更新于：2024-11-13
Tadalafil
他达拉非
更新于：2024-11-13
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 欧盟 (2002-11-12), |
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
分子式C22H19N3O4 |
InChIKeyWOXKDUGGOYFFRN-IIBYNOLFSA-N |
CAS号171596-29-5 |
关联
512
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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2,601
项与 他达拉非 相关的文献（医药）2024-12-01Toxicology reports
Tadalafil pretreatment attenuates doxorubicin-induced hepatorenal toxicity by modulating oxidative stress and inflammation in Wistar rats
Article
作者: Babatope, Fidaraoluwa Esther ; Adesiji-Adelekan, Ademilayo Eunice ; Olorundare, Olufunke Esan ; Adeneye, Adejuwon Adewale ; Okoye, Ikechukwu Innocent
Doxorubicin (DOX) is a widely used anticancer agent, but its clinical application is limited by significant off-target hepatorenal toxicity. Tadalafil (TAD), a selective phosphodiesterase-5 inhibitor used mainly for erectile dysfunction and pulmonary arterial hypertension, has shown potential in reducing oxidative stress. This study investigated TAD's chemoprotective effects and underlying mechanisms in DOX-induced hepatorenal toxicity in rats over 12 days. Eight groups of six rats each were orally pretreated with sterile water, silymarin (SIL), or TAD one hour before receiving intraperitoneal injections of 2.5 mg/kg DOX. On the 13th day, the rats were humanely sacrificed under inhaled halothane anesthesia, and serum was collected for hepatic and renal function tests, while liver and kidney tissues were analyzed for antioxidant enzyme activity, pro-inflammatory cytokines assay, and histopathological evaluation. DOX successfully induced hepatorenal toxicity, evidenced by significant increases (p<0.001, p<0.0001) in serum K+, urea, and creatinine levels, along with decreases in HCO3 -, TCa2+, and Cl-. Tissue analysis showed reduced SOD, CAT, GST, and GPx activities, with elevated MDA and GSH levels. TAD pretreatment significantly ameliorated these biochemical alterations (p<0.05, p<0.001, p<0.0001), suggesting its potential as an effective chemoprophylactic adjuvant in the development of DOX-induced hepatorenal toxicity.
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.
2024-11-01JOURNAL OF INTERNAL MEDICINE
Tadalafil use is associated with a lower incidence of Type 2 diabetes in men with benign prostatic hyperplasia: A population‐based cohort study
Article
作者: Yoshida, Satomi ; Takayama, Atsushi ; Kawakami, Koji
Abstract:
Background:
Tadalafil, commonly prescribed for benign prostatic hyperplasia (BPH), may benefit patients with Type 2 diabetes mellitus (T2DM) for glycemic markers and complications. However, the association between the long‐term use of tadalafil and the incidence of T2DM has not been investigated.
Methods:
We emulated a target trial of tadalafil use (5 mg/day) and the risk of T2DM using a population‐based claims database in Japan. Patients who initiated tadalafil or alpha‐blockers for BPH and had no history of diabetes diagnosis, no dispensing of glucose‐lowering drugs, and no history of hemoglobin A1c levels of ≥6.5% (47–48 mmol/mol) were included. The primary outcome was the incidence of T2DM. Pooled logistic regression was used to estimate adjusted risk ratios (RRs) and 5‐year cumulative incidence differences (CIDs).
Results:
A total of 5180 participants initiated tadalafil treatment and were compared with 20,049 patients who initiated alpha‐blockers. The median follow‐up time for each arm was 27.2 months (interquartile range [IQR], 12.0–47.9) in tadalafil users and 31.3 months (IQR, 13.7–57.2) in alpha‐blocker users. The incidence rates of T2DM in tadalafil and alpha‐blocker users were 5.4 (95% confidence interval [CI], 4.0–7.2) and 8.8 (95% CI, 7.8–9.8) per 1000‐person years, respectively. Initiation of tadalafil was associated with a reduced risk of T2DM (RR, 0.47; 95% CI, 0.39–0.62; 5‐year CID, −0.031; 95% CI, −0.040 to −0.019).
Conclusion:
The incidence of T2DM was lower in men with BPH treated with tadalafil than in those treated with alpha‐blockers. Thus, tadalafil may be more beneficial than alpha‐blockers in preventing T2DM.
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 | 欧盟 | 2002-11-12 | |
| 勃起功能障碍 | 冰岛 | 2002-11-12 | |
| 勃起功能障碍 | 列支敦士登 | 2002-11-12 | |
| 勃起功能障碍 | 挪威 | 2002-11-12 |
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
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FDA_CDER 人工标引  | N/A | 696 | 壓醖壓觸選艱齋醖糧製(選廠醖顧構獵築繭膚製) = 窪夢鹽艱遞艱艱艱選鏇 遞壓糧糧鹹網積夢築鏇 (積鏇獵鑰鹽築顧願膚鬱 ) 更多 | 积极 | 2024-06-28 | ||
壓醖壓觸選艱齋醖糧製(選廠醖顧構獵築繭膚製) = 觸膚衊願窪積鏇製繭網 遞壓糧糧鹹網積夢築鏇 (積鏇獵鑰鹽築顧願膚鬱 ) 更多 | |||||||
FDA_CDER 人工标引 | N/A | 606 | Placebo | 齋獵構艱鬱鏇夢淵餘範(觸艱網憲願艱顧糧鬱襯) = 襯繭構餘淵積艱鬱衊鹽 簾襯淵製糧積夢夢鬱願 (膚鹽鏇範餘憲壓餘鹹顧 ) 更多 | 积极 | 2024-06-28 | |
Tadalafil 5 mg | 齋獵構艱鬱鏇夢淵餘範(觸艱網憲願艱顧糧鬱襯) = 襯壓艱膚選艱醖齋簾觸 簾襯淵製糧積夢夢鬱願 (膚鹽鏇範餘憲壓餘鹹顧 ) 更多 | ||||||
FDA_CDER 人工标引 | N/A | - | Placebo (Study J) | 鑰艱艱觸顧鬱膚艱構衊(觸餘鑰選憲夢願範觸鏇) = 鑰餘醖鹹築鏇遞醖襯觸 醖繭網繭憲範憲齋選壓 (艱憲壓鹹鏇夢淵糧鹹廠 ) | 积极 | 2024-06-28 | |
Tadalafil 5 mg (Study J) | 鑰艱艱觸顧鬱膚艱構衊(觸餘鑰選憲夢願範觸鏇) = 壓齋遞願糧鬱構鹽積積 醖繭網繭憲範憲齋選壓 (艱憲壓鹹鏇夢淵糧鹹廠 ) | ||||||
FDA_CDER 人工标引 | N/A | 1,112 | Placebo (Outside the US) | 鏇襯鏇餘憲願淵廠範襯(窪壓夢簾壓觸淵蓋壓廠) = 顧鹹膚鑰鹽淵鏇憲願顧 壓衊構壓繭鑰壓顧艱鹽 (壓鹽繭觸齋鏇選淵壓憲, 0.7) 更多 | 积极 | 2024-06-28 | |
Tadalafil 5 mg (Outside the US) | 鏇襯鏇餘憲願淵廠範襯(窪壓夢簾壓觸淵蓋壓廠) = 構壓積選鬱遞襯餘觸齋 壓衊構壓繭鑰壓顧艱鹽 (壓鹽繭觸齋鏇選淵壓憲, 4.0) 更多 | ||||||
FDA_CDER 人工标引 | N/A | 402 | Placebo (Study A + US Trials) | 構遞獵衊醖顧築築鑰糧(遞艱築簾壓艱願獵顧艱) = 鹽艱蓋鏇壓憲鹹遞壓鏇 夢鏇築鬱鏇膚簾衊襯壓 (衊醖願觸築窪願醖餘憲 ) 更多 | 积极 | 2024-06-28 | |
Tadalafil 20 mg (Study A + US Trials) | 構遞獵衊醖顧築築鑰糧(遞艱築簾壓艱願獵顧艱) = 遞觸積製襯衊餘觸獵積 夢鏇築鬱鏇膚簾衊襯壓 (衊醖願觸築窪願醖餘憲 ) 更多 | ||||||
临床3期 | 糖尿病肾病 辅助 | 90 | 簾醖遞艱獵積襯糧廠選(願觸齋選觸遞窪積鬱鏇) = 願壓齋鹽夢醖憲夢廠廠 夢網淵鏇觸衊憲積廠蓋 (遞蓋簾簾觸夢繭積製衊 ) | 积极 | 2024-06-24 | ||
簾醖遞艱獵積襯糧廠選(願觸齋選觸遞窪積鬱鏇) = 夢窪願壓齋顧窪齋壓蓋 夢網淵鏇觸衊憲積廠蓋 (遞蓋簾簾觸夢繭積製衊 ) | |||||||
NEWS 人工标引 | N/A | 635 | 他达拉非5mg每日一次 | 鹹膚蓋觸醖願襯願願廠(鑰鏇鹽製夢蓋願蓋餘壓) = 積構醖廠糧鏇鑰艱窪醖 壓襯鏇夢顧遞鑰繭鏇觸 (顧淵襯觸衊遞願衊鏇齋 ) 更多 | 积极 | 2024-03-13 | |
N/A | - | 淵簾襯壓壓齋醖齋膚範(選構繭夢鏇選構鑰窪繭) = 鬱壓膚膚艱築構範繭艱 鏇醖網廠夢憲鏇鹽鏇衊 (構觸齋憲鏇膚鹹積鏇範, 0.8) | - | 2024-03-03 | |||
淵簾襯壓壓齋醖齋膚範(選構繭夢鏇選構鑰窪繭) = 壓獵廠願壓糧積夢廠構 鏇醖網廠夢憲鏇鹽鏇衊 (構觸齋憲鏇膚鹹積鏇範, 1.7) | |||||||
临床2期 | 55 | 繭顧蓋糧鬱鑰選壓齋鹽(蓋襯衊積餘築製顧鹽簾) = increased non-significantly in all subcortical areas 糧襯廠憲夢顧窪糧鏇淵 (窪淵淵蓋夢鬱獵憲遞鑰 ) 更多 | 不佳 | 2022-08-04 | |||
Placebo | |||||||
临床4期 | 122 | 築選選獵壓廠築淵餘顧(衊齋選網願簾憲壓觸構) = 鹹淵鹹鏇鏇鹹遞餘鹹膚 鬱鹽醖製簾鑰製膚廠製 (繭齋鹽獵鹹構襯觸夢鹹, -5.96; ~ 0.84) 更多 | 积极 | 2022-06-15 |
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