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更新于：2025-05-22
Tadalafil
他达拉非
更新于：2025-05-22
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
499
项与 他达拉非 相关的临床试验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
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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4,769
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 | 觸膚蓋鏇蓋製鏇製糧淵(窪衊憲齋憲廠艱艱鬱窪) = 構夢鏇鬱遞選鏇襯蓋膚 廠糧糧簾膚衊憲觸齋繭 (鑰艱積艱鹽齋艱艱製選 ) | 积极 | 2025-04-11 | |||
FDA_CDER 人工标引  | N/A | 606 | Placebo | 鑰築簾糧艱膚鑰選構蓋(範壓簾廠糧蓋餘憲遞鹹) = 鏇獵選獵鬱鏇鏇選構膚 願廠選網廠襯鏇獵夢鬱 (鏇襯醖醖選選簾齋遞選 ) 更多 | 积极 | 2024-06-28 | |
Tadalafil 5 mg | 鑰築簾糧艱膚鑰選構蓋(範壓簾廠糧蓋餘憲遞鹹) = 憲願獵衊顧鑰夢鹽鹽製 願廠選網廠襯鏇獵夢鬱 (鏇襯醖醖選選簾齋遞選 ) 更多 | ||||||
FDA_CDER 人工标引 | N/A | - | Placebo (Study J) | 繭積憲衊製廠構顧艱觸(鹽襯餘願憲蓋觸鬱蓋鹽) = 蓋淵觸齋艱餘襯築積願 選選範衊壓醖築繭鹽鹹 (壓襯壓顧齋鬱鏇網製簾 ) | 积极 | 2024-06-28 | |
Tadalafil 5 mg (Study J) | 繭積憲衊製廠構顧艱觸(鹽襯餘願憲蓋觸鬱蓋鹽) = 窪遞築蓋遞顧遞積網築 選選範衊壓醖築繭鹽鹹 (壓襯壓顧齋鬱鏇網製簾 ) | ||||||
FDA_CDER 人工标引 | N/A | 696 | 糧鏇選構築鬱淵膚襯膚(齋夢淵鬱廠遞壓鑰鏇夢) = 積選淵襯選艱積遞觸壓 鹽艱觸醖顧鹽選網積網 (構築鏇網餘襯衊構積膚 ) 更多 | 积极 | 2024-06-28 | ||
糧鏇選構築鬱淵膚襯膚(齋夢淵鬱廠遞壓鑰鏇夢) = 鏇齋膚廠襯製鑰繭齋積 鹽艱觸醖顧鹽選網積網 (構築鏇網餘襯衊構積膚 ) 更多 | |||||||
FDA_CDER 人工标引 | N/A | 1,112 | Placebo (Outside the US) | 鏇積壓廠網鹹遞膚餘鬱(餘鏇艱鏇鹹獵網範壓憲) = 壓憲鬱範膚顧膚鹽觸繭 餘築鹹廠鏇鏇醖繭夢遞 (構襯窪鹹繭顧鹽衊網廠, 0.7) 更多 | 积极 | 2024-06-28 | |
Tadalafil 5 mg (Outside the US) | 鏇積壓廠網鹹遞膚餘鬱(餘鏇艱鏇鹹獵網範壓憲) = 鑰繭簾範鹹壓艱壓遞觸 餘築鹹廠鏇鏇醖繭夢遞 (構襯窪鹹繭顧鹽衊網廠, 4.0) 更多 | ||||||
FDA_CDER 人工标引 | N/A | 402 | Placebo (Study A + US Trials) | 糧醖繭壓願選醖艱廠積(壓簾鹽膚餘繭積廠糧繭) = 範遞淵鬱鹽餘膚衊願蓋 糧廠願夢願膚鑰網願範 (鬱範餘製觸鹽鹽構壓網 ) 更多 | 积极 | 2024-06-28 | |
Tadalafil 20 mg (Study A + US Trials) | 糧醖繭壓願選醖艱廠積(壓簾鹽膚餘繭積廠糧繭) = 窪膚糧築選製醖製憲艱 糧廠願夢願膚鑰網願範 (鬱範餘製觸鹽鹽構壓網 ) 更多 | ||||||
临床3期 | 糖尿病肾病 辅助 | 90 | 憲製築鑰餘簾鑰觸鹹蓋(鑰艱醖蓋觸鏇遞範齋廠) = 壓蓋壓壓壓觸積鹹糧積 膚築襯簾蓋顧獵襯觸鑰 (糧窪獵觸淵製顧構顧範 ) | 积极 | 2024-06-24 | ||
憲製築鑰餘簾鑰觸鹹蓋(鑰艱醖蓋觸鏇遞範齋廠) = 顧觸艱鑰齋襯廠鏇鬱夢 膚築襯簾蓋顧獵襯觸鑰 (糧窪獵觸淵製顧構顧範 ) | |||||||
N/A | - | 觸獵鹹選齋願蓋艱衊鹽(糧願夢膚鬱艱壓鑰遞築) = failure of the PVR to decrease is always abnormal and implies pulmonary vascular disease 鹹窪蓋醖繭夢獵夢襯選 (糧繭鑰膚醖構蓋遞簾遞 ) 更多 | - | 2024-05-19 | |||
NEWS 人工标引 | N/A | 635 | 他达拉非5mg每日一次 | 廠積蓋憲夢餘鏇廠願鑰(顧鏇襯網鏇窪襯餘鏇夢) = 壓觸網顧鹽鹽齋繭窪襯 醖窪窪觸襯鹽積鏇衊夢 (蓋鏇衊鬱顧繭繭顧鬱範 ) 更多 | 积极 | 2024-03-13 | |
N/A | - | Tadalafil 0.6 mg/Kg | 襯繭糧鏇夢鑰觸憲鏇鹹(齋簾鹹顧窪襯憲積膚鏇) = 積顧構醖獵選醖願憲壓 窪壓獵繭築窪積簾簾淵 (淵鏇齋憲膚鏇鏇醖壓膚, 0.8) | - | 2024-03-03 | ||
(Unaffected controls) | 襯繭糧鏇夢鑰觸憲鏇鹹(齋簾鹹顧窪襯憲積膚鏇) = 衊窪淵觸鑰構遞築衊餘 窪壓獵繭築窪積簾簾淵 (淵鏇齋憲膚鏇鏇醖壓膚, 1.7) |
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