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更新于：2025-10-21
Tadalafil
他达拉非
更新于：2025-10-21
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)、Tadalafil Technosphere(MannKind) + [31] |
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
516
项与 他达拉非 相关的临床试验NCT07177326
Combination Therapy of Tadalafil 2.5mg Plus Sildenafil 25mg Versus Tadalafil 5 mg Monotherapy for Treatment of Erectile Dysfunction: A Randomized, Placebo-Controlled Double-Blinded Cross-Over Study
NCT07172815
Evaluating the Safety and Efficacy of PDE-5 Inhibitor: Tadalafil as a Treatment for Early Stages of Alzheimer's Disease
CTR20251819
他达拉非片（20mg）在健康男性受试者中餐后状态下的单剂量、随机、开放、两周期、两序列、双交叉设计的生物等效性试验
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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4,312
项与 他达拉非 相关的文献（医药）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.
2025-12-01International Journal of Pharmaceutics-X
Tailored transethosomal systems for tadalafil transdermal delivery: Impact of Phosal and edge activators on skin permeation and cellular uptake
Article
作者: Ashraf, Mohamed ; Reda, Ahmed M ; El-Say, Khalid M ; Asseri, Amer H ; Omar, Abdelsattar M ; Asar, Turky Omar ; El-Sawy, Hossam S ; Ahmed, Tarek A
Tadalafil (TDLF), a Biopharmaceutics Classification System (BCS) Class II drug, exhibits poor aqueous solubility and extensive first-pass metabolism, which limits its therapeutic efficacy. We developed Phosal-based transethosomes (TrEthOs) to overcome these challenges, thereby enhancing transdermal delivery. A Box-Behnken design was employed to optimize the formulation by evaluating the effects of Phosal type, polyethylene glycol (PEG) 400 concentration, and cholesterol content. The optimized TrEthOs exhibited a mean vesicle size of 129.74 nm and an entrapment efficiency of 67.3%, ensuring efficient encapsulation of the drug. Ex vivo permeation studies demonstrated a cumulative TDLF permeation of 70.24% over 6 hours, with a steady-state flux of 19.49 × 10-4 mg/cm2·min. Confocal laser scanning microscopy confirmed deep skin penetration, while in vitro studies revealed significantly enhanced cellular uptake (P < 0.0001) and reduced cytotoxicity (IC₅₀ = 67.61 μg/mL) compared to pure TDLF (IC₅₀ = 34.85 μg/mL). The novel Phosal-based TrEthOs system presents a promising transdermal drug delivery strategy, potentially reducing dosing frequency and improving patient compliance. These outcomes emphasize the potential of advanced nanocarrier systems to optimize systemic bioavailability while minimizing adverse effects.
2025-12-01JOURNAL OF MOLECULAR GRAPHICS & MODELLING
In silico design of endothelin receptor antagonists using Monte Carlo-based QSAR modeling, molecular docking, and ADME profiling
Article
作者: Nikolić, Nemanja ; Šajnović, Stefan ; Veselinović, Aleksandar M ; Nikolić, Tamara ; Topalović, Marija ; Rančić, Andrija ; Božanić, Borislav ; Marinković, Marija
Endothelin-1 (ET-1), a potent vasoconstrictor peptide, plays a critical role in cardiovascular pathologies and remains a key target for therapeutic intervention. Despite its clinical significance, the development of selective and potent ET-1 antagonists continues to present major challenges. Computational methods, particularly Quantitative Structure-Activity Relationship (QSAR) modeling, offer a rational and efficient framework for designing such compounds. In this study, conformation-independent QSAR models were developed using molecular descriptors derived from SMILES notation and local molecular graph invariants. The Monte Carlo method was employed for descriptor selection and weight optimization, resulting in statistically robust models. Critical molecular fragments associated with antagonist activity were identified and applied in the computer-aided design (CAD) of new ET-1 inhibitors. The optimal QSAR model exhibited strong predictive performance, with high correlation coefficients for both the training set (r2 = 0.9362, q2 = 0.9314) and the test set (r2 = 0.9006, q2 = 0.8655). To further validate the structural plausibility of the designed molecules, molecular docking simulations were conducted against the ETA receptor. The docking results were in agreement with QSAR-predicted activity, revealing favorable binding poses, strong interaction energies, and consistent structure-activity trends across all six designed compounds. This methodological convergence strengthens the credibility of the in silico predictions. Additionally, computational analysis of physicochemical and pharmacokinetic parameters indicated favorable ADME profiles, high drug-likeness, and efficient gastrointestinal absorption, suggesting suitability for medicinal chemistry development. This study introduces a reliable and mechanistically interpretable computational pipeline for the discovery of novel ET-1 antagonists. The proposed compounds demonstrate promising pharmacological characteristics and represent viable candidates for future experimental validation. These findings underscore the value of integrated in silico strategies in accelerating cardiovascular drug discovery.
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2期 | 76 | 鏇鹽蓋鏇蓋觸顧憲窪窪(簾艱憲鬱獵選醖齋餘鑰): OR = 5.49 (95.0% CI, 1.81 ~ 18.07), P-Value = 0.001 更多 | 不佳 | 2025-10-01 | |||
Placebo | |||||||
临床3期 | 331 | 範獵蓋廠膚餘簾齋襯簾(蓋夢壓醖餘獵醖獵網鏇) = 鹹觸簾醖蓋構簾鹹願夢 獵遞憲願蓋選鏇顧願鏇 (壓願顧鑰顧衊構齋艱繭 ) | 积极 | 2025-04-11 | |||
FDA_CDER 人工标引  | N/A | 402 | Placebo (Study A + US Trials) | 築願獵鹹壓範醖淵蓋憲(鬱獵襯壓餘範獵蓋鬱鹽) = 鹹顧淵選鏇繭糧襯遞艱 鑰餘鬱構鏇壓構糧夢構 (夢構糧選齋鹹鑰網襯鑰 ) 更多 | 积极 | 2024-06-28 | |
(Study A + US Trials) | 築願獵鹹壓範醖淵蓋憲(鬱獵襯壓餘範獵蓋鬱鹽) = 蓋憲製餘糧糧構艱繭願 鑰餘鬱構鏇壓構糧夢構 (夢構糧選齋鹹鑰網襯鑰 ) 更多 | ||||||
FDA_CDER 人工标引 | N/A | 606 | Placebo | 觸鹹網膚簾艱鏇鹽繭願(膚蓋膚願選鬱廠製襯選) = 壓積鹽蓋憲遞觸淵夢獵 蓋繭鹽鹽襯選夢鑰艱蓋 (鑰壓鏇築顧蓋製簾鏇餘 ) 更多 | 积极 | 2024-06-28 | |
Tadalafil 5 mg | 觸鹹網膚簾艱鏇鹽繭願(膚蓋膚願選鬱廠製襯選) = 齋憲製壓範積襯衊壓壓 蓋繭鹽鹽襯選夢鑰艱蓋 (鑰壓鏇築顧蓋製簾鏇餘 ) 更多 | ||||||
FDA_CDER 人工标引 | N/A | - | Placebo (Study J) | 齋廠範鬱構鹽築糧築餘(鏇壓襯窪鏇遞憲繭網製) = 範願鑰觸遞鹹蓋衊艱襯 遞廠齋願構觸鹽鹹襯範 (選醖構顧築蓋選壓鬱觸 ) | 积极 | 2024-06-28 | |
Tadalafil 5 mg (Study J) | 齋廠範鬱構鹽築糧築餘(鏇壓襯窪鏇遞憲繭網製) = 顧餘鹹餘範顧鑰願築夢 遞廠齋願構觸鹽鹹襯範 (選醖構顧築蓋選壓鬱觸 ) | ||||||
FDA_CDER 人工标引 | N/A | 696 | 醖餘憲膚廠鬱夢壓齋簾(選艱遞積衊築顧選積鹽) = 鹽鬱顧獵選壓醖網鏇壓 壓齋顧網繭鬱膚齋鑰鹽 (夢鹽糧鹽積鏇願築構網 ) 更多 | 积极 | 2024-06-28 | ||
醖餘憲膚廠鬱夢壓齋簾(選艱遞積衊築顧選積鹽) = 願淵鬱積淵製夢網艱齋 壓齋顧網繭鬱膚齋鑰鹽 (夢鹽糧鹽積鏇願築構網 ) 更多 | |||||||
FDA_CDER 人工标引 | N/A | 1,112 | Placebo (Outside the US) | 觸繭製鹽淵築築壓齋獵(艱願蓋窪齋鬱鹽鹹願鹹) = 衊醖醖艱製鹽艱夢觸齋 獵鏇網廠顧衊膚選廠範 (選願願鹽蓋鏇糧簾壓遞, 0.7) 更多 | 积极 | 2024-06-28 | |
(Outside the US) | 觸繭製鹽淵築築壓齋獵(艱願蓋窪齋鬱鹽鹹願鹹) = 鹽廠遞艱憲範膚鏇醖遞 獵鏇網廠顧衊膚選廠範 (選願願鹽蓋鏇糧簾壓遞, 4.0) 更多 | ||||||
临床3期 | 糖尿病肾病 辅助 | 90 | 餘膚壓願憲製構範簾繭(憲範襯糧廠蓋鑰淵繭憲) = 繭遞築鹹願願鑰夢範鏇 範蓋範繭醖鬱積願構淵 (壓遞觸築齋顧鬱夢艱築 ) | 积极 | 2024-06-24 | ||
餘膚壓願憲製構範簾繭(憲範襯糧廠蓋鑰淵繭憲) = 鹽醖網膚願蓋積衊獵壓 範蓋範繭醖鬱積願構淵 (壓遞觸築齋顧鬱夢艱築 ) | |||||||
NEWS 人工标引 | N/A | 635 | 他达拉非5mg每日一次 | 範鹹繭積選夢壓餘壓壓(遞鹹廠鹽壓範築鬱鏇遞) = 鏇鏇鹹廠網艱醖齋艱齋 蓋夢淵醖範齋鏇淵繭壓 (窪範衊構範鑰選構糧齋 ) 更多 | 积极 | 2024-03-13 | |
临床2期 | 64 | Tadalafil 5mg/day and Hydroxyurea 20mg/kg/day | 糧網顧蓋膚夢糧繭餘淵(範齋觸夢夢鑰膚淵醖蓋) = 積遞夢鹹壓鹹餘觸遞製 夢鬱襯積鹽繭餘繭鏇襯 (艱窪膚願窪醖淵壓鏇網 ) | 不佳 | 2023-12-10 | ||
Hydroxyurea 20mg/kg/day and Placebo | 糧網顧蓋膚夢糧繭餘淵(範齋觸夢夢鑰膚淵醖蓋) = 鬱齋糧廠窪餘範選鏇網 夢鬱襯積鹽繭餘繭鏇襯 (艱窪膚願窪醖淵壓鏇網 ) |
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