预约演示
更新于：2026-01-27
Sildenaifl Citrate
枸橼酸西地那非
更新于：2026-01-27
概要
基本信息
简介伟哥可以放松血管壁中的肌肉，增加流向身体特定部位的血液。伟哥用于治疗男性勃起功能障碍（阳痿）。 西地那非的另一个品牌是 Revatio，用于治疗肺动脉高压和提高男性和女性的运动能力。 此页面包含伟哥的特定信息，而不是 Revatio。 西地那非通过阻断磷酸二酯酶 5 (PDE5) 发挥作用，PDE5 是一种促进 cGMP 分解的酶，可调节阴茎中的血流。 它需要性唤起才能起作用。 它还会导致肺部血管扩张。 辉瑞公司最初是在 1989 年发现这种药物的，当时正在寻找治疗与心脏相关的胸痛的方法。 它于 1998 年在美国和欧盟被批准用于医疗用途。 |
药物类型 小分子化药 |
别名 Pahtension、Revatio、Revatio OD + [45] |
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) |
原研机构 |
在研机构 |
最高研发阶段批准上市 |
首次获批日期 美国 (1998-03-27), |
最高研发阶段(中国)批准上市 |
特殊审评孤儿药 (美国)、孤儿药 (欧盟)、孤儿药 (日本)、孤儿药 (韩国)、临床急需境外新药 (中国)、优先审评 (中国) |
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结构/序列
分子式C28H38N6O11S |
InChIKeyDEIYFTQMQPDXOT-UHFFFAOYSA-N |
CAS号171599-83-0 |
关联
709
项与 枸橼酸西地那非 相关的临床试验NCT07290400
Phase 2 Crossover Study Assessing the Effect of Moderate Alcohol Intake on the Absorption and Onset of Action of Hezkue® Sildenafil Oral Suspension
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Evaluation of the Pharmacokinetics and Onset Performance of Hezkue® Oral Sildenafil Suspension Following Alcohol Consumption in Healthy Adults
NCT06800092
Sildenafil to Prevent and Reduce Cancer Related Cognitive Impairment
100 项与 枸橼酸西地那非 相关的临床结果
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100 项与 枸橼酸西地那非 相关的转化医学
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100 项与 枸橼酸西地那非 相关的专利（医药）
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8,629
项与 枸橼酸西地那非 相关的文献（医药）2026-03-01JOURNAL OF STRUCTURAL BIOLOGY
Mechanistic study of PDE5A inhibitors from the prepared folium of Epimedium sagittatum maxim
Article
作者: Xie, Huifang ; Zheng, Xiangwei ; Shi, Wanyin ; Fang, Yuan ; Wu, Siqi ; Pan, Lifeng ; Yao, Guangtao ; Zang, Yunxiang ; Xu, Jian ; Li, Senjie ; Wang, Hongji ; Tao, Houchao ; Chen, Jialiang
Phosphodiesterase-5 (PDE5A) is a critical therapeutic target for treating male erectile dysfunction (ED). PDE5A inhibitors like sildenafil are clinically effective, but exhibit side effects due to non-specific inhibition of related PDE isoforms. This necessitates the discovery of safer and specific PDE5A inhibitors. The prepared folium of Epimedium sagittatum (PFES) is a primary sovereign drug in traditional Chinese medicine (TCM) formulations for ED. As part of ongoing research into its pharmacodynamic basis, this study isolated and identified forty-four flavonoids and organic acids from PFES. The inhibitory activities of these compounds against PDE5A were systematically evaluated, and three compounds (1, 5, and 6) are demonstrated to have significant PDE5A inhibition activities. Notably, the compound 6 (baohuoside I), was previously confirmed the activitywith PDE5A, and its co-crystal structure with PDE5A was also reported. To elucidate the molecular mechanisms underlying the inhibition of PDE5A by compound 1 and 5, we solved the crystal structures of the catalytic domain of PDE5A in complex with compound 1 and 5. Further structural analyses revealed distinct binding modes adopted by 1 and 5 for occupying the PDE5A active site, highlighting their specific interactions with PDE5A compared to each other and to other established inhibitors like sildenafil. In summary, these findings underscore the potential of PFES-derived natural compounds as specific PDE5A inhibitors, and provide crucial insights for the rational development of novel ED therapeutics with potentially improved specificity and reduced side effects based on TCM constituents.
2026-02-01JOURNAL OF ETHNOPHARMACOLOGY
In vivo aphrodisiac efficacy of aqueous and hydroalcoholic extracts of the leaf and root bark of Citropsis articulata (Willd. ex Spreng.) Swingle & M.Kellerm. in male Wistar rats
Article
作者: Tusiimire, Jonans ; Angupale, Jimmy Ronald ; Ogwang, Patrick Engeu ; Amito, Vivian Sharon ; Ajayi, Clement Olusoji ; Amaza, Ronald Anyase ; Amutuhaire, Treasure Angie ; Abdelgadir, Abdelgadir Alamin ; Anywar, Godwin
ETHNOPHARMACOLOGICAL RELEVANCE:
Citropsis articulata (Willd. ex Spreng.) Swingle & M.Kellerm (Rutaceae), commonly known as the African cherry orange, is traditionally used to enhance male sexual performance and manage erectile dysfunction in various African communities.
AIM OF THE STUDY:
This study aimed to evaluate the aphrodisiac efficacy of the aqueous and hydroalcoholic extracts of C. articulata leaf and root bark in male Wistar rats.
MATERIALS AND METHODS:
Aqueous extracts (decoctions) were prepared by boiling 500 g of dried herbal powder in 4 L of distilled water for 60 min. Hydroalcoholic extracts were obtained by Soxhlet extraction, where 500 g of the powder was continuously percolated with 2.5 L of 70 % ethanol. Male Wistar rats (n = 6 per group) were administered the extracts at doses of 100, 500, and 1000 mg/kg daily for 28 days. Control groups included two negative controls (distilled water and 10% DMSO + 0.1% gum arabic) and a positive control (sildenafil citrate, 5 mg/kg). Sexual behaviour parameters-including attraction to the female, penile erection, mount frequency, and mount latency-were assessed on days 0, 3, 7, 14, 21, and 28. At day 28, three animals per group were sacrificed for evaluation of testosterone levels, sexual organ weights, and histological analysis. The remaining three animals in each group were observed without further dosing for an additional 14 days, with behavioural assessments on days 35 and 42, before being sacrificed for post-treatment evaluation of sustained or delayed effects.
RESULTS:
Both the root bark and leaf extracts of C. articulata significantly enhanced attraction towards the female, penile erection, and mount frequency, while reducing mount latency in male Wistar rats. The leaf extracts exhibited a slightly stronger aphrodisiac effect compared to the root bark, especially at the 500 mg/kg dose, where the leaf decoction produced a greater increase in testosterone levels and more pronounced improvements in sexual behaviour. Notably, administration of the leaf decoction at 500 mg/kg resulted in a significantly higher testosterone level (14.50 ± 2.53 ng/ml) compared to the positive control (sildenafil citrate, 4.00 ± 2.70 ng/ml; p = 0.021, 95 % CI: -19.45 to -1.533). After 28 days of treatment, testosterone levels were elevated across all extract-treated groups but declined markedly in animals monitored for an additional 14 days without dosing. Histological analysis showed active spermatogenesis during treatment, which diminished following cessation of extract administration.
CONCLUSION:
This study revealed that both the root bark and leaf of C. articulata have aphrodisiac efficacy in male Wistar rats in vivo.
2026-02-01VETERINARY RESEARCH COMMUNICATIONS
The impacts of L-citrulline and sildenafil on penile and testicular vascular perfusion pattern, advanced testicular analysis, steroids, and semen picture in normospermic dogs
Article
作者: Abdelnaby, Elshymaa A
This study aimed for the first time to demonstrate the effects of combination of L-citrulline and sildenafil (L-Cit + S) on penile and testicular vascular perfusions in dogs regarding the semen quality and hormonal profile. Normospermic German Shepherd dogs were subdivided into three groups (n = 6/each); control group that injected 1 ml saline, second group subjected to L-Citrulline intravenous injection (L-Cit), and third one administrated oral dose of sildenafil with injected L-Cit (L-Cit + S). Dogs were examined at time points of assessment by hours. Semen collection, blood sampling, hormonal assaying, Doppler evaluation and testicular echo-texture analysis were performed. Testicular colored area (TCA) elevated significantly (P = 0.03) in L-Cit group at 8-120 h compared to other groups. While volume, echogenicity, and heterogeneity were not changed (P ≥ 0.05) among groups. Testicular and penile arteries Doppler indices were decreased (P = 0.01) in L-Cit group from 1 to 48 h with a sharp decrease (P = 0.01) was observed in L-Cit + S group within 1-8 h with a significant (P = 0.01) elevation of peak velocity and blood flow rate within the same hours in the same group. Motility % and sperm concentrations were increased (P = 0.02) at 4 h in third group. Circulating L-Cit levels were increased in second and third groups from 4 to 24 h, while S levels were (P = 0.01) increased from 1 to 4 h only in third group. An elevation of nitric oxide and estradiol levels was observed (P = 0.01) form 1 h in L-Cit + S group compared to other groups, while testosterone levels were increased (P = 0.01) from 1 h but rapidly declined till reach a lowest value at 48 h compared to other groups. Addition of L-citrulline to sildenafil demonstrated a more efficiency in improvement of blood flow, hormonal profile, and semen quality than using sildenafil alone due to the action of L-Cit on nitric oxide.
100 项与 枸橼酸西地那非 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 |
|---|---|---|---|
| 特发性肺动脉高压 | 欧盟 | 2016-09-15 | |
| 特发性肺动脉高压 | 冰岛 | 2016-09-15 | |
| 特发性肺动脉高压 | 列支敦士登 | 2016-09-15 | |
| 特发性肺动脉高压 | 挪威 | 2016-09-15 | |
| 肺性高血压 | 日本 | 2008-01-25 | |
| 家族性肺动脉高压 | 欧盟 | 2005-10-28 | |
| 家族性肺动脉高压 | 冰岛 | 2005-10-28 | |
| 家族性肺动脉高压 | 列支敦士登 | 2005-10-28 | |
| 家族性肺动脉高压 | 挪威 | 2005-10-28 | |
| 与先天性心脏病相关的肺动脉高压 | 欧盟 | 2005-10-28 | |
| 与先天性心脏病相关的肺动脉高压 | 冰岛 | 2005-10-28 | |
| 与先天性心脏病相关的肺动脉高压 | 列支敦士登 | 2005-10-28 | |
| 与先天性心脏病相关的肺动脉高压 | 挪威 | 2005-10-28 | |
| 与结缔组织病相关的肺动脉高压 | 欧盟 | 2005-10-28 | |
| 与结缔组织病相关的肺动脉高压 | 冰岛 | 2005-10-28 | |
| 与结缔组织病相关的肺动脉高压 | 列支敦士登 | 2005-10-28 | |
| 与结缔组织病相关的肺动脉高压 | 挪威 | 2005-10-28 | |
| 肺动脉高压 | 美国 | 2005-06-03 | |
| 勃起功能障碍 | 美国 | 1998-03-27 |
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 |
|---|---|---|---|---|
| 心脏衰竭 | 临床3期 | 加拿大 | 2018-03-12 | |
| 低氧性呼吸衰竭 | 临床3期 | 美国 | 2013-08-05 | |
| 低氧性呼吸衰竭 | 临床3期 | 比利时 | 2013-08-05 | |
| 低氧性呼吸衰竭 | 临床3期 | 加拿大 | 2013-08-05 | |
| 低氧性呼吸衰竭 | 临床3期 | 丹麦 | 2013-08-05 | |
| 低氧性呼吸衰竭 | 临床3期 | 法国 | 2013-08-05 | |
| 低氧性呼吸衰竭 | 临床3期 | 德国 | 2013-08-05 | |
| 低氧性呼吸衰竭 | 临床3期 | 意大利 | 2013-08-05 | |
| 低氧性呼吸衰竭 | 临床3期 | 荷兰 | 2013-08-05 | |
| 低氧性呼吸衰竭 | 临床3期 | 挪威 | 2013-08-05 |
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临床结果
临床结果
适应症
分期
评价
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临床2期 | 125 | (Cohort 1, Sildenafil) | 廠鑰範醖獵鹽醖鹹蓋顧 = 鏇選衊網製範鏇膚鏇衊 鑰構鹽製糧鏇築鏇廠醖 (蓋廠蓋壓醖醖觸餘蓋願, 膚積艱衊齋積夢廠齋艱 ~ 齋夢襯鑰觸積衊鹹願構) 更多 | - | 2026-01-26 | ||
(Cohort 2, Sildenafil) | 廠鑰範醖獵鹽醖鹹蓋顧 = 醖壓齋築艱醖蓋蓋積鑰 鑰構鹽製糧鏇築鏇廠醖 (蓋廠蓋壓醖醖觸餘蓋願, 鏇餘製構艱醖糧顧蓋襯 ~ 遞廠築蓋廠壓艱鑰蓋窪) 更多 | ||||||
临床2期 | 22 | Ocular Coherence Tomography-Angiography (OCT-A)+sildenafil | 製夢鹽鬱網膚選願鹹夢(願襯夢顧獵築淵膚顧築) = 選蓋構膚積鹹艱獵艱鏇 廠製膚簾淵餘鏇築齋獵 (糧構鏇蓋選鹹築衊鏇膚, 0.21) 更多 | - | 2025-07-04 | ||
N/A | - | 糧壓壓齋夢製蓋願醖鏇(範簾鏇憲積鹹壓憲遞範) = Macitentan and Bosentan had statistically significant ROR of deaths when compared to Ambrisentan 鹽製夢積夢憲齋鏇夢齋 (糧築餘餘製鏇衊繭願鑰 ) 更多 | - | 2025-05-16 | |||
临床1/2期 | 心脏衰竭 cGMP | 67 | Low-dose intravenous BNP (0.005 µg/kg per minute) | 鏇網獵範齋製鹽鬱顧觸(糧糧觸遞壓窪製夢衊簾) = 積築廠餘齋鹹蓋餘襯鬱 齋鬱憲膚憲襯膚鏇蓋構 (餘獵網襯壓觸構糧簾簾, -14.6% ~ +9.4%) 更多 | 不佳 | 2024-12-01 | |
鏇網獵範齋製鹽鬱顧觸(糧糧觸遞壓窪製夢衊簾) = 齋廠繭醖壓餘顧齋顧簾 齋鬱憲膚憲襯膚鏇蓋構 (餘獵網襯壓觸構糧簾簾, -5.3% ~ +18.8%) 更多 | |||||||
临床2期 | 193 | 蓋簾獵壓構衊襯願膚蓋(窪鑰鏇淵艱積遞網觸窪) = 憲遞製網鏇糧顧襯艱製 餘遞選遞構餘鑰蓋積淵 (壓觸艱廠廠簾廠膚窪襯 ) 更多 | 积极 | 2024-07-31 | |||
Placebo | 蓋簾獵壓構衊襯願膚蓋(窪鑰鏇淵艱積遞網觸窪) = 製鏇鑰壓糧鏇顧獵網鬱 餘遞選遞構餘鑰蓋積淵 (壓觸艱廠廠簾廠膚窪襯 ) 更多 | ||||||
早期临床1期 | 20 | (Sildenafil) | 鬱淵衊鹹憲艱簾願鑰齋(艱鹽構廠窪夢顧繭鹹觸) = 壓範遞獵窪窪鹽構齋夢 糧鬱積膚憲網繭繭襯衊 (鑰淵襯衊襯淵築顧淵窪, 顧鬱糧遞簾築窪繭膚蓋 ~ 蓋簾廠獵襯獵網遞範網) 更多 | - | 2024-07-10 | ||
Placebo Oral Tablet (Placebo Oral Tablet) | 鬱淵衊鹹憲艱簾願鑰齋(艱鹽構廠窪夢顧繭鹹觸) = 壓選網遞蓋窪網窪餘餘 糧鬱積膚憲網繭繭襯衊 (鑰淵襯衊襯淵築顧淵窪, 窪襯獵壓繭獵鏇窪衊憲 ~ 壓鑰淵襯憲衊壓構餘鹽) 更多 | ||||||
临床2期 | 75 | 夢齋網鹹餘繭簾構積齋(選廠齋膚淵鬱範範醖選) = 鏇鏇積鬱齋網鹽夢製鹽 網齋憲鏇鬱衊夢獵蓋壓 (鏇願鹽製壓艱觸鹽壓艱, 0.5 ~ 3.15) 更多 | 积极 | 2024-07-05 | |||
临床4期 | 385 | Sildenafil 80 mg TID | 憲願壓廠繭鏇鏇襯壓鑰(網衊鹽繭艱鹹鏇選壓鹹): HR = 0.51 (95% CI, 0.22 ~ 1.21), P-Value = <0.001 更多 | 非劣 | 2024-06-18 | ||
Sildenafil 5 mg TID | |||||||
临床2期 | - | 顧範壓齋廠膚範構選餘(艱鹹獵鏇製鹽艱鹹夢繭) = 構壓窪鑰鹽蓋憲膚鹹鹹 齋鹹願顧鏇製觸鏇簾獵 (築鏇繭選窪願範簾壓糧, 0.62) | 积极 | 2024-06-18 | |||
Placebo | 顧範壓齋廠膚範構選餘(艱鹹獵鏇製鹽艱鹹夢繭) = 夢憲鹽網壓餘衊襯願鹹 齋鹹願顧鏇製觸鏇簾獵 (築鏇繭選窪願範簾壓糧, 0.04) | ||||||
临床1期 | 晚期恶性实体瘤 PDE5 expression in tumor samples | 29 | 簾壓簾齋觸鏇鬱鏇遞齋(夢蓋餘鬱築鹹衊鹽餘齋) = The most common toxicities included palmar-plantar erythrodysesthesia syndrome (20 patients, 69%) and hypophosphatemia (18 patients, 62%). 廠窪鹹鏇夢齋顧範製鏇 (糧顧製觸獵膚網鹽獵窪 ) 更多 | 积极 | 2024-03-08 |
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