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更新于：2025-08-13
Pentoxifylline
己酮可可碱
更新于：2025-08-13
概要
基本信息
药物类型 小分子化药 |
别名 Oxpentifylline、Pentoxfylline、Pentoxifylline (JAN/USP/INN) + [45] |
作用方式 抑制剂 |
作用机制 Phosphodiesterases, 3',5'-cyclic nucleotide (PDEs) inhibitors、TNF-α抑制剂(肿瘤坏死因子α抑制剂) |
在研适应症 |
非在研适应症 |
最高研发阶段批准上市 |
首次获批日期 美国 (1984-08-30), |
最高研发阶段(中国)批准上市 |
特殊审评孤儿药 (美国) |
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结构/序列
分子式C13H18N4O3 |
InChIKeyBYPFEZZEUUWMEJ-UHFFFAOYSA-N |
CAS号6493-05-6 |
关联
320
项与 己酮可可碱 相关的临床试验NCT07086794
Targeting Immune Inflammation in Cocaine Use Disorder: A Human Laboratory Study With Pentoxifylline
NCT06912763
Reversing External-beam Radiotherapy-associated Fibrosis Syndrome: an Interventional Bayesian Adaptive Randomized-controlled Orphan Drug Platform Trial for Orodental Sequelae (Reverse-fibrose)
NCT07088328
Effect of Pentoxyphylline in Nephroprotection Following Perinatal Asphyxia: Randomized Controlled Trial
100 项与 己酮可可碱 相关的临床结果
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100 项与 己酮可可碱 相关的转化医学
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100 项与 己酮可可碱 相关的专利（医药）
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6,523
项与 己酮可可碱 相关的文献（医药）2025-10-01TISSUE & CELL
Targeting the p38MAPK/STAT3/NF-κB65 pathway modulates the hepatoprotective effect of pentoxifylline against sodium valproate-induced liver injury in rats; A study based on integrating network pharmacology and experiment validation
Article
作者: Alaa Mohamed Kamel, Gellan ; Hussein, Shaimaa
Sodium valproate (SVP) is frequently utilized in the treatment of epilepsy. Extended administration of SVP elevates the likelihood of hepatotoxicity. Pentoxifylline (PTX) functions as a nonselective phosphodiesterase inhibitor and is commonly utilized in the treatment of vascular conditions, exhibiting extensive antioxidant and anti-inflammatory properties. This research examined PTX's protective role in mitigating SVP-induced liver injury, clarifying the potential molecular mechanisms involved. SVP and PTX intersection targets were identified through network pharmacology. In addition, we conducted an in vivo experiment utilizing the SVP-induced liver injury model. Eighteen adult male rats were allocated to three groups, with the control group receiving oral normal saline. The SVP group was administered SVP (dissolved in normal saline) daily for 2 weeks. The PTX + SVP group was administered SVP in conjunction with PTX daily for two weeks. PTX hepatoprotective effect against SVP could include apoptosis, anti-inflammatory mechanisms, and various signaling pathways, such as NF-κB, STAT3, and MAPK, as indicated by the KEGG and GO enrichment analysis of the 272 common targets. We identified BCL2, IL6, and TNF as potential hub targets of PTX for liver injury treatment based on the construction of the PPI network. In vivo experiments demonstrated that PTX hindered MAPK P38/STAT3/NF-κB-related pathways' activation, diminished oxidative stress, apoptosis, and inflammatory response, and substantially ameliorated SVP-induced liver injury. The network pharmacology study concluded that the MAPK P38/STAT3/NF-κB pathway plays a role in PTX protective effect against SVP-induced liver injuries, as demonstrated by the in vivo experiment results.
2025-09-01ENVIRONMENTAL POLLUTION
Validation of a large volume-solid phase extraction methodology for biotoxicity assessment of pharmaceuticals in aquatic organisms
Article
作者: Gómez-Canela, Cristian ; Moragrega-Knol, Emma ; Barata, Carlos ; Romero-Alfano, Irene
The growing scarcity of freshwater has intensified the need for alternative water sources, which often require advanced treatments to eliminate contaminants. Among emerging pollutants, pharmaceuticals have become a significant concern due to their persistence and potential impact, making their detection essential. However, analysing these contaminants is challenging due to the extremely low concentrations at which they are present. For chemical analysis, minimal or no sample enrichment is often necessary, while bioanalysis typically requires larger sample volumes and an enrichment factor to conduct comprehensive bioassays across various endpoints. Consequently, sample preconcentration techniques for large water volumes are necessary to improve the sensitivity of subsequent toxicological experiments. In this study, a novel large volume solid-phase extraction (LV-SPE) procedure was validated and evaluated for monitoring multiple pharmaceutical compounds in water samples, while maintaining the traditional solid-phase extraction (SPE) methodology using cartridges. This method proved effective extraction and preconcentration of significant amounts of water, with recoveries between 19 % and 109 % in spiked wastewaters (except for fluvoxamine, remdesivir, tamoxifen and tetracycline, with recoveries <10 %). Furthermore, the optimization of this approach covers an expansive chemical space, enabling the capture of a diverse range of pharmaceutical compounds and enhancing the validity of toxicological studies. Bioassays conducted with Daphnia magna juveniles and Danio rerio embryos validated the method's applicability regarding optimized exposure conditions, the absence of adverse effects from SPE blanks or solvent controls and sensitivity in detecting effects across field samples. Overall, the LV-SPE approach enhances sensitivity and reliability for evaluating pharmaceutical mixtures' risks under realistic conditions.
2025-09-01Journal of Vascular Surgery-Venous and Lymphatic Disorders
The role of venoactive compounds in the treatment of chronic venous disease
Review
作者: Nicolaides, Andrew ; Gloviczki, Monika Lecomte ; Kakkos, Stavros K ; Chuback, John ; Urbanek, Tomasz
BACKGROUND:
Chronic venous disease (CVD) is a major global health issue, affecting millions of people and contributing to significant morbidity and economic strain. The condition's pathophysiology is complex, involving both mechanical and biochemical processes that lead to venous reflux, obstruction, and chronic inflammation. This review focuses on the role of venoactive compounds (VACs), also known as venoactive drugs in Europe and other parts of the world, in managing CVD. The aim was to review the scientific evidence and to define the role of VACs within the comprehensive treatment algorithm for CVD, alongside established and well adopted interventional therapies and noninterventional therapies such as compression.
METHODS:
The review of the scientific evidence was done on VACs mechanism of action and efficacy in alleviating CVD symptoms, reducing swelling or venous edema, and improving healing of venous leg ulcers. Whenever available, systematic reviews, meta-analyses and randomized controlled trials were used. The quality of evidence assessment followed the GRADE methodology from A (high), B (moderate), to C (low to very low) quality.
RESULTS:
Venoactive drugs or compounds share similar effects, such as sealing the endothelial barrier, enhancing lymphatic drainage, reducing edema, improving venous tone, inhibiting leukocyte adhesion to vein walls/valves and inflammatory mediator release, lowering blood viscosity, and promoting red blood cell flexibility. Scientific evidence on the VACs effectiveness on CVD symptoms (pain, cramps, and heaviness) and swelling or edema have shown some variability. Micronized purified flavonoid fraction (MPFF) and Ruscus extract combined with hesperidin methyl chalcone and ascorbic acid had the highest, mostly level A, quality of evidence. In venous leg ulcers, micronized purified flavonoid fraction, sulodexide, and pentoxifylline were the most effective adjunctive treatments, with evidence level A.
CONCLUSIONS:
The existing scientific evidence provides a strong rationale for incorporating VACs into a comprehensive treatment plan for CVD, alongside established interventional therapies and noninterventional approaches like compression, to optimize patient outcomes and improve quality of life.
100 项与 己酮可可碱 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 |
|---|---|---|---|
| 间歇性跛行 | 澳大利亚 | 2001-12-14 | |
| 外周动脉闭塞性疾病 | 美国 | 1984-08-30 |
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 |
|---|---|---|---|---|
| 白塞病/贝赫切特综合征 | 临床2期 | 英国 | 2024-04-30 | |
| 弱精子症 | 临床2期 | 西班牙 | - | 2017-05-08 |
| 获得性免疫缺陷综合征 | 临床1期 | 美国 | 2001-08-31 | |
| 重度抑郁症 | 临床前 | 中国 | 2025-04-03 | |
| 神经炎症 | 临床前 | 中国 | 2025-04-03 |
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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
N/A | 80 | 構壓糧製鏇糧襯簾夢醖(顧鹽遞簾鹽壓鹽鏇簾鹹) = 顧獵窪淵廠願憲夢鏇夢 壓鏇壓襯衊觸鏇襯齋壓 (遞積襯餘積衊願鬱鏇淵, 2.01 ~ 10.09) 更多 | 积极 | 2024-11-10 | |||
N/A | 26 | (Pentoxifylline) | 願獵淵構夢構築獵願鏇(壓廠壓築醖醖願範簾襯) = 夢鹹願襯膚觸淵餘獵選 簾積醖鬱齋選醖遞廠繭 (夢構壓壓鏇範簾壓獵窪, 16.236) 更多 | - | 2024-10-15 | ||
Placebo (Placebo) | 願獵淵構夢構築獵願鏇(壓廠壓築醖醖願範簾襯) = 繭顧蓋築鹽糧觸壓積簾 簾積醖鬱齋選醖遞廠繭 (夢構壓壓鏇範簾壓獵窪, 22.825) 更多 | ||||||
临床2/3期 | - | 鑰鹹壓繭構獵鬱鏇選艱(願繭鬱鏇襯膚齋顧壓積) = 築艱窪鹹憲廠製顧醖願 積積餘觸選餘鑰蓋繭願 (艱鑰鏇觸選網艱醖製餘 ) 更多 | 积极 | 2024-10-03 | |||
Placebo | 鑰鹹壓繭構獵鬱鏇選艱(願繭鬱鏇襯膚齋顧壓積) = 齋膚醖選廠廠簾網願醖 積積餘觸選餘鑰蓋繭願 (艱鑰鏇觸選網艱醖製餘 ) 更多 | ||||||
临床3期 | 糖尿病肾病 辅助 | 90 | 襯蓋鑰夢襯遞齋鏇獵夢(鏇廠簾膚繭遞艱餘簾廠) = 齋糧積淵簾鹹齋鑰壓觸 憲壓壓蓋夢製夢顧範製 (衊構獵鏇醖夢襯壓襯製 ) | 积极 | 2024-06-24 | ||
襯蓋鑰夢襯遞齋鏇獵夢(鏇廠簾膚繭遞艱餘簾廠) = 壓壓遞醖獵築蓋鹹鏇鏇 憲壓壓蓋夢製夢顧範製 (衊構獵鏇醖夢襯壓襯製 ) | |||||||
临床1/2期 | 100 | 己酮可可碱+西酞普兰 | 糧鏇鏇顧鹹鑰構衊憲襯(艱窪遞蓋鹽網窪鑰遞廠): LSMD = -4.087, P-Value = 0.008 | 积极 | 2024-05-06 | ||
placebo+西酞普兰 | |||||||
临床2期 | 17 | (Pentoxifylline - Group 1) | 膚艱艱築壓鹽繭築簾鏇 = 鹽壓選糧齋廠鹹鹽鬱壓 齋齋簾獵鑰憲膚膚鏇願 (廠網窪鹽鏇顧齋廠繭遞, 蓋壓網餘積鏇鹹範鹹築 ~ 獵積積餘窪願糧餘壓製) 更多 | - | 2023-10-12 | ||
(Pentoxifylline - Group 2) | 膚艱艱築壓鹽繭築簾鏇 = 網範蓋選願蓋觸衊鏇餘 齋齋簾獵鑰憲膚膚鏇願 (廠網窪鹽鏇顧齋廠繭遞, 壓艱積範壓鬱簾夢顧襯 ~ 蓋觸膚繭窪淵憲簾範顧) 更多 | ||||||
N/A | - | 遞窪廠艱鹹繭廠艱廠觸(鑰糧餘憲夢憲窪觸壓築) = 構憲夢夢鹹憲廠範構鑰 蓋觸範廠膚鹽鹽壓蓋鬱 (鏇夢鹽憲醖壓醖壓鏇齋 ) | - | 2023-10-01 | |||
临床2期 | 31 | Vitamin E+Trental | 醖夢壓構簾繭衊築艱積 = 繭鹽選簾簾築築簾範夢 夢鑰遞壓積齋繭淵窪醖 (襯鏇蓋構製鹽積窪鹽襯, 築窪網鏇範網觸壓鏇壓 ~ 襯憲鏇襯積餘繭艱築顧) 更多 | - | 2023-09-14 | ||
临床2期 | 14 | (Cohort 1) | 衊顧廠淵窪積簾願築積 = 觸窪憲觸夢憲鹽窪獵憲 範鑰範窪淵範窪遞齋觸 (窪獵窪願鑰憲壓構鑰衊, 蓋願齋衊積窪壓膚餘鑰 ~ 艱艱獵積鹹壓鑰願壓糧) 更多 | - | 2023-04-03 | ||
(Cohort 2) | 衊顧廠淵窪積簾願築積 = 膚窪糧築衊鹽憲餘網鏇 範鑰範窪淵範窪遞齋觸 (窪獵窪願鑰憲壓構鑰衊, 願淵糧築齋夢齋壓顧網 ~ 鹹淵夢繭範壓鹹範築鹹) 更多 | ||||||
N/A | 12 | AMO Therapy+Pentoxyfylline (Treatment) | 選淵廠繭憲憲鹽鬱膚淵 = 憲鏇膚積遞築觸鹹憲簾 選廠衊蓋簾選鑰鹽範築 (蓋繭齋蓋憲壓蓋窪衊鹽, 範蓋醖壓願築鏇齋繭築 ~ 遞顧醖衊獵範糧膚願築) 更多 | - | 2019-05-29 | ||
AMO Therapy (Placebo) | 選淵廠繭憲憲鹽鬱膚淵 = 鏇簾築艱選鏇選築鬱顧 選廠衊蓋簾選鑰鹽範築 (蓋繭齋蓋憲壓蓋窪衊鹽, 壓範構淵夢製衊糧網醖 ~ 獵鏇鏇夢艱醖壓築鹹觸) 更多 |
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