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更新于：2026-04-28
E-6742
更新于：2026-04-28
概要
基本信息
药物类型 小分子化药 |
别名 E 6742 |
作用方式 拮抗剂 |
作用机制 TLR7拮抗剂(Toll样受体7拮抗剂)、TLR8拮抗剂(Toll样受体8拮抗剂) |
在研适应症 |
非在研适应症- |
原研机构 |
在研机构 |
非在研机构 |
最高研发阶段临床2期 |
首次获批日期- |
最高研发阶段(中国)临床2期 |
特殊审评- |
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关联
4
项与 E-6742 相关的临床试验NCT07515014
A Phase 2, Randomized, Double-Blind, Placebo-Controlled, Multicenter, Dose Response Study to Evaluate the Efficacy and Safety of E6742 in Subjects With Systemic Lupus Erythematosus
NCT05278663
A Randomized, Double-Blind, Placebo-Controlled, Multi-center, Multiple Ascending Dose Study to Assess the Safety, Tolerability, and Pharmacokinetics of E6742 in Systemic Lupus Erythematosus Patients
NCT04683185
A Randomized, Double-Blind, Placebo-Controlled, Multiple Ascending Dose Study to Assess the Safety, Tolerability, and Pharmacokinetics of E6742 in Japanese Healthy Adult Subjects
100 项与 E-6742 相关的临床结果
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100 项与 E-6742 相关的转化医学
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100 项与 E-6742 相关的专利（医药）
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4
项与 E-6742 相关的文献（医药）2024-09-01RMD Open
Safety, pharmacokinetics, biomarker response and efficacy of E6742: a dual antagonist of Toll-like receptors 7 and 8, in a first in patient, randomised, double-blind, phase I/II study in systemic lupus erythematosus
Article
作者: Yamamuro, Shintaro ; Kumanogoh, Atsushi ; Atsumi, Tatsuya ; Akira, Shizuo ; Tanaka, Yoshiya ; Ishii, Tomonori ; Tago, Fumitoshi ; Aoki, Mari
Objectives:
To evaluate the safety, tolerability, pharmacokinetics (PK), biomarker response and efficacy of E6742 in a phase I/II study in patients with systemic lupus erythematosus (SLE).
Methods:
Two sequential cohorts of patients with SLE were enrolled and randomised to 12 weeks of two times per day treatment with E6742 (100 or 200 mg; n=8 or 9) or placebo (n=9). The primary endpoint was safety, the secondary endpoints were PK and interferon gene signature (IGS), and the exploratory endpoints were efficacy and biomarker.
Results:
The proportion of patients with any treatment-emergent adverse events (TEAEs) was 58.8% in the E6742 group (37.5% (3/8 patients) for 100 mg; 77.8% (7/9 patients) for 200 mg) and 66.7% (6/9 patients) in the placebo group. No Common Terminology Criteria for Adverse Events≥Grade 3 TEAEs occurred. PK parameters were similar to these in previous phase I studies in healthy adults. The IGS and levels of proinflammatory cytokines after ex-vivo challenge with a Toll-like receptor 7/8 agonist were immediately decreased by E6742 treatment. The response rate of the British Isles Lupus Assessment Group-based Composite Lupus Assessment at week 12 was 37.5% (3/8 patients) for E6742 100 mg, 57.1% (4/7 patients) for E6742 200 mg and 33.3% (3/9 patients) for placebo group.
Conclusions:
E6742 had a favourable safety profile and was well tolerated, with suppression of IGS responses and preliminary efficacy signals in patients with SLE. These results provide the first clinical evidence to support E6742 in the treatment of SLE, and support larger, longer-term clinical trials.
Trial registration number:
NCT05278663.
2024-01-02Immunological medicine
A new therapeutic target for systemic lupus erythematosus: the current landscape for drug development of a toll-like receptor 7/8 antagonist through academia-industry-government collaboration
Review
作者: Tago, Fumitoshi ; Akira, Shizuo ; Tanaka, Yoshiya ; Yamakawa, Naoto ; Yagi, Takuya ; Aoki, Mari
Systemic Lupus Erythematosus (SLE) is an autoimmune disease characterized by inflammation in multiple organs. A few treatments for SLE currently exist, including antimalarials, glucocorticoids, immunosuppressants, and two recently approved antibody agents; however, an unmet medical need remains for SLE. In addition, developing new drugs targeting SLE is a challenge since no specific biomarkers exist for the prediction of disease progression or drug response. A new drug candidate, E6742, is a specific antagonist of the toll-like receptors 7/8. To address the challenges for drug development in SLE, the process of developing E6742 utilizes a unique system of the Japan Agency for Medical Research and Development (AMED), the Cyclic Innovation for Clinical Empowerment (CiCLE) program. In the CiCLE program, a Phase 1 study in healthy adults was completed (NCT04683185) and a Phase 1/2 study in patients with SLE is on-going (NCT05278663). One of the potential benefits of this program is to conduct academia-led clinical research to identify specific biomarkers for E6742 in parallel with clinical studies (UMIN000042037). The aim of this review is to present current progress within the strategic collaboration of the AMED CiCLE program that optimize clinical development for patients with SLE.
2023-10-01European journal of pharmacology
A novel Toll-like receptor 7/8–specific antagonist E6742 ameliorates clinically relevant disease parameters in murine models of lupus
Article
作者: Hawkins, Lynn ; Tago, Fumitoshi ; Ishizaka, Sally T ; Zhang, Zhikuan ; Chen, Qian ; Shirato, Manabu ; Yagi, Takuya ; Shimizu, Toshiyuki ; Sakaniwa, Kentaro
The sensing of self RNA by the endosomal Toll-like receptors (TLRs) 7 and 8 initiates pathogenic mechanisms underlying the autoimmune disease lupus. A blockade of the TLR7/8 signals may, therefore, be a novel therapeutic intervention for lupus. To test the hypothesis, a novel compound E6742 that blocks TLR7/8 activation was identified. The mode of action of E6742 was investigated by analysis of the tertiary structure of TLR7 and 8 in complex with E6742. The in vitro activities of the compound were examined in cellular systems and its therapeutic potential was evaluated in murine lupus models. Tertiary structures of the extracellular domain of TLR7 and 8 in complex with E6742 showed that E6742 binds specifically and non-covalently to the hydrophobic pocket located at the interface of TLR7 or TLR8 homodimers. E6742 potently and selectively inhibited several TLR7/8-mediated cytokine responses in human PBMC. In two mouse models of lupus, oral dosing of E6742 after the onset of disease suppressed increase in autoantibodies and blocked the advance of organ damage. Collectively, the data show that TLR7/8 activation contributes to disease progression and its blocking by E6742 has potential as a therapeutic intervention for lupus.
100 项与 E-6742 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 |
|---|---|---|---|---|
| 系统性红斑狼疮 | 临床2期 | 中国 | 2026-03-31 | |
| 系统性红斑狼疮 | 临床2期 | 日本 | 2026-03-31 |
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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1/2期 | 26 | 鬱獵積選憲衊膚鹽選遞(遞顧選廠鬱淵鑰襯遞憲) = 齋鏇鏇築淵壓夢獵獵範 範鬱繭顧積構鏇衊憲積 (願襯襯獵膚窪糧糧憲淵 ) 更多 | 积极 | 2024-11-10 | |||
鬱獵積選憲衊膚鹽選遞(遞顧選廠鬱淵鑰襯遞憲) = 鹽窪鬱鬱蓋餘膚簾積選 範鬱繭顧積構鏇衊憲積 (願襯襯獵膚窪糧糧憲淵 ) 更多 | |||||||
临床1/2期 | 系统性红斑狼疮 interferon gene signature (IGS) | proinflammatory cytokines | - | 獵齋廠壓艱範襯衊窪網(鏇餘壓顧鹹鬱製選選選) = immediately decreased by E6742 treatment 窪壓襯鏇願鹽遞窪餘襯 (餘襯鑰製鏇蓋壓積遞廠 ) | 积极 | 2024-09-01 | ||
临床1/2期 | 26 | 淵襯簾壓蓋築齋築鏇蓋(衊鬱願鑰膚艱鹹遞願選) = 憲齋衊獵齋簾獵襯築鹹 鹽繭選齋願膚蓋範餘願 (廠範憲鹽壓壓衊觸餘築 ) 更多 | 积极 | 2024-06-12 | |||
淵襯簾壓蓋築齋築鏇蓋(衊鬱願鑰膚艱鹹遞願選) = 淵淵衊艱餘網衊網糧積 鹽繭選齋願膚蓋範餘願 (廠範憲鹽壓壓衊觸餘築 ) 更多 |
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