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更新于：2026-03-12
Tetrodotoxin
替曲朵辛
更新于：2026-03-12
概要
基本信息
非在研机构 |
最高研发阶段临床3期 |
首次获批日期- |
最高研发阶段(中国)临床2期 |
特殊审评快速通道 (美国) |
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结构/序列
分子式C11H17N3O8 |
InChIKeyCFMYXEVWODSLAX-QOZOJKKESA-N |
CAS号4368-28-9 |
关联
13
项与 替曲朵辛 相关的临床试验NCT06848348
A Randomized, Double-Blind, Placebo Controlled, Multicenter, Efficacy and Safety Study of Halneuron in the Treatment of Chemotherapy-Induced Neuropathic Pain
CTIS2022-500318-24-00
Evaluation of quantitative sensory testing (QST) using subcutaneous administration of single escalating doses of halneuron® (tetrodotoxin (TTX)) for injection in healthy volunteers
NCT05359133
A Randomized, Double-Blind, Placebo Controlled, Multicenter, Efficacy and Safety Trial of Single Cycle Tetrodotoxin in the Treatment of Chemotherapy Induced Neuropathic Pain
100 项与 替曲朵辛 相关的临床结果
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100 项与 替曲朵辛 相关的转化医学
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100 项与 替曲朵辛 相关的专利（医药）
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15,760
项与 替曲朵辛 相关的文献（医药）2026-04-01TOXICON
Tetrodotoxin in diet items of highly toxic ribbon worm Cephalothrix cf. simula (Palaeonemertea, Nemertea)
Article
作者: Malykin, G V ; Kuznetsov, V G ; Magarlamov, T Yu ; Puzanov, M S ; Velansky, P V
We, for the first time, have carried out a search for tetrodotoxin and its analogues (TTXs) in extracts of various animals being potential diet items for highly toxic nemerteans Cephalothrix cf. simula using high-performance liquid chromatography with tandem mass spectrometry (HPLC-MS/MS). We have screened TTXs in a total of 57 specimens from 2 classes. Рresence of TTX from five polychaetes species belonging to three families was shown. We here discuss the role of diet items as a source of TTXs for carnivorous TTX-bearing animals.
2026-03-10PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
Extended local anesthesia enabled by flavonoid permeation enhancers
Article
作者: Ma, Xiaojing ; Xue, Tianrui ; Wang, Yuan ; Han, Yiyuan ; Kohane, Daniel S. ; Bean, Bruce P. ; Torre, Matthew ; Jo, Sooyeon ; Fujita, Akie
Site 1 sodium channel blockers (S1SCBs), such as tetrodotoxin (TTX) and neosaxitoxin, are ultrapotent local anesthetics with low tissue toxicity. Their duration of action is relatively brief, but increasing the dose can lead to systemic toxicity. Here, we report that selected flavonoids—puerarin (PUE), naringenin, and kaempferol—prolong nerve block from S1SCBs 4- to 25-fold. Using both tympanic membrane (TM) permeation and sciatic nerve fluorescence distribution models, we demonstrate the flavonoids increase drug penetration across biological barriers (the TM and the barriers in and around nerve), suggesting that they act as chemical permeation enhancers (CPEs). Importantly, flavonoids exhibited minimal tissue toxicity compared to conventional CPEs. Coencapsulation of TTX and PUE into a liposomal delivery system further prolonged local anesthesia to over 25 d from a single injection. These findings establish flavonoid compounds as a safe class of CPEs and provide a platform of long-acting, nonopioid pain therapies. Flavonoids may be attractive alternatives to conventional CPEs in biomedical applications.
2026-02-27JOURNAL OF NATURAL PRODUCTS
Identification of Deoxy- and
epi
-Tetrodotoxin Analogues from the Newt
Cynops ensicauda popei
Suggests Stepwise Oxidation in Terrestrial Tetrodotoxin Biosynthesis
Article
作者: Horie, Shugo ; Hanifin, Charles T. ; Cho, Yuko ; Konoki, Keiichi ; Yotsu-Yamashita, Mari ; Kudo, Yuta
Tetrodotoxin (TTX, 1) is a potent neurotoxin that selectively blocks voltage-gated sodium channels and occurs in various marine and terrestrial organisms, yet its biosynthetic pathway remains unresolved. In this study, five deoxy-type TTX analogues were identified from the toxic newt Cynops ensicauda popei. The structures of four analogues, 6-epi-11-deoxyTTX (2), 8-epi-6-deoxyTTX (3), 1-hydroxy-8-epi-6,11-dideoxyTTX (4), and 1-hydroxy-4,9-anhydro-8-epi-10-hemiketal-5,6,11-trideoxyTTX (5), were elucidated by NMR spectroscopy, and an additional natural TTX analogue, 8-epi-6,11-dideoxyTTX (6), was characterized by high-resolution LCMS/MS. The structural features of these analogues suggest that stepwise oxidation at C-6 and C-11 occurs after formation of a TTX- or 10-hemiketal-type skeleton. Although this oxidative logic parallels that proposed for marine TTX-producing organisms, the analogue profile in newts is clearly distinct from that of marine organisms and is characterized by the presence of deoxy analogues in the 6-epi and 8-epi forms. These findings indicate that, although late-stage oxidative steps in TTX biosynthesis may be conserved, structural diversification has proceeded differently in terrestrial and marine systems, reflecting divergence in their biosynthetic pathways. This study provides insight into stepwise oxidation processes potentially involved in terrestrial TTX biosynthesis. A cell-based assay showed that 6-epi-11-deoxyTTX (2) retains voltage-gated sodium channel inhibitory activity, consistent with previously reported structure-activity trends.
100 项与 替曲朵辛 相关的药物交易
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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 |
|---|---|---|---|---|
| 肿瘤 | 临床3期 | 加拿大 | 2008-04-01 | |
| 癌症疼痛 | 临床3期 | 加拿大 | 2008-04-01 | |
| 神经痛 | 临床2期 | 美国 | 2025-02-21 | |
| 海洛因依赖 | 临床2期 | 中国 | 2015-02-05 | |
| 海洛因戒断 | 临床2期 | 中国 | 2015-02-05 | |
| 镇痛 | 临床2期 | 中国 | 2014-05-07 | |
| 阿片相关性障碍 | 临床2期 | 加拿大 | - | |
| 中毒 | 临床2期 | 中国 | - | |
| 麻醉 | 临床前 | 加拿大 | - |
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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 | 97 | 鏇製鹽淵繭糧觸夢構廠(構艱襯艱網廠鑰壓遞鑰) = demonstrating separation from placebo 壓築淵衊觸糧願選顧網 (鏇艱構夢醖醖憲觸膚糧 ) | 积极 | 2025-12-22 | |||
Placebo | |||||||
临床2期 | 125 | Placebo (Placebo (Twice Daily)) | 膚齋鬱憲窪蓋憲觸餘蓋(簾淵鏇鏇獵夢遞構窪衊) = 獵蓋鹽顧範齋鑰製糧膚 構襯衊淵餘襯窪範鏇遞 (築廠繭鑰構淵鑰糧鹹範, 1.4832) 更多 | - | 2018-10-30 | ||
(Low Dose Tetrodotoxin (Twice Daily)) | 膚齋鬱憲窪蓋憲觸餘蓋(簾淵鏇鏇獵夢遞構窪衊) = 製廠製壓繭糧繭獵壓遞 構襯衊淵餘襯窪範鏇遞 (築廠繭鑰構淵鑰糧鹹範, 1.3312) 更多 | ||||||
临床3期 | 165 | 獵鏇積範鏇艱壓膚襯築(衊製蓋餘鑰積襯窪憲構) = 獵膚襯鬱築製夢觸廠壓 壓鹽鏇獵餘簾淵遞選繭 (襯遞廠淵壓鹽壓餘範醖 ) 更多 | 积极 | 2017-01-01 | |||
Placebo | 廠構獵願齋膚膚積積鏇(窪簾餘廠餘餘積積醖壓) = 憲積淵鑰獵顧鏇淵網鑰 繭鏇築鹽糧醖鑰襯鬱願 (鬱夢範遞鑰繭範襯築淵 ) |
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