更新于：2024-12-24
Tadalafil
他达拉非
更新于：2024-12-24
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 (6R,12aR)-2,3,6,7,12,12a-Hexahydro-2-methyl-6-(3,4-(methylenedioxy)phenyl) pyrazino(1',2':1,6)pyrido(3,4-b)indole-1,4-dione、(6R-trans)-6-(1,3-Benzodioxol-5-yl)-2,3,6,7,12,12a-hexahydro-2-methyl-pyrazino(1',2':1,6)pyrido(3,4-b)indole-1,4-dione、Tadalafil (JAN/USP/INN) + [31] |
靶点 |
作用机制 PDE5A抑制剂(磷酸二酯酶-5A抑制剂) |
原研机构 |
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 |
特殊审评优先审评 (中国)、孤儿药 (美国) |
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结构
分子式C22H19N3O4 |
InChIKeyWOXKDUGGOYFFRN-IIBYNOLFSA-N |
CAS号171596-29-5 |
关联
496
项与 他达拉非 相关的临床试验A Single Dose Randomized Five-Way Crossover Pharmacokinetics (PK) Study of Tadalafil Semi-Chewable (Gummy) Formulations in Healthy Volunteers
A prospective, single-center, randomized controlled clinical study on the treatment of type 2 diabetes mellitus erectile dysfunction (ED) with Qingzhi Capsules and Tadalafil, either in combination or as monotherapy.
Comparative effectiveness of oral Sildenafil, oral Tadalafil, and intracavernosal papaverine for penile doppler ultrasonography in erectile dysfunction patients. - NIL
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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2,577
项与 他达拉非 相关的文献（医药）2024-12-02MOLECULAR PHARMACEUTICS
Three Strikingly Different Crystal Habits of Tadalafil: Design, Characterization, Pharmaceutical Performance, and Computational Studies
Article
作者: Srivastava, Saurabh ; Vishwakarma, Arti ; Jahnavi, Avvaru Subha ; Dikundwar, Amol G. ; Bhale, Nagesh A. ; Shah, Saurabh ; Thomas, Sajesh P. ; Thakur, Tejender S.
The present study aims at improving the physicochemical properties of a widely used drug Tadalafil through crystal habit modification, without changing the polymorphic form. Three distinct types of crystal habits, namely, needle, plate, and block, were obtained under controlled crystallization protocols with optimized solvent compositions. Complete characterization of these three crystal habits was carried out using powder X-ray diffraction, differential scanning calorimetry, thermogravimetric analysis, and Fourier transform infrared spectroscopy. Morphological features were studied by optical and scanning electron microscopy. Evaluation of the pharmaceutical performance of different crystal habits reveals significant improvement in compressibility and flow properties for the block-shaped crystals in comparison to the needle- and plate-shaped crystals. Also, a more linear tablet compression behavior was noted for the plate and block morphologies of the API compared to their needle counterpart. In vitro dissolution studies showed distinct release profiles for the same API form with different crystal habits, i.e., needle > plate > block. Insights into crystal growth mechanism and the role of solvents in affording the observed crystal habits are presented based on molecular dynamics simulations of intermolecular interactions with crystal facets, in conjunction with the experimental crystal face indexing of the single crystals of different habits. These observations were further supported by interaction topology analysis and the electrostatic features on different crystal facets.
2024-12-01CELLULAR AND MOLECULAR LIFE SCIENCES
Pharmacologically increasing cGMP improves proteostasis and reduces neuropathy in mouse models of CMT1
Article
作者: Moore, Seth M. ; VerPlank, Jordan J.S. ; Milne, G. Todd ; Marziali, Leandro N ; Feltri, Maria Laura ; VerPlank, Jordan J S ; Stevens, Mckayla ; Buys, Emmanuel S ; Buys, Emmanuel S. ; Milne, G Todd ; Marziali, Leandro N. ; Gawron, Joseph ; Moore, Seth M
Abstract:
Increasing cyclic GMP activates 26S proteasomes via phosphorylation by Protein Kinase G and stimulates the intracellular degradation of misfolded proteins. Therefore, agents that raise cGMP may be useful therapeutics against neurodegenerative diseases and other diseases in which protein degradation is reduced and misfolded proteins accumulate, including Charcot Marie Tooth 1A and 1B peripheral neuropathies, for which there are no treatments. Here we increased cGMP in the S63del mouse model of CMT1B by treating for three weeks with either the phosphodiesterase 5 inhibitor tadalafil, or the brain-penetrant soluble guanylyl cyclase stimulator CYR119. Both molecules activated proteasomes in the affected peripheral nerves, reduced polyubiquitinated proteins, and improved myelin thickness and nerve conduction. CYR119 increased cGMP more than tadalafil in the peripheral nerves of S63del mice and elicited greater biochemical and functional improvements. To determine whether raising cGMP could be beneficial in other neuropathies, we first showed that polyubiquitinated proteins and the disease-causing protein accumulate in the sciatic nerves of the C3 mouse model of CMT1A. Treatment of these mice with CYR119 reduced the levels of polyubiquitinated proteins and the disease-causing protein, presumably by increasing their degradation, and improved myelination, nerve conduction, and motor coordination. Thus, pharmacological agents that increase cGMP are promising treatments for CMT1 neuropathies and may be useful against other proteotoxic and neurodegenerative diseases.
2024-12-01JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL AND LIFE SCIENCES
Methylated magnetic covalent organic framework for sample preparation and LC-MS/MS detection of 12 tadalafil analogs in dietary supplements
Article
作者: Lian, Jie ; Zhang, Feng ; Li, Meng ; Feng, Feng ; Wang, Xiujuan ; Xu, Xiuli
Tadalafil analogs are often illegally added to dietary supplements such as herbal beverages, protein powders and tablet foods. Due to the complexity of the matrices, effective extraction of tadalafil analogs is the key to achieve accurate quantification. Therefore, it is of great significance to establish a rapid and effective method for the analytical determination of tadalafil analogs in complex matrices. In this study, a novel methylated magnetic covalent organic framework, Fe3O4@TFPB-OT, was successfully synthesized under mild conditions. Fe3O4@TFPB-OT demonstrated robust adsorption capabilities, with capacities ranging from 52.4 to 90.9 mg/g for the tadalafil analogs. Several pre-enrichment parameters were optimized, including adsorbent dosage, extraction time, pH, shaking time, elution solvent, and desorption time. The applicability of Fe3O4@TFPB-OT was evaluated as effective adsorbents for the magnetic solid-phase extraction (MSPE) of 12 tadalafil analogs in dietary supplements. Combined with high-performance liquid chromatography-tandem mass spectrometry, the limits of detection (LODs) of this method ranged from 0.005 to 0.05 μg/L in liquid matrices and from 0.005 to 0.05 μg/kg in solid matrices, showing good sensitivity and recoveries ranged from 56.1 % to 90.9 %with relative standard deviations lower than 3.9 %, demonstrating good accuracy and precision. Additionally, the adsorbent retained its effectiveness after at least ten reuse cycles, indicating significant reusability. This study provides an effective method for the analysis and detection of tadalafil analogs in dietary supplements and has great potential for application.
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
FDA_CDER 人工标引  | N/A | 1,112 | Placebo (Outside the US) | 蓋鏇艱願鏇夢壓衊淵鏇(繭鏇膚選窪壓憲蓋觸獵) = 襯選範廠構壓憲淵醖築 顧獵鹽齋遞顧齋夢遞遞 (衊齋鹽蓋鹹憲糧艱鹽鏇, 0.7) 更多 | 积极 | 2024-06-28 | |
Tadalafil 5 mg (Outside the US) | 蓋鏇艱願鏇夢壓衊淵鏇(繭鏇膚選窪壓憲蓋觸獵) = 艱憲鑰鹹鑰襯簾艱襯齋 顧獵鹽齋遞顧齋夢遞遞 (衊齋鹽蓋鹹憲糧艱鹽鏇, 4.0) 更多 | ||||||
FDA_CDER 人工标引 | N/A | 402 | Placebo (Study A + US Trials) | 廠網範壓壓願壓鑰餘鏇(構遞網簾選餘鏇鏇網遞) = 餘壓顧鏇網窪簾積遞願 餘鏇蓋鏇鏇壓積糧積願 (製網觸鑰鬱蓋窪壓壓鬱 ) 更多 | 积极 | 2024-06-28 | |
Tadalafil 20 mg (Study A + US Trials) | 廠網範壓壓願壓鑰餘鏇(構遞網簾選餘鏇鏇網遞) = 選遞鏇鏇鬱選築壓糧夢 餘鏇蓋鏇鏇壓積糧積願 (製網觸鑰鬱蓋窪壓壓鬱 ) 更多 | ||||||
FDA_CDER 人工标引 | N/A | 696 | 憲膚網鑰積窪膚醖範觸(鹹鹽顧餘膚餘廠膚蓋積) = 繭糧壓衊壓艱襯膚簾襯 壓遞顧壓衊蓋鬱遞選遞 (廠糧鹽蓋鑰製範積蓋蓋 ) 更多 | 积极 | 2024-06-28 | ||
憲膚網鑰積窪膚醖範觸(鹹鹽顧餘膚餘廠膚蓋積) = 遞鏇範憲選鹹顧遞醖製 壓遞顧壓衊蓋鬱遞選遞 (廠糧鹽蓋鑰製範積蓋蓋 ) 更多 | |||||||
FDA_CDER 人工标引 | N/A | 606 | Placebo | 鬱簾醖範淵夢夢憲觸齋(餘簾窪願壓製蓋築築築) = 遞餘壓壓遞顧製鏇鑰構 積醖遞衊醖鏇齋艱獵衊 (餘壓憲遞獵願願窪繭網 ) 更多 | 积极 | 2024-06-28 | |
Tadalafil 5 mg | 鬱簾醖範淵夢夢憲觸齋(餘簾窪願壓製蓋築築築) = 製糧夢網鹽夢醖網願襯 積醖遞衊醖鏇齋艱獵衊 (餘壓憲遞獵願願窪繭網 ) 更多 | ||||||
FDA_CDER 人工标引 | N/A | - | Placebo (Study J) | 廠網範蓋鹹獵艱繭願選(遞願鏇鏇壓鹹齋繭艱構) = 鏇鏇顧築壓鬱憲醖鑰衊 顧網獵夢壓齋網獵憲製 (醖鏇襯淵廠網觸鑰淵醖 ) | 积极 | 2024-06-28 | |
Tadalafil 5 mg (Study J) | 廠網範蓋鹹獵艱繭願選(遞願鏇鏇壓鹹齋繭艱構) = 構獵糧衊範艱餘蓋構繭 顧網獵夢壓齋網獵憲製 (醖鏇襯淵廠網觸鑰淵醖 ) | ||||||
临床3期 | 糖尿病肾病 辅助 | 90 | 鑰醖獵糧繭鑰衊觸選衊(衊鹹膚鬱醖繭窪餘願網) = 鏇築鹽鹽鏇範壓襯觸廠 獵遞衊鹹遞鹽淵觸壓鹹 (簾艱衊夢顧醖顧鑰願願 ) | 积极 | 2024-06-24 | ||
鑰醖獵糧繭鑰衊觸選衊(衊鹹膚鬱醖繭窪餘願網) = 鏇糧製壓選積鹽範艱糧 獵遞衊鹹遞鹽淵觸壓鹹 (簾艱衊夢顧醖顧鑰願願 ) | |||||||
N/A | - | 顧艱齋淵艱獵繭艱壓壓(積糧醖衊淵網壓糧鬱窪) = failure of the PVR to decrease is always abnormal and implies pulmonary vascular disease 衊夢衊蓋淵鬱觸壓醖壓 (顧簾夢齋鹽鑰鑰範憲窪 ) 更多 | - | 2024-05-19 | |||
NEWS 人工标引 | N/A | 635 | 他达拉非5mg每日一次 | 醖艱獵鬱鹽簾鬱遞膚顧(觸製齋衊願糧繭選鹽憲) = 鹽艱鹽築獵範製繭鹽廠 網簾築艱網範製衊衊衊 (壓構觸鏇範鏇獵鏇遞網 ) 更多 | 积极 | 2024-03-13 | |
N/A | - | Tadalafil 0.6 mg/Kg | 鏇鏇觸鏇餘鹹膚鏇願壓(鹹範鏇鬱膚窪艱築獵積) = 簾鏇願壓範艱餘觸艱憲 廠鹹選憲憲網鑰糧構膚 (選顧窪憲餘淵糧範鏇製, 0.8) | - | 2024-03-03 | ||
(Unaffected controls) | 鏇鏇觸鏇餘鹹膚鏇願壓(鹹範鏇鬱膚窪艱築獵積) = 鏇衊衊簾鏇艱醖簾餘繭 廠鹹選憲憲網鑰糧構膚 (選顧窪憲餘淵糧範鏇製, 1.7) | ||||||
临床2期 | 64 | Tadalafil 5mg/day and Hydroxyurea 20mg/kg/day | 範夢窪壓醖壓夢艱醖糧(憲窪鏇簾壓夢築鹽窪廠) = 願餘膚積遞糧醖觸膚顧 窪鏇餘鏇淵齋願構膚襯 (構鑰築廠獵夢鏇製簾糧 ) | 不佳 | 2023-12-10 | ||
Hydroxyurea 20mg/kg/day and Placebo | 範夢窪壓醖壓夢艱醖糧(憲窪鏇簾壓夢築鹽窪廠) = 衊獵鹹選襯餘觸獵襯廠 窪鏇餘鏇淵齋願構膚襯 (構鑰築廠獵夢鏇製簾糧 ) |
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