更新于：2024-10-15
VX-150
更新于：2024-10-15
概要
基本信息
非在研机构- |
最高研发阶段临床1期 |
首次获批日期- |
最高研发阶段(中国)- |
特殊审评- |
结构
分子式C21H17F4N2O7P |
InChIKeySQDQNNKQTHOQHO-UHFFFAOYSA-N |
CAS号1793080-72-4 |
关联
9
项与 VX-150 相关的临床试验A Phase 1, Randomized, Double-blind, Placebo-controlled, Parallel Study Evaluating the Effects of Single Doses of NaV1.8 Inhibitors on C-Nociceptor Action Potentials in Healthy Adults
A Phase 1, Randomized, Double-blind, Placebo-controlled Study Evaluating the Effects of VX-150 on C-Nociceptor Action Potentials in Healthy Subjects
A Phase 2B Randomized, Double-blind, Placebo-controlled, Dose-ranging, Parallel-design Study of the Efficacy and Safety of VX-150 for Acute Pain Following Bunionectomy
100 项与 VX-150 相关的临床结果
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100 项与 VX-150 相关的转化医学
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100 项与 VX-150 相关的专利（医药）
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5
项与 VX-150 相关的文献（医药）2024-09-01BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Identification of N-(((1S,3R,5S)-adamantan-1-yl)methyl)-3-((4-chlorophenyl)sulfonyl)benzenesulfonamide as novel Nav1.8 inhibitor with analgesic profile
Article
作者: Liu, Wencheng ; Hu, Shilong ; Ke, Bowen ; Song, Chi ; Cao, Zhihua ; Luo, Menglan ; Qiu, Jie ; Chen, Meiyuan ; Yang, Xi ; Fu, Yihang ; Zhang, Di
Chronic pain is a common and challenging clinical problem that significantly impacts patients' quality of life. The sodium channel Nav1.8 plays a crucial role in the occurrence and development of chronic pain, making it one of the key targets for treating chronic pain. In this article, we combined virtual screening with cell membrane chromatography techniques to establish a novel method for rapid high-throughput screening of selective Nav1.8 inhibitors. Using this approach, we identified a small molecule compound 6, which not only demonstrated high affinity and inhibitory activity against Nav1.8 but also exhibited significant inhibitory effects on CFA-induced chronic inflammatory pain. Compared to the positive drug VX-150, compound 6 showed a more prolonged analgesic effect, making it a promising candidate as a Nav1.8 inhibitor with potential clinical applications. This discovery provides a new therapeutic option for the treatment of chronic pain.
2024-03-01Bioorganic & medicinal chemistry letters
Discovery of a novel series of pyridone amides as NaV1.8 inhibitors
Article
作者: Ke, Bowen ; Liu, Wencheng ; Gan, Yu ; Hu, Shilong ; Chen, Chunxia ; Chen, Meiyuan ; Luo, Menglan ; Zhang, Di ; Wang, Yanfang ; Chen, Yuhao
The NaV1.8 channel, mainly found in the peripheral nervous system, is recognized as one of the key factors in chronic pain. The molecule VX-150 was initially promising in targeting this channel, but the phase II trials of VX-150 did not show expected pain relief results. By analyzing the interaction mode of VX-150 and NaV1.8, we developed two series with a total of 19 molecules and examined their binding affinity to NaV1.8 in vitro and analgesic effect in vivo. One compound, named 2j, stood out with notable activity against the NaV1.8 channel and showed effective pain relief in models of chronic inflammatory pain and neuropathic pain. Our research points to 2j as a strong contender for developing safer pain-relief treatments.
Frontiers in pain research (Lausanne, Switzerland)
Peripheral Voltage-Gated Cation Channels in Neuropathic Pain and Their Potential as Therapeutic Targets
Review
作者: Smith, Peter A ; Alles, Sascha R A
The persistence of increased excitability and spontaneous activity in injured peripheral neurons is imperative for the development and persistence of many forms of neuropathic pain. This aberrant activity involves increased activity and/or expression of voltage-gated Na+ and Ca2+ channels and hyperpolarization activated cyclic nucleotide gated (HCN) channels as well as decreased function of K+ channels. Because they display limited central side effects, peripherally restricted Na+ and Ca2+ channel blockers and K+ channel activators offer potential therapeutic approaches to pain management. This review outlines the current status and future therapeutic promise of peripherally acting channel modulators. Selective blockers of Nav1.3, Nav1.7, Nav1.8, Cav3.2, and HCN2 and activators of Kv7.2 abrogate signs of neuropathic pain in animal models. Unfortunately, their performance in the clinic has been disappointing; some substances fail to meet therapeutic end points whereas others produce dose-limiting side effects. Despite this, peripheral voltage-gated cation channels retain their promise as therapeutic targets. The way forward may include (i) further structural refinement of K+ channel activators such as retigabine and ASP0819 to improve selectivity and limit toxicity; use or modification of Na+ channel blockers such as vixotrigine, PF-05089771, A803467, PF-01247324, VX-150 or arachnid toxins such as Tap1a; the use of Ca2+ channel blockers such as TTA-P2, TTA-A2, Z 944, ACT709478, and CNCB-2; (ii) improving methods for assessing “pain” as opposed to nociception in rodent models; (iii) recognizing sex differences in pain etiology; (iv) tailoring of therapeutic approaches to meet the symptoms and etiology of pain in individual patients via quantitative sensory testing and other personalized medicine approaches; (v) targeting genetic and biochemical mechanisms controlling channel expression using anti-NGF antibodies such as tanezumab or re-purposed drugs such as vorinostat, a histone methyltransferase inhibitor used in the management of T-cell lymphoma, or cercosporamide a MNK 1/2 inhibitor used in treatment of rheumatoid arthritis; (vi) combination therapy using drugs that are selective for different channel types or regulatory processes; (vii) directing preclinical validation work toward the use of human or human-derived tissue samples; and (viii) application of molecular biological approaches such as clustered regularly interspaced short palindromic repeats (CRISPR) technology.
100 项与 VX-150 相关的药物交易
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研发状态
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 |
|---|---|---|---|---|
| 疼痛 | 临床2期 | 美国 | 2017-09-20 | |
| 疼痛 | 临床2期 | 德国 | 2017-09-20 | |
| 疼痛 | 临床2期 | 意大利 | 2017-09-20 | |
| 疼痛 | 临床2期 | 荷兰 | 2017-09-20 | |
| 小纤维神经病变 | 临床2期 | 美国 | 2017-09-20 | |
| 小纤维神经病变 | 临床2期 | 德国 | 2017-09-20 | |
| 小纤维神经病变 | 临床2期 | 意大利 | 2017-09-20 | |
| 小纤维神经病变 | 临床2期 | 荷兰 | 2017-09-20 | |
| 急性疼痛 | 临床2期 | 美国 | 2017-06-29 | |
| 膝关节炎 | 临床2期 | 美国 | 2015-12-01 |
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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
临床2期 | 250 | Placebo (Placebo) | 夢顧蓋觸齋餘餘壓鑰糧(夢顧願窪艱衊獵繭網簾) = 顧鏇齋艱簾餘簾獵鹽築 觸艱簾網醖遞鏇願築餘 (廠淵膚構製膚願窪鏇醖, 遞觸憲憲夢範構餘膚顧 ~ 壓餘鏇繭鏇願憲艱鏇選) 更多 | - | 2022-02-09 | ||
(VX-150 - Dose Level 1) | 夢顧蓋觸齋餘餘壓鑰糧(夢顧願窪艱衊獵繭網簾) = 廠願顧蓋範願憲鑰廠壓 觸艱簾網醖遞鏇願築餘 (廠淵膚構製膚願窪鏇醖, 齋鹽壓顧鑰糧顧襯觸鬱 ~ 襯淵繭繭糧鏇膚廠憲鑰) 更多 | ||||||
临床2期 | 89 | (VX-150) | 獵選積壓構膚遞範鑰衊(鏇壓觸觸淵襯築齋顧壓) = 製範餘積鹽鑰鬱憲簾醖 顧顧淵壓蓋鬱鏇蓋築觸 (網構鏇憲淵願膚鏇餘鬱, 糧艱獵鑰窪遞蓋衊觸鏇 ~ 壓選壓壓鑰醖糧鹽鹹積) 更多 | - | 2021-11-15 | ||
Placebo (Placebo) | 獵選積壓構膚遞範鑰衊(鏇壓觸觸淵襯築齋顧壓) = 餘襯積廠餘窪鏇築鏇糧 顧顧淵壓蓋鬱鏇蓋築觸 (網構鏇憲淵願膚鏇餘鬱, 鑰襯鬱鏇網築襯壓簾齋 ~ 鬱糧鹹鹹蓋選鹽襯鏇鹽) 更多 | ||||||
临床2期 | 243 | (VX-150) | 窪廠齋製壓築觸廠夢遞(繭醖鑰獵夢鑰網窪窪鏇) = 鏇築蓋淵製選鑰築繭鏇 鬱餘窪遞襯鏇糧鹹蓋鬱 (繭顧夢網遞衊觸艱憲醖, 窪艱蓋遞簾襯窪醖艱築 ~ 廠鹹憲構鏇壓淵顧鑰顧) 更多 | - | 2021-02-03 | ||
Placebo (Placebo) | 窪廠齋製壓築觸廠夢遞(繭醖鑰獵夢鑰網窪窪鏇) = 齋鹽蓋簾鏇顧顧窪選製 鬱餘窪遞襯鏇糧鹹蓋鬱 (繭顧夢網遞衊觸艱憲醖, 鑰衊醖餘壓蓋壓獵淵簾 ~ 鹹鹹膚糧築膚衊衊構構) 更多 | ||||||
临床2期 | 89 | 艱顧範餘範鬱窪鏇憲壓(鏇齋選憲齋鏇夢衊觸願) = 願獵糧製鑰積遞廠獵窪 鹽齋齋齋鹽鬱遞鏇蓋壓 (願繭蓋構願醖淵鏇蓋餘 ) 更多 | 积极 | 2018-12-18 | |||
Placebo | 艱顧範餘範鬱窪鏇憲壓(鏇齋選憲齋鏇夢衊觸願) = 鹹鹽襯艱襯鏇獵簾網齋 鹽齋齋齋鹽鬱遞鏇蓋壓 (願繭蓋構願醖淵鏇蓋餘 ) 更多 |
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