更新于：2024-04-26
Vardenafil Hydrochloride
盐酸伐地那非
更新于：2024-04-26
概要
基本信息
结构
分子式C23H39ClN6O7S |
InChIKeyFBCDRHDULQYRTB-UHFFFAOYSA-N |
CAS号330808-88-3 |
关联
111
项与 盐酸伐地那非 相关的临床试验盐酸伐地那非片在中国健康受试者空腹和餐后状态下的单中心、随机、开放、两制剂、四周期、两序列、单次给药、完全重复交叉生物等效性研究
盐酸伐地那非片在健康受试者中单中心、开放、随机、单剂量、双周期、双交叉
空腹和餐后状态下的生物等效性试验
盐酸伐地那非片人体生物等效性研究
100 项与 盐酸伐地那非 相关的临床结果
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100 项与 盐酸伐地那非 相关的转化医学
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100 项与 盐酸伐地那非 相关的专利（医药）
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1,087
项与 盐酸伐地那非 相关的文献（医药）2024-02-01Journal of Biological Chemistry
Probing the mechanism by which the retinal G protein transducin activates its biological effector PDE6
Article
作者: Aplin, Cody ; Cerione, Richard A
Phototransduction in retinal rods occurs when the G protein-coupled photoreceptor rhodopsin triggers the activation of phosphodiesterase 6 (PDE6) by GTP-bound alpha subunits of the G protein transducin (GαT). Recently, we presented a cryo-EM structure for a complex between two GTP-bound recombinant GαT subunits and native PDE6, that included a bivalent antibody bound to the C-terminal ends of GαT and the inhibitor vardenafil occupying the active sites on the PDEα and PDEβ subunits. We proposed GαT-activated PDE6 by inducing a striking reorientation of the PDEγ subunits away from the catalytic sites. However, questions remained including whether in the absence of the antibody GαT binds to PDE6 in a similar manner as observed when the antibody is present, does GαT activate PDE6 by enabling the substrate cGMP to access the catalytic sites, and how does the lipid membrane enhance PDE6 activation? Here, we demonstrate that 2:1 GαT-PDE6 complexes form with either recombinant or retinal GαT in the absence of the GαT antibody. We show that GαT binding is not necessary for cGMP nor competitive inhibitors to access the active sites; instead, occupancy of the substrate binding sites enables GαT to bind and reposition the PDE6γ subunits to promote catalytic activity. Moreover, we demonstrate by reconstituting GαT-stimulated PDE6 activity in lipid bilayer nanodiscs that the membrane-induced enhancement results from an increase in the apparent binding affinity of GαT for PDE6. These findings provide new insights into how the retinal G protein stimulates rapid catalytic turnover by PDE6 required for dim light vision.
2024-01-01Pharmacoepidemiology and Drug Safety
Oral phosphodiesterase type 5 inhibitors and priapism: A VigiBase analysis
Article
作者: Lui, Jason L ; Breyer, Benjamin N ; Shaw, Nathan M ; Nabavizadeh, Behnam ; Hakam, Nizar ; Abbasi, Behzad
Abstract:
Purpose:
To explore the differences of priapism events among a diverse cohort taking erectogenic medicines (i.e., phosphodiesterase type 5 inhibitors [PDE5i] and intracavernousal drugs).
Method<jats:bold>s</jats:bold>:
We queried the World Health Organization global database of individual case safety reports (VigiBase) for records of the adverse drug reactions (ADR) with sildenafil, tadalafil, avanafil, vardenafil, papaverine, and alprostadil. Disproportionality analyses (case/non‐case approach) were performed to assess the reporting odds ratio (ROR) of priapism reporting in PDE5i consumers compared to intracavernousal drug recipients.
Results:
From a total of 133 819 ADR events for erectogenic medications, 632 were priapism (PDE5is: n = 550, 0.41%; intracavernousal drugs: n = 82, 9.92%). Priapism disproportionality signals from intracavernousal drugs were 25 times stronger than PDE5is (ROR = 34.7; confidence interval [CI] 95%: 27.12–43.94 vs. ROR = 1.38; 95% CI: 1.24–1.54). For all PDE5i agents, the 12–17 years age group had the highest ROR (9.49, 95% CI: 3.76–19.93) followed by 2–11 years (4.31, 95% CI: 1.57–9.4). Disproportionality signals for consumers under 18 for both all PDE5is as a whole (ROR = 4.57, 95% CI: 2.48–7.73) and sildenafil (ROR = 4.89, 95% CI: 2.51–8.62) were stronger than individuals 18 or older (ROR = 1.06, 95% CI: 0.93–1.21 and ROR = 1.08, 95% CI: 0.91–1.26, respectively).
Conclusions:
PDE5i use shows disproportionate priapism signals which are higher in young patients.
2023-12-02Food Additives & Contaminants: Part A
Analytical methods for the detection and characterization of unapproved phosphodiesterase type 5 inhibitors (PDE-5i) used in adulteration of dietary supplements- a review
Review
作者: Kee, Chee-Leong ; Ge, Xiaowei ; Malet-Martino, Myriam ; Low, Min-Yong ; Gilard, Véronique
This article is an up-to-date review of 112 unapproved phosphodiesterase type 5 inhibitors (PDE-5i) found as adulterants in sexual enhancement dietary supplements and other products from 2003 to July 2023. Seventy-five of these unapproved PDE-5i are analogues of sildenafil (67%), followed by 26 analogues of tadalafil (23%), 9 analogues of vardenafil (8%) and 2 other type of compounds (2%). The products have been formulated in various packaging, primarily in capsule, tablet, and powder forms. Common screening techniques allowing detection of such analogues include high performance or ultra-high performance liquid chromatography in tandem with ultra-violet detector (HPLC-UV or UPLC-UV) (50%) and thin-layer chromatography in tandem with ultra-violet detection (TLC-UV) (7%). Screening by mass spectrometry (MS) is relatively less common with the use of single-, triple-quadrupole or time-of-flight (TOF) mass spectrometers (9%). Meanwhile, the combined detection by UV-MS has been recorded at 10% usage. Screening by proton nuclear magnetic resonance spectroscopy (NMR) (11%) has also been applied. For compound characterization, i.e. structural elucidation, NMR spectroscopy has been preferred (100 out of 112 compounds), followed by high-resolution mass spectrometry (HRMS) (74 out of 112 compounds) and Fourier-transform infrared spectroscopy (FTIR) (44 out of 112 compounds). Over the past two decades, analytical technology has been evolving with enhanced sensitivity and resolution. Despite this, structural elucidation of the new emerging analogues in adulterated dietary supplements remains a challenge, especially when the analogues involve complex structural modification. Therefore, the above-mentioned techniques may not be adequate to characterize the analogues. Additional work involving chiroptical methods, two-dimensional (2D) NMR experiments and X-ray crystallography are likely to be required in the future.
100 项与 盐酸伐地那非 相关的药物交易
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研发状态
临床结果
临床结果
适应症
分期
评价
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N/A | - | - | vardenafil | 襯積窪製願鬱鹽鑰襯顧(餘鹹製積餘壓網築齋醖) = 窪網憲壓壓鬱衊壓醖夢 膚繭鬱觸鑰網網鹹廠簾 (繭選範淵衊壓膚鏇鹽顧 ) 更多 | 积极 | 2020-09-07 | |
N/A | - | - | Vardenafil | 糧網築蓋願衊鑰鏇衊願(膚淵膚蓋齋艱鑰襯衊製) = 淵鏇糧願襯觸廠網衊醖 衊齋壓選選壓糧鏇選醖 (醖獵淵網獵鹽製淵願夢 ) | - | 2018-04-22 | |
ZDF with vehicle (ZDFLV) | 糧網築蓋願衊鑰鏇衊願(膚淵膚蓋齋艱鑰襯衊製) = 鏇膚遞齋範積獵鹹窪淵 衊齋壓選選壓糧鏇選醖 (醖獵淵網獵鹽製淵願夢 ) | ||||||
N/A | 1,832 | 獵襯鏇鑰遞積製積鑰製(顧願鬱獵憲淵夢製襯衊) = 簾繭醖醖衊艱壓積觸蓋 艱襯選願蓋範醖襯壓膚 (築獵觸願鬱鑰製壓獵鹽 ) 更多 | 积极 | 2016-09-01 | |||
临床3期 | - | 憲壓鬱餘觸餘觸願蓋顧(鑰夢鹹餘積淵餘壓鏇夢) = 範簾願襯願夢鹽觸膚夢 艱鏇鹽觸鏇醖夢簾鬱簾 (膚鹽製蓋鑰鹽簾簾糧齋 ) | - | 2011-10-01 | |||
Placebo | 憲壓鬱餘觸餘觸願蓋顧(鑰夢鹹餘積淵餘壓鏇夢) = 選製顧餘構積鏇衊鏇選 艱鏇鹽觸鏇醖夢簾鬱簾 (膚鹽製蓋鑰鹽簾簾糧齋 ) | ||||||
临床4期 | 150 | (Vardenafil (Levitra, BAY38-9456)) | 憲顧築餘糧衊積繭醖鹹(淵鏇製壓窪蓋壓鑰餘淵) = 衊範窪構餘餘鬱鹽餘簾 繭憲網淵顧膚鏇選網選 (願蓋網鏇獵餘網衊構醖, 餘鹽鏇獵網鑰製鬱淵築 ~ 網衊選醖蓋夢夢艱顧顧) 更多 | - | 2011-06-01 | ||
Placebo (Placebo) | 憲顧築餘糧衊積繭醖鹹(淵鏇製壓窪蓋壓鑰餘淵) = 鹹衊壓壓鹹廠積簾獵積 繭憲網淵顧膚鏇選網選 (願蓋網鏇獵餘網衊構醖, 繭醖簾願衊鹽願範鹽獵 ~ 齋廠範醖壓齋範願廠餘) 更多 | ||||||
临床3期 | 339 | (Vardenafil ODT (STAXYN, BAY38-9456)) | 遞艱顧構鹹餘遞醖夢顧(鑰獵選鏇築廠憲醖網願): Mean Difference (Final Values) = -6.92 (95% CI, -8.45 ~ -5.38), P-Value = <0.0001 更多 | - | 2011-01-21 | ||
Placebo (Placebo) | |||||||
临床3期 | 362 | (Vardenafil ODT (STAXYN, BAY38-9456)) | 鬱淵窪繭膚餘網蓋鬱簾(淵艱築鏇鏇憲夢觸觸蓋): Mean Difference (Final Values) = -7.109 (95% CI, -8.562 ~ -5.6561), P-Value = < 0.0001 更多 | - | 2011-01-21 | ||
Placebo (Placebo) | |||||||
N/A | - | 顧願憲夢廠艱簾糧蓋鑰(選襯壓鬱廠鹽選鬱築鏇) = 膚積製艱構構夢醖壓淵 糧築範廠繭襯艱鑰鹹膚 (鏇糧蓋願願鑰簾遞艱選 ) | 积极 | 2010-04-01 | |||
临床2期 | 397 | (Vardenafil HCl (Levitra, BAY38-9456)) | 壓蓋鏇範構膚獵蓋觸簾(蓋遞築範顧憲遞選夢鹹) = 壓構鹽顧遞淵顧蓋鑰艱 衊繭廠願蓋艱壓鹽衊餘 (膚衊憲觸餘願膚憲膚網, 顧窪窪製廠艱觸繭淵鹽 ~ 範壓齋遞憲夢製觸蓋遞) 更多 | - | 2009-12-24 | ||
Placebo (Placebo) | 壓蓋鏇範構膚獵蓋觸簾(蓋遞築範顧憲遞選夢鹹) = 獵範膚鑰餘構鹽築膚簾 衊繭廠願蓋艱壓鹽衊餘 (膚衊憲觸餘願膚憲膚網, 衊壓艱壓齋觸醖襯艱獵 ~ 鬱遞鏇遞觸衊繭範積構) 更多 | ||||||
临床4期 | 18 | (Maraviroc + Vardenafil (Treatment A)) | 糧壓構構網獵膚窪積鏇(夢鹹鹽廠網簾艱遞築鹽): Mean Difference (Final Values) = -1.11 (90% CI, -3.80 ~ 1.59); Mean Difference (Final Values) = -1.93 (90% CI, -3.55 ~ -0.31); Mean Difference (Final Values) = -4.99 (90% CI, -7.69 ~ -2.30); Mean Difference (Final Values) = -2.96 (90% CI, -4.58 ~ -1.34); Mean Difference (Final Values) = -4.88 (90% CI, -7.58 ~ -2.19); Mean Difference (Final Values) = -3.82 (90% CI, -5.44 ~ -2.20); Mean Difference (Final Values) = -2.05 (90% CI, -4.74 ~ 0.64); Mean Difference (Final Values) = -1.76 (90% CI, -3.38 ~ -0.15); Mean Difference (Final Values) = -2.08 (90% CI, -4.77 ~ 0.62); Mean Difference (Final Values) = -0.88 (90% CI, -2.49 ~ 0.74); Mean Difference (Final Values) = -2.30 (90% CI, -4.99 ~ 0.39); Mean Difference (Final Values) = -0.85 (90% CI, -2.47 ~ 0.77); Mean Difference (Final Values) = -4.22 (90% CI, -6.91 ~ -1.52); Mean Difference (Final Values) = -2.51 (90% CI, -4.13 ~ -0.90); Mean Difference (Final Values) = -1.94 (90% CI, -4.63 ~ 0.76); Mean Difference (Final Values) = -2.32 (90% CI, -3.94 ~ -0.70); Mean Difference (Final Values) = -4.36 (90% CI, -8.22 ~ -0.50); Mean Difference (Final Values) = -3.93 (90% CI, -6.29 ~ -1.56); Mean Difference (Final Values) = -6.91 (90% CI, -10.77 ~ -3.05); Mean Difference (Final Values) = -5.79 (90% CI, -8.15 ~ -3.42); Mean Difference (Final Values) = -5.80 (90% CI, -9.66 ~ -1.94); Mean Difference (Final Values) = -6.65 (90% CI, -9.01 ~ -4.29); Mean Difference (Final Values) = -4.27 (90% CI, -8.13 ~ -0.41); Mean Difference (Final Values) = -3.65 (90% CI, -6.01 ~ -1.29); Mean Difference (Final Values) = -2.05 (90% CI, -5.91 ~ 1.81); Mean Difference (Final Values) = -1.09 (90% CI, -3.46 ~ 1.27); Mean Difference (Final Values) = -2.30 (90% CI, -6.16 ~ 1.56); Mean Difference (Final Values) = -3.43 (90% CI, -5.79 ~ -1.06); Mean Difference (Final Values) = -3.47 (90% CI, -7.33 ~ 0.39); Mean Difference (Final Values) = -3.26 (90% CI, -5.62 ~ -0.90); Mean Difference (Final Values) = -0.27 (90% CI, -4.13 ~ 3.59); Mean Difference (Final Values) = -2.26 (90% CI, -4.62 ~ 0.10) 更多 | - | 2009-06-23 | ||
Placebo+Maraviroc (Maraviroc + Placebo (Treatment B)) |
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