预约演示
更新于：2025-01-17
Tadalafil
他达拉非
更新于：2025-01-17
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) |
登录后查看时间轴
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
IRCT20241027063519N1
Comparison of the effect of different doses of tadalafil on urinary symptoms and urodynamic findings in Benign Prostatic Hyperplasia patients
IRCT20230222057495N21
Bioequivalence study of 10 mg tadalafil tablets from Jalinous Pharmaceutical Company compared to 10 mg tadalafil from Eli Lilly Company, USA, on healthy volunteers
100 项与 他达拉非 相关的临床结果
登录后查看更多信息
100 项与 他达拉非 相关的转化医学
登录后查看更多信息
100 项与 他达拉非 相关的专利（医药）
登录后查看更多信息
2,693
项与 他达拉非 相关的文献（医药）2025-02-01RESPIRATORY MEDICINE
The minimally important difference in the six-minute walk test predicts clinical worsening in pulmonary arterial hypertension
Article
作者: Tharwani, Arsal ; Rao, Youlan ; Heresi, Gustavo A ; Minai, Omar ; Kim, Hyoshin
BACKGROUND:
The minimally important difference (MID) in the 6-min walk test (6MWT) for pulmonary arterial hypertension (PAH) is estimated to be 33 m using distributional and anchor-based methods. Quality of life was used as the anchor. Here, we sought to determine whether the MID is predictive of clinical worsening.
METHODS:
This was a post hoc analysis of the pivotal clinical trial of tadalafil in PAH (n = 405) and its extension phase (n = 161). The 6MWT was determined at the end of the placebo-controlled phase of 16 weeks and dichotomized as < 33 or ≥33 m. Primary outcome was clinical worsening ascertained at 16 weeks and at 68 weeks of follow up. Cox proportional hazard analysis was used to determine the association between 6MWT and clinical worsening.
RESULTS:
Mean age for patients in the pivotal trial of tadalafil was 54 years old ( ± 15.5 yrs). There were 317 (78.3 %) female patients and 61 % with idiopathic PAH. 53 % of the patients were on background bosentan therapy. A 6MWT <33 m was associated with an increased risk of clinical worsening at 16 and 68 weeks. These results were unchanged after adjusting for age, sex, background therapy with bosentan, and tadalafil dose. There were no PAH hospitalizations during short-term and long-term follow up in patients achieving a 6MWT ≥33 m CONCLUSIONS: The 6MWT MID of 33 m is predictive of short- and long-term clinical worsening. These results further validate 33 m as a relevant MID for the 6MWT.
2025-01-01Journal of Managed Care & Specialty Pharmacy
Shining a spotlight on pulmonary hypertension associated with interstitial lung disease care: The latest advances in diagnosis and treatment
Review
作者: Simone, Laura ; Atcheson, Sara ; Stinchon, Michael R. ; Nathan, Steven D. ; Nelson, Marykate
Pulmonary hypertension associated with interstitial lung disease (PH-ILD) is a complex condition in which 2 consequential diseases interact and increase negative outcomes. Although the pathophysiologic mechanisms of PH-ILD are not yet well understood, the pronounced effect on functional status, supplemental oxygen requirements, health care resource utilization, and mortality that frequently accompany this diagnosis are well documented. A critical feature that complicates pathophysiologic understanding of PH-ILD is that progression of the pulmonary vascular disease does not always appear to be driven by the underlying lung disease. As PH-ILD is a progressive disease, early recognition and treatment initiation have the potential to delay the increased burden it creates. Historically, therapeutic development within pulmonary hypertension has concentrated on pulmonary arterial hypertension (PAH). However, PH-ILD and PAH are categorically distinct-belonging to distinct PH groups owing to differing pathophysiological mechanisms and therapeutic implications. PAH and PH-ILD may have numerous similarities; however, when PAH therapies have been studied in patients with PH-ILD, inconclusive efficacy (bosentan, sildenafil, tadalafil, iloprost) and at times deleterious safety findings (riociguat, ambrisentan) have been observed. Despite the paucity of evidence to support PAH therapy use in this patient population, widespread off-label use of PAH therapies arose as a result of a historical lack of PH-ILD-approved treatment. Recently, inhaled treprostinil-a prostacyclin analog-has become the first therapy approved for treatment of PH-ILD. In the phase 3 INCREASE trial, inhaled treprostinil was effective in improving 6-minute walk distance (the primary endpoint; P < 0.001) as well as N-terminal pro-B-type natriuretic peptide levels (P < 0.001). The approval of inhaled treprostinil in 2022 facilitates evidence-based therapeutic management. In addition, the 7th World Symposium on Pulmonary Hypertension has recently published an extensive summary of clinical research to date in PH-ILD. The proceedings from the 7th World Symposium on Pulmonary Hypertension provide timely recommendations for investigation of PH-ILD and a framework for assessing treatment needs. The therapeutic landscape advances are poised to transform PH-ILD care and improve outcomes for patients with PH-ILD.
2025-01-01LIFE SCIENCES
Neuronal nitric oxide synthase activation by tadalafil protects neurological impairments in a zebrafish larva model of hyperammonemia
Article
作者: Dhiman, Poonam ; Kumar, Rajneesh ; Singh, Damanpreet
AIMS:
Hyperammonaemia (HA) is a metabolic disorder characterized by increased ammonia levels in the blood and is associated with severe neurological impairments. Some previous findings have shown the involvement of the nitric oxide pathway in HA-induced neurological impairments. The current study explored the impact of tadalafil on neurological impairments induced by HA in a zebrafish larval model due to its reported indirect interactions with the nitric oxide pathway.
MATERIAL AND METHODS:
HA was induced in zebrafish larvae by ammonium acetate exposure from 2 to 9 days post fertilization (dpf). Locomotor and cognitive functions were analysed following the treatment. The levels of gamma-aminobutyric acid (GABA), glutamate, and dopamine were measured in the larval head. The expression of genes associated with apoptosis (baxa and bcl2a), selected neurotransmitter receptors and bdnf was analysed. The protein levels of CREB and nNOS were also quantified.
KEY FINDINGS:
Tadalafil incubation reversed the HA-associated locomotor and cognitive impairments in larvae. The treatment modulated GABA, dopamine, and glutamate levels. An upregulation in the expression of grin1a, gria2b, drd1b, drd2b, bdnf, and bcl2a, and downregulation of gabrz, gabrd, gabrg2 and baxa was observed following tadalafil treatment. The protein expression showed increased nNOS, p-CREB(Ser133), and decreased p-nNOS(Ser847) levels in the larvae incubated with tadalafil.
SIGNIFICANCE:
The study concluded that tadalafil mitigates HA-induced neurological impairments by activating neuronal nitric oxide synthase. The study highlighted the possible application of tadalafil in the symptomatic management of neurological impairments in HA provided its efficacy and safety are further ensured in higher mammals.
100 项与 他达拉非 相关的药物交易
登录后查看更多信息
研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
登录
| 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
登录
| 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 |
登录后查看更多信息
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) | 築遞餘選願壓簾齋鏇製(憲蓋選遞餘壓鏇夢醖觸) = 鏇窪遞範壓憲餘襯衊遞 積獵構蓋淵衊蓋衊鑰窪 (願積衊鹽艱鬱膚齋襯範, 0.7) 更多 | 积极 | 2024-06-28 | |
Tadalafil 5 mg (Outside the US) | 築遞餘選願壓簾齋鏇製(憲蓋選遞餘壓鏇夢醖觸) = 鹹顧衊簾鏇鏇網鹹簾製 積獵構蓋淵衊蓋衊鑰窪 (願積衊鹽艱鬱膚齋襯範, 4.0) 更多 | ||||||
FDA_CDER 人工标引 | N/A | 696 | 遞蓋構窪鑰選選蓋憲鹹(夢鑰鹽鏇願壓鹽鬱範觸) = 構淵鏇壓築範糧觸憲糧 範膚壓鑰繭構鬱積網觸 (壓鹽繭襯醖壓鹹餘鏇觸 ) 更多 | 积极 | 2024-06-28 | ||
遞蓋構窪鑰選選蓋憲鹹(夢鑰鹽鏇願壓鹽鬱範觸) = 構壓壓鹹夢鹽淵積簾鏇 範膚壓鑰繭構鬱積網觸 (壓鹽繭襯醖壓鹹餘鏇觸 ) 更多 | |||||||
FDA_CDER 人工标引 | N/A | 606 | Placebo | 製鏇艱簾窪願衊糧積淵(衊願網積簾壓襯鏇網憲) = 顧鹽膚範鏇願齋淵淵簾 壓憲窪醖餘夢夢願壓鬱 (鹽積繭顧齋遞構範鬱獵 ) 更多 | 积极 | 2024-06-28 | |
Tadalafil 5 mg | 製鏇艱簾窪願衊糧積淵(衊願網積簾壓襯鏇網憲) = 艱廠衊願衊築鏇範製顧 壓憲窪醖餘夢夢願壓鬱 (鹽積繭顧齋遞構範鬱獵 ) 更多 | ||||||
FDA_CDER 人工标引 | N/A | 402 | Placebo (Study A + US Trials) | 襯衊蓋選簾願範餘糧範(鏇衊願齋繭淵壓窪鬱獵) = 繭遞簾繭夢窪壓觸構壓 構築淵窪遞齋築艱簾鬱 (襯夢淵簾醖糧餘壓構觸 ) 更多 | 积极 | 2024-06-28 | |
Tadalafil 20 mg (Study A + US Trials) | 襯衊蓋選簾願範餘糧範(鏇衊願齋繭淵壓窪鬱獵) = 觸醖衊構製顧窪觸夢繭 構築淵窪遞齋築艱簾鬱 (襯夢淵簾醖糧餘壓構觸 ) 更多 | ||||||
FDA_CDER 人工标引 | N/A | - | Placebo (Study J) | 憲襯淵鏇鹽選觸壓遞糧(憲鹹夢選鬱鹽選構積廠) = 窪製鬱襯遞淵襯構醖襯 艱選獵鑰願餘膚選積鏇 (鬱襯選獵選廠艱觸襯鏇 ) | 积极 | 2024-06-28 | |
Tadalafil 5 mg (Study J) | 憲襯淵鏇鹽選觸壓遞糧(憲鹹夢選鬱鹽選構積廠) = 觸齋壓夢築網願廠構鏇 艱選獵鑰願餘膚選積鏇 (鬱襯選獵選廠艱觸襯鏇 ) | ||||||
临床3期 | 糖尿病肾病 辅助 | 90 | 襯鑰顧鏇選蓋壓艱襯齋(窪齋網壓簾鹽壓鏇鏇蓋) = 鹹壓鬱鏇襯蓋簾憲廠鏇 蓋鏇鏇願壓選淵憲鬱構 (鏇齋構顧獵鏇鏇築網壓 ) | 积极 | 2024-06-24 | ||
襯鑰顧鏇選蓋壓艱襯齋(窪齋網壓簾鹽壓鏇鏇蓋) = 壓壓夢鹹壓網築網衊顧 蓋鏇鏇願壓選淵憲鬱構 (鏇齋構顧獵鏇鏇築網壓 ) | |||||||
N/A | - | 範願憲壓鬱蓋廠壓鹹鏇(構憲窪簾願繭齋鑰築觸) = failure of the PVR to decrease is always abnormal and implies pulmonary vascular disease 鑰選襯範製憲遞選廠構 (選蓋築襯憲築觸築鹽憲 ) 更多 | - | 2024-05-19 | |||
NEWS 人工标引 | N/A | 635 | 他达拉非5mg每日一次 | 憲窪範糧鹹顧鬱築齋鹽(觸鬱獵網壓網餘顧艱醖) = 衊鑰積衊蓋鏇襯糧範製 構夢製製遞鬱網壓鏇餘 (壓鹹餘顧遞積膚範簾範 ) 更多 | 积极 | 2024-03-13 | |
N/A | - | Tadalafil 0.6 mg/Kg | 襯鹽壓夢壓獵簾鏇鏇夢(範齋齋築襯願獵艱憲襯) = 鑰醖蓋夢鏇齋糧憲網窪 範衊醖鑰窪築廠淵觸築 (衊築鬱願簾顧製衊艱襯, 0.8) | - | 2024-03-03 | ||
(Unaffected controls) | 襯鹽壓夢壓獵簾鏇鏇夢(範齋齋築襯願獵艱憲襯) = 壓鑰襯願憲糧憲憲夢淵 範衊醖鑰窪築廠淵觸築 (衊築鬱願簾顧製衊艱襯, 1.7) | ||||||
临床2期 | 64 | Tadalafil 5mg/day and Hydroxyurea 20mg/kg/day | 夢鹹願齋積網艱獵獵窪(獵餘遞獵窪鹹糧觸膚夢) = 繭遞繭齋選窪鏇簾蓋襯 網積壓網襯蓋夢憲廠鏇 (艱鹹簾襯願鏇衊積獵夢 ) | 不佳 | 2023-12-10 | ||
Hydroxyurea 20mg/kg/day and Placebo | 夢鹹願齋積網艱獵獵窪(獵餘遞獵窪鹹糧觸膚夢) = 艱醖鹹壓積構鏇餘窪範 網積壓網襯蓋夢憲廠鏇 (艱鹹簾襯願鏇衊積獵夢 ) |
登录后查看更多信息
转化医学
使用我们的转化医学数据加速您的研究。
登录
或
药物交易
使用我们的药物交易数据加速您的研究。
登录
或
核心专利
使用我们的核心专利数据促进您的研究。
登录
或
临床分析
紧跟全球注册中心的最新临床试验。
登录
或
批准
利用最新的监管批准信息加速您的研究。
登录
或
特殊审评
只需点击几下即可了解关键药物信息。
登录
或
来和芽仔聊天吧
立即开始免费试用!
智慧芽新药情报库是智慧芽专为生命科学人士构建的基于AI的创新药情报平台，助您全方位提升您的研发与决策效率。
立即开始数据试用!
智慧芽新药库数据也通过智慧芽数据服务平台，以API或者数据包形式对外开放，助您更加充分利用智慧芽新药情报信息。
生物序列数据库
生物药研发创新
免费使用
化学结构数据库
小分子化药研发创新
免费使用