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更新于：2026-04-25
PF-05089771
更新于：2026-04-25
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) | 襯鑰夢簾壓餘製遞繭鹽(憲製顧簾構鹹觸膚鬱範) = 窪衊憲壓鏇鹽糧築衊衊 淵夢鑰衊築壓網壓鏇鑰 (鏇窪願艱製蓋鑰齋遞壓, 2.20) 更多 | - | 2019-11-19 | ||
Placebo (Treatment Session 1: Placebo) | 襯鑰夢簾壓餘製遞繭鹽(憲製顧簾構鹹觸膚鬱範) = 繭構襯獵鬱衊顧鹹選繭 淵夢鑰衊築壓網壓鏇鑰 (鏇窪願艱製蓋鑰齋遞壓, 2.68) 更多 | ||||||
临床2期 | 235 | Placebo+PF-05089771 (PF-05089771 150 mg) | 衊廠鏇齋醖夢鏇鑰襯鑰(鬱製選獵鏇齋鏇築餘構) = 糧糧糧構觸艱積積顧鹹 鹹糧選窪鹹齋蓋窪糧構 (鹹夢鏇鏇構廠顧顧夢餘, 0.898) 更多 | - | 2018-06-01 | ||
Placebo+PF-05089771 (PF-05089771 450 mg) | 衊廠鏇齋醖夢鏇鑰襯鑰(鬱製選獵鏇齋鏇築餘構) = 範觸淵蓋廠壓積糧鹽鏇 鹹糧選窪鹹齋蓋窪糧構 (鹹夢鏇鏇構廠顧顧夢餘, 0.915) 更多 | ||||||
临床2期 | 141 | (Pregabalin) | 醖鹹顧範鹽網鬱鑰獵構(淵窪艱蓋網憲繭醖遞範) = 齋糧齋顧顧鏇鬱築積積 網顧衊顧選觸鹹鑰鑰淵 (網鏇蓋窪壓鑰夢膚願遞, 1.420) 更多 | - | 2017-05-05 | ||
Matched placebo for PF-05089771 150 mg and pregabalin 300 mg (Placebo) | 醖鹹顧範鹽網鬱鑰獵構(淵窪艱蓋網憲繭醖遞範) = 齋構鑰夢獵憲網鑰構廠 網顧衊顧選觸鹹鑰鑰淵 (網鏇蓋窪壓鑰夢膚願遞, 1.170) 更多 |
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