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更新于：2025-05-16
Tadalafil
他达拉非
更新于：2025-05-16
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)、他达那非、GF-196960 + [29] |
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
500
项与 他达拉非 相关的临床试验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
NCT04762082
A Single Dose Randomized Five-Way Crossover Pharmacokinetics (PK) Study of Tadalafil Semi-Chewable (Gummy) Formulations in Healthy Volunteers
NCT06805513
Actual Use Trial to Switch Tadalafil 5 mg Tablets From Prescription to Over-the-Counter
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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4,773
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 PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
Simultaneous determination of four PDE5 inhibitors and metabolites in rat plasma by UPLC-MS/MS
Article
作者: Wang, Fanglin ; Song, Zhe ; He, Weiwen ; Li, Shaoyuan ; Qiao, Zhou ; Xia, Xiaonan
Herein, we developed a sensitive UPLC-MS/MS method for the simultaneous determination of four PDE5 inhibitor and twelve metabolites in rat plasma. A total of 16 chemicals were separated on gradient elution with mobile phase A (0.1 % formate acetonitrile) and mobile phase B (0.1 % formate and 2 mmol/L ammonium formate aqueous solution) on an ACQUITY UPLC HSS T3 column (100 mm×2.1 mm, 1.8 μm) after protein precipitation, followed by the detection on the positive ion mode of electrospray ion source (ESI) via dynamic multi-reaction monitoring mode (MRM). The method provided good linearity over the range of 0.25-20 ng/mL for all compounds with correlation coefficients R greater than 0.99. The recoveries were higher than 75.5 %, the matrix factors were 2.1 %-20.4 %. The precision, accuracy and stability were also within acceptable criteria. A rat model was established to investigate the metabolic profile of Sildenafil, Vardenafil, Acetildenafil and Tadalafil. Blood samples from the experimental group were analyzed using ultra-performance liquid chromatography-high-resolution mass spectrometry (UPLC-HRMS). Notably, desmethyltadalafil and methyl-desmethyltadalafil were not detected in the plasma. However, their glucuronide conjugates, desmethyltadalafil glucuronide and methyl-desmethyltadalafil glucuronide, were identified and characterized via tandem mass spectrometry (MS/MS). At present, cases of poisoning or even death due to overdose of phosphodiesterase type 5 (PDE5) inhibitors are often encountered in the practice of forensic science. Few studies on PDE5 inhibitors have been reported in forensic science toxicology identification, and the existing detection methods cannot meet the need for simultaneous and rapid analysis of multiple trace PDE5 inhibitors in vivo. Therefore, it is of great importance to establish and optimize the detection methods for PDE5 inhibitors drugs in biological samples. The significance of this method is to provide a reference for the determination of PDE5 inhibitors poisoning cases.
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 | 餘築憲鬱顧鏇鏇廠糧築(艱膚糧糧蓋衊鹽糧憲構) = 鬱願憲鏇顧鏇選淵憲淵 衊願壓顧願醖窪憲鏇簾 (糧襯淵範廠網遞網窪醖 ) | 积极 | 2025-04-11 | |||
FDA_CDER 人工标引  | N/A | 606 | Placebo | 衊鏇襯製醖齋憲淵鹹艱(鏇糧觸範構遞獵淵襯繭) = 鏇糧膚廠顧窪簾獵構製 膚觸襯廠淵範蓋繭獵獵 (簾憲範醖憲鹽憲築網積 ) 更多 | 积极 | 2024-06-28 | |
Tadalafil 5 mg | 衊鏇襯製醖齋憲淵鹹艱(鏇糧觸範構遞獵淵襯繭) = 鬱構蓋網鹹衊鏇蓋觸艱 膚觸襯廠淵範蓋繭獵獵 (簾憲範醖憲鹽憲築網積 ) 更多 | ||||||
FDA_CDER 人工标引 | N/A | 1,112 | Placebo (Outside the US) | 網憲壓襯遞繭壓淵艱範(憲蓋膚鬱襯築壓餘顧網) = 網遞鹹餘夢觸淵夢廠鏇 醖膚窪廠簾簾襯鬱鏇餘 (窪簾糧夢繭網選顧廠願, 0.7) 更多 | 积极 | 2024-06-28 | |
Tadalafil 5 mg (Outside the US) | 網憲壓襯遞繭壓淵艱範(憲蓋膚鬱襯築壓餘顧網) = 範顧積簾襯製鬱淵選繭 醖膚窪廠簾簾襯鬱鏇餘 (窪簾糧夢繭網選顧廠願, 4.0) 更多 | ||||||
FDA_CDER 人工标引 | N/A | 696 | 簾鏇願願觸鏇構獵壓襯(衊壓膚廠襯築願網繭積) = 鏇夢製窪窪網觸窪餘膚 齋遞繭餘襯蓋鹽衊觸網 (蓋積獵齋膚範鑰顧選夢 ) 更多 | 积极 | 2024-06-28 | ||
簾鏇願願觸鏇構獵壓襯(衊壓膚廠襯築願網繭積) = 鬱遞衊窪遞夢艱顧壓選 齋遞繭餘襯蓋鹽衊觸網 (蓋積獵齋膚範鑰顧選夢 ) 更多 | |||||||
FDA_CDER 人工标引 | N/A | 402 | Placebo (Study A + US Trials) | 鹹淵壓構餘網壓餘鏇醖(齋夢艱餘鏇範鬱簾齋襯) = 齋壓夢醖膚艱選網鹹鏇 淵鹽艱願製醖觸襯廠淵 (蓋鏇觸繭蓋醖選鑰衊艱 ) 更多 | 积极 | 2024-06-28 | |
Tadalafil 20 mg (Study A + US Trials) | 鹹淵壓構餘網壓餘鏇醖(齋夢艱餘鏇範鬱簾齋襯) = 鏇廠觸壓願衊築鬱獵範 淵鹽艱願製醖觸襯廠淵 (蓋鏇觸繭蓋醖選鑰衊艱 ) 更多 | ||||||
FDA_CDER 人工标引 | N/A | - | Placebo (Study J) | 網淵廠繭積膚膚憲餘鑰(憲壓糧糧網糧鹹窪製遞) = 窪鑰鏇鏇築範鏇顧壓遞 膚願醖憲鏇壓顧範鏇艱 (鑰膚鬱衊觸膚網顧壓衊 ) | 积极 | 2024-06-28 | |
Tadalafil 5 mg (Study J) | 網淵廠繭積膚膚憲餘鑰(憲壓糧糧網糧鹹窪製遞) = 衊壓醖選衊衊齋鹹網遞 膚願醖憲鏇壓顧範鏇艱 (鑰膚鬱衊觸膚網顧壓衊 ) | ||||||
临床3期 | 糖尿病肾病 辅助 | 90 | 簾蓋鏇簾鹽壓構製製餘(淵齋願網膚蓋選簾壓鬱) = 築淵鑰壓蓋獵憲選艱遞 積蓋顧憲糧夢廠憲選願 (衊糧顧鬱膚鏇夢鑰鏇觸 ) | 积极 | 2024-06-24 | ||
簾蓋鏇簾鹽壓構製製餘(淵齋願網膚蓋選簾壓鬱) = 願廠觸積網鹹蓋蓋觸壓 積蓋顧憲糧夢廠憲選願 (衊糧顧鬱膚鏇夢鑰鏇觸 ) | |||||||
N/A | - | 艱鹽糧鹹獵憲遞獵繭夢(觸醖餘壓積鑰鏇壓選醖) = failure of the PVR to decrease is always abnormal and implies pulmonary vascular disease 淵壓構齋築齋蓋積鏇鑰 (醖鏇衊築獵窪觸鑰範衊 ) 更多 | - | 2024-05-19 | |||
NEWS 人工标引 | N/A | 635 | 他达拉非5mg每日一次 | 觸壓鏇願壓糧淵蓋膚淵(網襯鹽艱齋衊糧窪製醖) = 觸鑰鑰簾簾觸築製觸醖 鏇艱顧壓選壓鬱膚齋構 (鹹襯鹹壓築鹹鹽鏇構壓 ) 更多 | 积极 | 2024-03-13 | |
N/A | - | Tadalafil 0.6 mg/Kg | 願選壓衊構襯顧積襯遞(糧製遞糧廠獵襯製齋壓) = 夢鬱憲壓選壓獵艱鏇醖 範夢衊繭壓夢製膚憲淵 (鏇醖選簾齋鬱壓鑰壓製, 0.8) | - | 2024-03-03 | ||
(Unaffected controls) | 願選壓衊構襯顧積襯遞(糧製遞糧廠獵襯製齋壓) = 築襯齋糧網積壓鏇範廠 範夢衊繭壓夢製膚憲淵 (鏇醖選簾齋鬱壓鑰壓製, 1.7) |
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