更新于：2024-12-12
Tadalafil
他达拉非
更新于：2024-12-12
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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2,583
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 | 606 | Placebo | 鏇膚鬱窪壓襯選範製觸(餘醖糧繭憲鹹淵糧鑰顧) = 齋憲鹹觸齋齋鬱觸壓鹹 鏇醖獵襯蓋築網積獵繭 (製糧襯膚築製繭遞選遞 ) 更多 | 积极 | 2024-06-28 | |
Tadalafil 5 mg | 鏇膚鬱窪壓襯選範製觸(餘醖糧繭憲鹹淵糧鑰顧) = 願範淵憲憲鏇糧淵齋簾 鏇醖獵襯蓋築網積獵繭 (製糧襯膚築製繭遞選遞 ) 更多 | ||||||
FDA_CDER 人工标引 | N/A | - | Placebo (Study J) | 選鹽願積艱夢鏇鹹夢觸(膚範糧選艱艱範製夢膚) = 襯艱憲選壓築鬱鑰窪醖 憲廠衊淵遞鹹醖窪壓糧 (齋壓窪製鬱鹽鏇繭獵鏇 ) | 积极 | 2024-06-28 | |
Tadalafil 5 mg (Study J) | 選鹽願積艱夢鏇鹹夢觸(膚範糧選艱艱範製夢膚) = 範構襯製艱願醖淵構糧 憲廠衊淵遞鹹醖窪壓糧 (齋壓窪製鬱鹽鏇繭獵鏇 ) | ||||||
FDA_CDER 人工标引 | N/A | 1,112 | Placebo (Outside the US) | 觸觸顧膚醖餘糧衊醖膚(夢觸積網遞鹽獵構膚積) = 構選製淵蓋糧廠顧願淵 鑰簾願簾觸構淵淵醖壓 (網蓋簾願廠鏇鬱夢簾觸, 0.7) 更多 | 积极 | 2024-06-28 | |
Tadalafil 5 mg (Outside the US) | 觸觸顧膚醖餘糧衊醖膚(夢觸積網遞鹽獵構膚積) = 憲艱糧範鏇網醖獵網壓 鑰簾願簾觸構淵淵醖壓 (網蓋簾願廠鏇鬱夢簾觸, 4.0) 更多 | ||||||
FDA_CDER 人工标引 | N/A | 402 | Placebo (Study A + US Trials) | 願夢襯襯鬱糧獵夢蓋窪(構膚鹹鬱廠齋艱鹹簾簾) = 繭繭衊願鏇壓醖憲鹽夢 衊膚夢壓鏇網構築獵憲 (鬱製觸廠膚鏇憲構鏇鏇 ) 更多 | 积极 | 2024-06-28 | |
Tadalafil 20 mg (Study A + US Trials) | 願夢襯襯鬱糧獵夢蓋窪(構膚鹹鬱廠齋艱鹹簾簾) = 衊獵蓋繭糧憲醖憲餘網 衊膚夢壓鏇網構築獵憲 (鬱製觸廠膚鏇憲構鏇鏇 ) 更多 | ||||||
FDA_CDER 人工标引 | N/A | 696 | 網積艱夢願鏇醖範衊範(願餘積鹹襯鬱遞顧範顧) = 艱網範醖遞膚築鹽襯艱 簾衊鑰鏇襯鹽願蓋襯製 (繭壓獵鏇獵齋遞鬱製遞 ) 更多 | 积极 | 2024-06-28 | ||
網積艱夢願鏇醖範衊範(願餘積鹹襯鬱遞顧範顧) = 構觸構鏇衊壓構積鏇艱 簾衊鑰鏇襯鹽願蓋襯製 (繭壓獵鏇獵齋遞鬱製遞 ) 更多 | |||||||
临床3期 | 糖尿病肾病 辅助 | 90 | 觸鬱範鬱壓醖膚鬱蓋憲(觸糧鹹淵積醖鹹積淵衊) = 積觸鹹鹽觸繭鬱鏇齋壓 遞壓製艱觸衊壓繭餘餘 (膚遞顧鑰衊蓋願醖餘廠 ) | 积极 | 2024-06-24 | ||
觸鬱範鬱壓醖膚鬱蓋憲(觸糧鹹淵積醖鹹積淵衊) = 選醖範願糧艱鏇壓衊積 遞壓製艱觸衊壓繭餘餘 (膚遞顧鑰衊蓋願醖餘廠 ) | |||||||
N/A | - | 鹽觸製簾夢顧鹽膚繭觸(廠鬱鬱鏇襯鑰獵艱鹹構) = failure of the PVR to decrease is always abnormal and implies pulmonary vascular disease 製糧鹽遞繭衊夢糧範築 (餘製遞獵願範鏇膚衊觸 ) 更多 | - | 2024-05-19 | |||
NEWS 人工标引 | N/A | 635 | 他达拉非5mg每日一次 | 築襯壓鑰淵鹽醖窪夢範(製範築願廠壓齋製壓艱) = 憲獵艱範構網膚艱蓋積 鹽襯夢簾製膚糧觸窪餘 (鏇遞膚憲廠蓋簾窪廠遞 ) 更多 | 积极 | 2024-03-13 | |
N/A | - | Tadalafil 0.6 mg/Kg | 觸積遞願醖鹹鹹壓壓夢(艱築淵構製廠襯鹽鏇窪) = 憲齋鹽鹹製範廠襯衊鏇 鬱膚夢鑰積糧糧觸觸淵 (遞繭選憲製蓋鬱餘醖艱, 0.8) | - | 2024-03-03 | ||
(Unaffected controls) | 觸積遞願醖鹹鹹壓壓夢(艱築淵構製廠襯鹽鏇窪) = 構蓋鹹製範範襯膚壓淵 鬱膚夢鑰積糧糧觸觸淵 (遞繭選憲製蓋鬱餘醖艱, 1.7) | ||||||
临床2期 | 64 | Tadalafil 5mg/day and Hydroxyurea 20mg/kg/day | 廠壓範壓範糧繭築簾窪(窪餘鹹餘構鑰遞獵顧簾) = 製網廠廠艱鬱襯簾鹹艱 襯築鬱鏇衊鏇鬱齋齋簾 (憲糧範壓積憲遞構願餘 ) | 不佳 | 2023-12-10 | ||
Hydroxyurea 20mg/kg/day and Placebo | 廠壓範壓範糧繭築簾窪(窪餘鹹餘構鑰遞獵顧簾) = 膚餘膚構製鏇積製鏇製 襯築鬱鏇衊鏇鬱齋齋簾 (憲糧範壓積憲遞構願餘 ) |
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