欧盟 | 2008-10-01 | |
| 家族性肺动脉高压 | 冰岛 | 2008-10-01 | |
| 家族性肺动脉高压 | 列支敦士登 | 2008-10-01 | |
| 家族性肺动脉高压 | 挪威 | 2008-10-01 | |
| 肺动脉高压 | 欧盟 | 2008-10-01 | |
| 肺动脉高压 | 冰岛 | 2008-10-01 | |
| 肺动脉高压 | 列支敦士登 | 2008-10-01 | |
| 肺动脉高压 | 挪威 | 2008-10-01 | |
| 勃起功能障碍 | 澳大利亚 | 2002-10-23 |
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 |
|---|---|---|---|---|
| 杜氏肌营养不良症 | 临床3期 | 美国 | 2013-09-01 | |
| 杜氏肌营养不良症 | 临床3期 | 日本 | 2013-09-01 | |
| 杜氏肌营养不良症 | 临床3期 | 阿根廷 | 2013-09-01 | |
| 杜氏肌营养不良症 | 临床3期 | 比利时 | 2013-09-01 | |
| 杜氏肌营养不良症 | 临床3期 | 加拿大 | 2013-09-01 | |
| 杜氏肌营养不良症 | 临床3期 | 法国 | 2013-09-01 | |
| 杜氏肌营养不良症 | 临床3期 | 德国 | 2013-09-01 | |
| 杜氏肌营养不良症 | 临床3期 | 意大利 | 2013-09-01 | |
| 杜氏肌营养不良症 | 临床3期 | 荷兰 | 2013-09-01 | |
| 杜氏肌营养不良症 | 临床3期 | 波多黎各 | 2013-09-01 |
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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3期 | 331 | 憲壓憲鏇蓋醖製選廠網(鹹鹹鏇鬱顧淵網構淵廠) = 積範膚淵壓願襯淵鏇衊 衊願壓鬱築繭廠範醖夢 (製網鹹積範膚遞夢餘膚 ) | 积极 | 2025-04-11 | |||
FDA_CDER 人工标引  | N/A | 606 | Placebo | 鑰積蓋襯襯鑰齋獵築願(範獵網製壓餘鑰鹹鏇憲) = 憲觸願壓鹽築醖築觸選 積壓蓋襯鑰淵願網願築 (簾膚壓鹹繭範築鹽艱獵 ) 更多 | 积极 | 2024-06-28 | |
Tadalafil 5 mg | 鑰積蓋襯襯鑰齋獵築願(範獵網製壓餘鑰鹹鏇憲) = 艱鑰糧製鹹淵築鬱願願 積壓蓋襯鑰淵願網願築 (簾膚壓鹹繭範築鹽艱獵 ) 更多 | ||||||
FDA_CDER 人工标引 | N/A | - | Placebo (Study J) | 繭鬱觸餘鏇蓋鏇窪廠壓(鏇鏇簾膚襯願膚範鏇齋) = 鬱廠膚積窪淵窪簾窪壓 繭醖餘廠衊選選廠觸構 (製憲鏇膚鏇獵築觸鬱築 ) | 积极 | 2024-06-28 | |
Tadalafil 5 mg (Study J) | 繭鬱觸餘鏇蓋鏇窪廠壓(鏇鏇簾膚襯願膚範鏇齋) = 範鑰遞獵壓繭鹹餘簾願 繭醖餘廠衊選選廠觸構 (製憲鏇膚鏇獵築觸鬱築 ) | ||||||
FDA_CDER 人工标引 | N/A | 1,112 | Placebo (Outside the US) | 壓選膚鹽鏇廠膚構醖糧(鬱壓夢鹹糧繭憲膚觸觸) = 襯淵壓糧餘範憲窪顧衊 鬱鏇憲窪膚願夢糧繭鬱 (糧淵廠鹽構淵齋鏇艱網, 0.7) 更多 | 积极 | 2024-06-28 | |
Tadalafil 5 mg (Outside the US) | 壓選膚鹽鏇廠膚構醖糧(鬱壓夢鹹糧繭憲膚觸觸) = 齋簾願醖鑰膚夢廠鑰蓋 鬱鏇憲窪膚願夢糧繭鬱 (糧淵廠鹽構淵齋鏇艱網, 4.0) 更多 | ||||||
FDA_CDER 人工标引 | N/A | 696 | 膚窪醖繭醖遞鑰構鏇鹽(鏇鹽選獵憲範蓋選窪鑰) = 鑰餘淵簾鹹艱顧製醖窪 膚願鏇艱製獵窪鬱鬱願 (鏇鬱餘憲醖鹹壓網鏇艱 ) 更多 | 积极 | 2024-06-28 | ||
膚窪醖繭醖遞鑰構鏇鹽(鏇鹽選獵憲範蓋選窪鑰) = 膚獵窪積糧夢網襯願襯 膚願鏇艱製獵窪鬱鬱願 (鏇鬱餘憲醖鹹壓網鏇艱 ) 更多 | |||||||
FDA_CDER 人工标引 | N/A | 402 | Placebo (Study A + US Trials) | 構積壓鏇網製獵構襯簾(觸鏇範夢範鏇遞遞膚獵) = 簾鬱範範顧簾願顧網鑰 遞顧壓範鏇選蓋醖構顧 (糧衊夢構膚餘鑰觸鏇製 ) 更多 | 积极 | 2024-06-28 | |
Tadalafil 20 mg (Study A + US Trials) | 構積壓鏇網製獵構襯簾(觸鏇範夢範鏇遞遞膚獵) = 獵鹽鏇獵築鹽網齋簾顧 遞顧壓範鏇選蓋醖構顧 (糧衊夢構膚餘鑰觸鏇製 ) 更多 | ||||||
临床3期 | 糖尿病肾病 辅助 | 90 | 願鑰願顧獵衊鏇艱遞醖(憲齋獵鹽夢簾遞餘遞鏇) = 壓構築蓋積範顧廠鹹衊 鹽獵膚廠簾餘鹽夢遞襯 (鹹範獵夢淵窪艱廠鑰窪 ) | 积极 | 2024-06-24 | ||
願鑰願顧獵衊鏇艱遞醖(憲齋獵鹽夢簾遞餘遞鏇) = 醖衊願鬱齋鹹獵獵製鬱 鹽獵膚廠簾餘鹽夢遞襯 (鹹範獵夢淵窪艱廠鑰窪 ) | |||||||
N/A | - | 遞鏇艱艱醖顧壓餘網壓(鬱選積蓋鹽範壓鹽壓簾) = failure of the PVR to decrease is always abnormal and implies pulmonary vascular disease 醖構簾淵齋觸齋蓋鏇遞 (簾鏇餘襯餘蓋衊餘壓蓋 ) 更多 | - | 2024-05-19 | |||
NEWS 人工标引 | N/A | 635 | 他达拉非5mg每日一次 | 積餘繭窪遞鬱繭觸鏇憲(鏇簾餘鹹衊糧鏇艱鏇繭) = 襯齋鏇膚願齋窪簾遞鹽 蓋選顧壓膚襯淵網繭構 (範範齋齋壓醖夢願艱簾 ) 更多 | 积极 | 2024-03-13 | |
N/A | - | Tadalafil 0.6 mg/Kg | 遞蓋醖餘顧觸夢廠衊窪(襯艱築襯鏇製觸醖鹽範) = 繭廠網衊襯積鹹淵觸選 鹹網觸襯鏇糧膚獵餘獵 (憲膚觸觸網壓襯齋鬱鬱, 0.8) | - | 2024-03-03 | ||
(Unaffected controls) | 遞蓋醖餘顧觸夢廠衊窪(襯艱築襯鏇製觸醖鹽範) = 鹽襯醖顧廠鑰願積憲襯 鹹網觸襯鏇糧膚獵餘獵 (憲膚觸觸網壓襯齋鬱鬱, 1.7) |
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