预约演示
更新于：2025-11-12
Sitmutolimod
更新于：2025-11-12
概要
基本信息
原研机构 |
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)- |
特殊审评快速通道 (美国) |
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结构/序列
分子式C24H26N4O3 |
InChIKeyZAEIHDZLLJCJFP-UHFFFAOYSA-N |
CAS号1020634-41-6 |
Sequence Code 453693544
来源: *****
关联
11
项与 Sitmutolimod 相关的临床试验NCT06510504
A Phase 3, Randomized, Double-blind, 2-arm, Parallel-group, Placebo-controlled Study to Evaluate the Efficacy and Safety of BNC210 for the Acute, As-needed Treatment of Anxiety in Adults With Social Anxiety Disorder
NCT05193409
A Phase 2, Randomized, Double-blind Study to Evaluate the Efficacy and Safety of BNC210 Compared to Placebo for the Acute Treatment of Social Anxiety Disorder
NCT04951076
A Phase 2b, Randomized, Double Blind, Two Arm Study to Investigate the Effects of BNC210 Tablet Formulation Compared to Placebo in Adults With Post-Traumatic Stress Disorder (PTSD)
100 项与 Sitmutolimod 相关的临床结果
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100 项与 Sitmutolimod 相关的转化医学
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100 项与 Sitmutolimod 相关的专利（医药）
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9
项与 Sitmutolimod 相关的文献（医药）2025-04-01PSYCHIATRY RESEARCH
A phase 2, placebo-controlled study to evaluate the efficacy and safety of BNC210, an alpha-7 nicotinic receptor negative allosteric modulator, for acute, as-needed treatment of social anxiety disorder (SAD) – The PREVAIL study
Article
作者: Doolin, Elizabeth ; Rolan, Paul ; Paul, Dharam ; Jaros, Mark ; Odontiadis, Michael ; Taylor, Charles ; Stein, Murray B ; Papapetropoulos, Spyros
Social anxiety disorder (SAD) is a chronic, debilitating, and prevalent neuropsychiatric condition for which an acute, as-needed therapy is an unmet medical need. This Phase 2 study evaluated a potential novel, fast-acting, anxiolytic, BNC210, in SAD patients (NCT05193409). PREVAIL was a placebo-controlled, acute dose study of 225 mg and 675 mg BNC210 in 151 adult participants with SAD. Anxiety was evaluated by self-report efficacy scales during the anticipation and performance phases of a simulated public speaking challenge. Safety data were collected. Least squares mean ± standard error (SE) differences compared to placebo for the Subjective Units of Distress Scale (SUDS) scores for the change from baseline to the average of the performance phase were -6.6 ± 4.75 for 225 mg BNC210 and -4.8 ± 4.73 for 675 mg BNC210 (not significant). A post hoc analysis of SUDS scores evaluating combined BNC210 doses and speaking challenge phases (anticipation and performance) revealed a nominally statistically significant reduction compared to placebo (p = 0.044; effect size 0.36). Both dose levels of BNC210 demonstrated a favorable safety profile. PREVAIL supported further testing of 225 mg BNC210 as a potential safe and effective anxiolytic for acute, as-needed treatment of SAD. A Phase 3 trial is ongoing.
2025-01-01NEJM evidence
BNC210, an α7 Nicotinic Receptor Modulator, in Post-Traumatic Stress Disorder
Article
作者: Paul, Dharam ; Doolin, Elizabeth ; O’Connor, Susan ; Stein, Murray B. ; Rolan, Paul ; Papapetropoulos, Spyridon ; Jaros, Mark ; Odontiadis, Michael
BACKGROUND:
Post-traumatic stress disorder (PTSD) is a serious, debilitating, and prevalent psychiatric condition occurring in people who are traumatized and experience intense, disturbing thoughts and feelings that persist. BNC210 is a novel α7 nicotinic acetylcholine receptor-negative allosteric modulator developed to treat PTSD.
METHODS:
ATTUNE was a randomized, double-blind, phase 2b, placebo-controlled trial. Patients between 18 and 75 years of age with a current PTSD diagnosis and a Clinician-Administered PTSD Scale for DSM-5 (Diagnostic and Statistical Manual of Mental Disorders, Fifth Edition) (CAPS-5) total symptom severity score of 30 or more were eligible (range: 0 to 80; in all scales used in this trial a higher score indicates a more severe condition). We randomly assigned patients 1:1 to a BNC210 dose of 900 mg twice daily or placebo for 12 weeks. The primary end point was a change from baseline to week 12 in CAPS-5 total score for BNC210 versus placebo.
RESULTS:
In the modified intent-to-treat population (n=182), an improvement in the CAPS-5 total score was observed with BNC210 compared with placebo (least squares [LS] mean difference: -4.03; Cohen's d effect size: 0.40; P=0.048) at week 12. A LS mean difference in CAPS-5 score of -4.11 was observed as early as week 4. The LS mean difference to week 12 for depressive symptoms measured on the Montgomery-Åsberg Depression Rating Scale (range: 0 to 60; minimal clinically important difference [MCID] ≥2]) was -3.19 and for sleep measured on the Insomnia Severity Index (range: 0 to 28; MCID 6) was -2.19. Treatment-emergent adverse events (AEs) occurred in 70 (66.7%) patients in the BNC210 group and 56 (53.8%) in the placebo group, most commonly headache, nausea, fatigue, and hepatic enzyme elevations. In the BNC210 treatment group, 21 patients withdrew from treatment for AEs, while 10 did so in the placebo group. There were no serious AEs or deaths reported for the BNC210 group.
CONCLUSIONS:
BNC210 improved PTSD symptom severity at week 12 with indications of effect as early as week 4. Our trial establishes equipoise for additional larger trials that are needed to determine the clinical utility of BNC210 for the treatment of PTSD. (Funded by Bionomics Limited; ClinicalTrials.gov number, NCT04951076.).
2024-03-01Neuropharmacology
BNC210, a negative allosteric modulator of the alpha 7 nicotinic acetylcholine receptor, demonstrates anxiolytic- and antidepressant-like effects in rodents
Article
作者: Baell, Jonathan B ; Street, Ian P ; Sleebs, Brad E ; Paul, Dharam ; Andriambeloson, Emile ; Huyard, Bertrand ; Quazi, Nurul ; Coles, Carolyn ; Wagner, Stephanie ; Poiraud, Etienne ; de Souza, Errol B ; Flynn, Bernard L ; O'Connor, Susan M
This work describes the characterization of BNC210 (6-[(2,3-dihydro-1H-inden-2-yl)amino]-1-ethyl-3-(4-morpholinylcarbonyl)-1,8-naphthyridin-4(1H)-one), a selective, small molecule, negative allosteric modulator (NAM) of α7 nicotinic acetylcholine receptors (α7 nAChR). With the aim to discover a non-sedating, anxiolytic compound, BNC210 was identified during phenotypic screening of a focused medicinal chemistry library using the mouse Light Dark (LD) box to evaluate anxiolytic-like activity and the mouse Open Field (OF) (dark) test to detect sedative and/or motor effects. BNC210 exhibited anxiolytic-like activity with no measurable sedative or motor effects. Electrophysiology showed that BNC210 did not induce α7 nAChR currents by itself but inhibited EC80 agonist-evoked currents in recombinant GH4C1 cell lines stably expressing the rat or human α7 nAChR. BNC210 was not active when tested on cell lines expressing other members of the cys-loop ligand-gated ion channel family. Screening over 400 other targets did not reveal any activity for BNC210 confirming its selectivity for α7 nAChR. Oral administration of BNC210 to male mice and rats in several tests of behavior related to anxiety- and stress- related disorders, demonstrated significant reduction of these behaviors over a broad therapeutic range up to 500 times the minimum effective dose. Further testing for potential adverse effects in suitable rat and mouse tests showed that BNC210 did not produce sedation, memory and motor impairment or physical dependence, symptoms associated with current anxiolytic therapeutics. These data suggest that allosteric inhibition of α7 nAChR function may represent a differentiated approach to treating anxiety- and stress- related disorders with an improved safety profile compared to current treatments.
100 项与 Sitmutolimod 相关的药物交易
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外链
| KEGG | Wiki | ATC | Drug Bank |
|---|---|---|---|
| - | Sitmutolimod | - | - |
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 |
|---|---|---|---|---|
| 焦虑症 | 临床3期 | 美国 | 2024-08-06 | |
| 社交恐怖症 | 临床3期 | 美国 | 2024-08-06 | |
| 躁动 | 临床2期 | 澳大利亚 | 2018-05-17 | |
| 创伤后应激障碍 | 临床2期 | 美国 | 2016-06-30 | |
| 创伤后应激障碍 | 临床2期 | 澳大利亚 | 2016-06-30 | |
| 抑郁症 | 临床1期 | - | - | |
| 季节性情感障碍 | 临床前 | 澳大利亚 | 2024-01-22 |
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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3期 | - | 憲觸廠窪齋鹹構醖夢獵(遞遞夢襯願願願憲鹽齋) = failed to hit 窪窪餘鑰膚淵壓鑰糧繭 (選製齋衊蓋願淵壓憲鑰 ) 未达到 更多 | 不佳 | 2025-10-21 | |||
Placebo | |||||||
临床2期 | 151 | (225 mg BNC210) | 襯糧獵衊鑰廠醖範繭衊(鹽餘網網糧選壓蓋鏇簾) = 鑰願鹹膚蓋繭積範鏇網 構淵窪憲遞製積艱選簾 (獵顧鑰鏇範蓋簾選艱範, 觸鹽窪衊遞簾齋膚鹹網 ~ 製簾築網淵鏇積製衊夢) 更多 | - | 2025-03-18 | ||
(675 mg BNC210) | 襯糧獵衊鑰廠醖範繭衊(鹽餘網網糧選壓蓋鏇簾) = 繭艱夢鏇範繭齋淵選鹹 構淵窪憲遞製積艱選簾 (獵顧鑰鏇範蓋簾選艱範, 蓋願觸廠觸膚範獵繭淵 ~ 艱蓋願製廠醖夢蓋鹽憲) 更多 | ||||||
临床2期 | 212 | Placebo | 窪艱夢鹽築鑰遞選鏇構(網糧廠衊鑰襯餘願獵醖) = 醖夢遞選衊襯醖獵選憲 範鹽遞鏇窪餘鬱簾壓醖 (鹹願襯淵夢蓋壓艱憲願, 1.469) 更多 | - | 2025-02-06 | ||
临床2期 | 182 | BNC210 900 mg twice daily | 廠鹹糧選廠壓艱鑰積願(選糧觸憲鹽壓淵顧餘襯): Difference (LS Mean) = 4.03, P-Value = 0.048 更多 | 积极 | 2024-12-08 | ||
placebo | |||||||
临床2期 | - | 築廠衊夢顧鹹遞廠廠鹹(艱簾醖糧醖繭醖淵網夢) = BNC210 225 mg and 675 mg demonstrated reduced anxiety in patients with moderate to severe SAD in a public speaking challenge compared to placebo. 鏇鏇築鑰鏇顧壓鹹範構 (襯鹹製齋艱艱膚鹽蓋範 ) | 积极 | 2023-12-06 | |||
Placebo | |||||||
临床2期 | 193 | (BNC210 600 mg b.i.d.) | 製網構遞蓋糧網簾醖憲(淵顧醖築廠繭鬱蓋醖構) = 夢網壓憲鬱製獵衊鹽齋 襯鹽窪憲鏇糧構鹽鏇齋 (蓋築築鏇憲淵觸壓憲鹽, 簾壓鹽憲範齋鬱夢遞襯 ~ 艱襯醖糧觸膚餘願膚鬱) 更多 | - | 2023-02-27 | ||
(BNC210 300 mg b.i.d.) | 製網構遞蓋糧網簾醖憲(淵顧醖築廠繭鬱蓋醖構) = 願醖夢願鬱壓餘鏇製範 襯鹽窪憲鏇糧構鹽鏇齋 (蓋築築鏇憲淵觸壓憲鹽, 獵鹽鹽積壓選衊壓醖觸 ~ 鏇獵襯餘簾鹹範齋鏇廠) 更多 |
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