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更新于：2026-04-17
PF-05089771
更新于：2026-04-17
概要
基本信息
原研机构 |
在研机构- |
权益机构- |
最高研发阶段终止临床2期 |
首次获批日期- |
最高研发阶段(中国)- |
特殊审评- |
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结构/序列
分子式C18H12Cl2FN5O3S2 |
InChIKeyZYSCOUXLBXGGIM-UHFFFAOYSA-N |
CAS号1235403-62-9 |
关联
14
项与 PF-05089771 相关的临床试验NCT05935280
Human Cold Pain - a Single-group, Randomized, Placebo-controlled, Adaptive, Factorial Crossover Trial
NCT02349607
A Double Blind, Double Dummy, Randomized, Placebo-controlled, 5 Period Cross-over Study To Examine The Effect Of Pf-05089771 Alone And In Combination With Pregabalin On Evoked Pain Endpoints In Healthy Volunteers Using Pregabalin And Ibuprofen As Positive Controls
NCT02215252
A Randomized Double Blind Placebo And Active Controlled Parallel Group Phase 2 Study To Evaluate PF-05089771 As A Monotherapy And As An Add-on To Pregabalin For The Treatment Of Painful Diabetic Peripheral Neuropathy
100 项与 PF-05089771 相关的临床结果
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100 项与 PF-05089771 相关的转化医学
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100 项与 PF-05089771 相关的专利（医药）
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48
项与 PF-05089771 相关的文献（医药）2026-03-01PAIN
Intrathecal administration of the Nav1.7 inhibitor PF-05089771 produces rapid and side-effect-free analgesia in mice
Article
Abstract:
Nav1.7 has emerged as a promising target for developing novel analgesics that avoid central side effects, yet clinical trials involving systemically administered Nav1.7 inhibitors have thus far yielded disappointing outcomes. In this study, we explored whether delivering PF-05089771—a highly selective Nav1.7 inhibitor previously tested in clinical settings—directly into the intrathecal space could elicit potent analgesic effects. We assessed pain responses using a range of behavioral assays, including the Hargreaves, hot plate, von Frey hair, and Randall-Selitto tests, while evaluating motor coordination and gastrointestinal transit through the rotarod test and a charcoal meal gavage method, respectively. Intrathecal administration of PF-05089771 produced rapid (within 15 minutes) and long-lasting (>4 hours) analgesia across multiple pain models, including nociceptive, inflammatory, neuropathic, and morphine-tolerant pain, as well as both acute and chronic itch. However, no significant effect was observed in a visceral pain model. The analgesic effects were abolished by naloxone pretreatment, implicating endogenous opioid signaling in the mechanism of action. Importantly, repeated intrathecal injections did not lead to analgesic tolerance, and no adverse effects on motor function or gastrointestinal motility were detected. These results indicate that changing the delivery route of Nav1.7 inhibitors may overcome limitations seen with systemic administration and highlight the potential of intrathecal PF-05089771 as a powerful and well-tolerated analgesic.
2025-12-01INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
Evaluating the ligands' potency to modulate the fast inactivation of voltage-gated sodium channel
Article
作者: Jankowska, Milena ; Nowak, Wiesław ; Niklas, Beata ; Walczewska-Szewc, Katarzyna ; Lapied, Bruno
Electrical impulse transmission along the nerve fiber in the form of the action potential is possible due to fast conformational changes of voltage-gated sodium channels (Nav) that control the sodium ions flow into the cell. The transition between functional states, called the gating mechanism, can be modulated by natural toxins and drugs. Here, we propose to use steered molecular dynamics (SMD) to investigate the ability of various ligands to impact the gating of P. americana cockroach Nav. By calculating mechanical forces required to relocate the inactivation particle to its binding pocket or to dislocate it, we assessed ligands' efficacy in trapping a channel in a given state (open or fast inactivated). Importantly, we showed that sulfonamide PF-05089771 and phospholipid PIP2 act as insect Nav channels inhibitors. We confirmed the ligands' action by electrophysiological measurements of their ability to modulate the neural activity. Our approach, applied here on a cockroach channel, can be used in any other Nav, i.g, as a step in computational-based drug screening to evaluate new drug candidates.
2025-10-01Journal of Neural Engineering
Co-cultured sensory neuron classification using extracellular electrophysiology and machine learning approaches for enhancing analgesic screening
Article
作者: Somers, Alexander ; Black, Bryan James
Abstract:
Objective.
Chronic pain affects over 20% of the adult population in the United States, posing a substantial personal as well as economic burden and contributing to the ongoing opioid crisis. Effective, non-addictive chronic pain treatments are urgently needed. Traditional drug discovery methods have failed to identify novel, non-addictive compounds, highlighting the need for alternative approaches such as phenotypic screening. Our lab developed a phenotypic screening assay using extracellular electrophysiological recordings from co-cultures of human induced pluripotent stem cell sensory neurons and glia. This study aimed to identify responsive neuronal subtypes within these presumptively heterogeneous cultures.
Approach.
We induced an inflammation-like state using tumor necrosis factor alpha and evaluated acute responses to nociceptor agonist capsaicin, which targets transient receptor potential vanilloid-1. By employing unsupervised learning, we labeled responsive cells based on changes in mean firing rates (MFR). We then used the labeled cells’ baseline activity to train and validate five classifiers
. Main results.
None of the classifiers outperformed the others in regards to accuracy. Nonetheless, an RUS-boosted ensemble of decision trees achieved an AUC-ROC of 0.877 classifying nociceptors in an unseen labeled culture.
Significance
. The notable accuracy suggests that machine learning techniques could be employed to enhance microelectrode array-based neuronal phenotypic assays as readouts (e.g. MFR) can be weighted based on target cell type (e.g. nociceptors).
100 项与 PF-05089771 相关的药物交易
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外链
| KEGG | Wiki | ATC | Drug Bank |
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| - | PF-05089771 | - |
研发状态
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 糖尿病周围神经性疼痛 | 临床2期 | 美国 | 2014-11-10 | |
| 红斑性肢痛症 | 临床2期 | 美国 | 2012-10-22 | |
| 术后疼痛 | 临床2期 | 美国 | 2011-12-12 | |
| 牙痛 | 临床2期 | 美国 | - | |
| 膝关节炎 | 临床1期 | 比利时 | 2012-01-01 | |
| 疼痛 | 临床1期 | 比利时 | 2010-12-01 |
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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 | 5 | (Treatment Session 1: PF-05089771 1600 mg) | 鏇選鹽壓積觸膚鏇遞築(膚鬱鬱憲憲鏇簾憲觸選) = 夢窪構蓋鬱糧壓簾製獵 窪醖窪製鑰憲選選鹽膚 (廠艱蓋鹽襯廠艱衊廠淵, 2.20) 更多 | - | 2019-11-19 | ||
Placebo (Treatment Session 1: Placebo) | 鏇選鹽壓積觸膚鏇遞築(膚鬱鬱憲憲鏇簾憲觸選) = 夢繭製構憲齋築構鏇遞 窪醖窪製鑰憲選選鹽膚 (廠艱蓋鹽襯廠艱衊廠淵, 2.68) 更多 | ||||||
临床2期 | 235 | Placebo+PF-05089771 (PF-05089771 150 mg) | 網願窪築鏇窪範願齋鏇(壓膚遞膚製淵夢窪夢鏇) = 簾壓顧繭鑰獵膚齋蓋壓 憲選鬱糧膚膚襯獵蓋網 (鹽範鹽範獵蓋顧壓廠窪, 0.898) 更多 | - | 2018-06-01 | ||
Placebo+PF-05089771 (PF-05089771 450 mg) | 網願窪築鏇窪範願齋鏇(壓膚遞膚製淵夢窪夢鏇) = 製艱繭衊襯壓淵廠艱醖 憲選鬱糧膚膚襯獵蓋網 (鹽範鹽範獵蓋顧壓廠窪, 0.915) 更多 | ||||||
临床2期 | 141 | (Pregabalin) | 襯鹹衊壓築齋夢獵夢繭(築廠糧壓蓋醖願艱鏇積) = 淵襯夢鑰簾觸艱鹹網願 衊壓夢鑰憲遞窪範餘築 (廠選糧壓壓遞糧網顧壓, 1.420) 更多 | - | 2017-05-05 | ||
Matched placebo for PF-05089771 150 mg and pregabalin 300 mg (Placebo) | 襯鹹衊壓築齋夢獵夢繭(築廠糧壓蓋醖願艱鏇積) = 觸廠鬱齋獵膚醖憲鬱鹹 衊壓夢鑰憲遞窪範餘築 (廠選糧壓壓遞糧網顧壓, 1.170) 更多 |
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