A Combined Investigation of the Protective Impact of the NOF/Q Antagonist LY-2940094 on Stress-induced Depression- and Anxiety-related Phenotypes in Humans

This project will integrate pharmacological and psychophysiological methodology to mechanistically investigate, in humans, the role of N/OFQ in laboratory phenotypes of both disorders. Specifically, a N/OFQ receptor (NOPR) antagonist will be used to test the hypothesis that NOPR blockage will have antidepressant-like effects (potentiate reward processing); in addition, this study will also evaluate a key anxiety phenotype (fear learning). Finally, the impact of recent life stress on these processes will be assessed. Results will demonstrate the specificity of NOPR blockage on depressive phenotypes or suggest a common pathway for emotional disorders and will confirm a modulatory role of life stress.

开始日期2025-06-01

申办/合作机构

McLean Hospital, Inc.

[+1]

NCT03608371

/ Completed临床2期

Phase 2A, Double-blind, Placebo-controlled Study to Investigate the Safety, Tolerability, Pharmacokinetics, and Efficacy of BTRX-246040 in Parkinson's Disease Subjects With Motor Fluctuations

The purpose of this study is to assess the safety, tolerability, pharmacokinetics and efficacy of BTRX-246040 in participants with Parkinson's Disease who have motor fluctuations and predictable early morning off periods.

开始日期2018-08-31

申办/合作机构

BlackThorn Therapeutics, Inc.

NCT03193398

/ Completed临床2期

A Randomized, Double-Blind, Placebo-Controlled, Parallel-Group Efficacy And Safety Study Of BTRX-246040 Administered Once Daily In Patients With Major Depressive Disorder With Or Without Anhedonia

This study will determine the efficacy, safety, and tolerability of a once-daily (QD) dose of up to 80 mg of BTRX-246040 for 8 weeks in participants with MDD.

开始日期2017-06-12

申办/合作机构

BlackThorn Therapeutics, Inc.

100 项与 LY-2940094 相关的临床结果

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100 项与 LY-2940094 相关的转化医学

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100 项与 LY-2940094 相关的专利（医药）

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项与 LY-2940094 相关的文献（医药）

2024-09-01·Neurotherapeutics

LY2940094, an NOPR antagonist, promotes oligodendrocyte generation and myelin recovery in an NOPR independent manner

Article

作者: Duan, Yanhui ; Ye, Chenyuan ; Xie, Xin ; Liao, Jingyi

The myelin sheath plays crucial roles in brain development and neuronal functions. In the central nervous system, myelin is generated by oligodendrocytes, that differentiate from oligodendrocyte progenitor cells (OPC). In demyelinating diseases, the differentiation capacity of OPC is impaired and remyelination is dampened. Boosting remyelination by promoting OPC differentiation is a novel strategy for the treatment of demyelinating diseases. The opioid system, which consists of four receptors and their ligands, has been implicated in OPC differentiation and myelin formation. However, the exact roles of each opioid receptor and the relevant pharmacological molecules in OPC differentiation and myelin formation remain elusive. In the present study, specific agonists and antagonists of each opioid receptor were used to explore the function of opioid receptors in OPC differentiation. Nociceptin/orphanin FQ receptor (NOPR) specific antagonist LY2940094 was found to stimulate OPC differentiation and myelination in both in vitro and in vivo models. Unexpectedly, other NOPR ligands did not affect OPC differentiation, and NOPR knockdown did not mimic or impede the effect of LY2940094. LY2940094 was found to modulate the expression of the oligodendrocytes differentiation-associated transcription factors ID4 and Myrf, although the exact mechanism remains unclear. Since LY2940094 has been tested clinically to treat depression and alcohol dependency and has displayed an acceptable safety profile, it may provide an alternative approach to treat demyelinating diseases.

2023-07-31·The international journal of neuropsychopharmacology

BTRX-246040 Acts Through the Ventrolateral Periaqueductal Gray to Exert Antidepressant-Relevant Actions in Mice

Article

作者: Lin, Tzer-Bin ; Liu, Xueman ; Lai, Cheng-Yuan ; Lee, Chau-Shoun ; Wu, Han-Fang ; Xu, Yuanyuan ; Peng, Hsien-Yu ; Li, Zhenlong ; Hsieh, Ming-Chun ; Sheng, Zhenyu ; Chen, Xinya ; Chou, Dylan ; Li, Rourou

Abstract:

Background:

BTRX-246040, a nociceptin/orphanin FQ peptide receptor antagonist, is being developed for the treatment of depressive patients. However, the underlying mechanism of this potential antidepressant is still largely unclear. Here, we studied the antidepressant-related actions of BTRX-246040 in the ventrolateral periaqueductal gray (vlPAG).

Methods:

The tail suspension test, forced swim test, female urine sniffing test, sucrose preference test, and learned helplessness (LH) combined with pharmacological approaches were employed to examine the antidepressant-like effects and drug effects on LH-induced depressive-like behavior in C57BL/6J mice. Electrophysiological recordings in vlPAG neurons were used to study synaptic activity.

Results:

Intraperitoneal administration of BTRX-246040 produced antidepressant-like behavioral effects in a dose-dependent manner. Systemic BTRX-246040 (10 mg/kg) resulted in an increased frequency and amplitude of miniature excitatory postsynaptic currents (EPSCs) in the vlPAG. Moreover, slice perfusion of BTRX-246040 directly elevated the frequency and amplitude of miniature EPSCs and enhanced the evoked EPSCs in the vlPAG, which were blocked by pretreatment with the nociceptin/orphanin FQ peptide receptor agonist Ro 64-6198. In addition, intra-vlPAG application of BTRX-246040 produced antidepressant-like behavioral effects in a dose-dependent manner. Moreover, intra-vlPAG pretreatment with 6-cyano-7-nitroquinoxaline-2,3-dione reversed both systemic and local BTRX-246040–mediated antidepressant-like behavioral effects. Furthermore, both systemic and local BTRX-246040 decreased the LH phenotype and reduced LH-induced depressive-like behavior.

Conclusions:

The results suggested that BTRX-246040 may act through the vlPAG to exert antidepressant-relevant actions. The present study provides new insight into a vlPAG-dependent mechanism underlying the antidepressant-like actions of BTRX-246040.

2022-07-01·Neuropharmacology2区 · 医学

The NOP antagonist BTRX-246040 increases stress resilience in mice without affecting adult neurogenesis in the hippocampus

2区 · 医学

Article

作者: Azevedo Neto, Joaquim ; Robert, Cathaline ; Gavioli, Elaine C ; Ruzza, Chiara ; Sturaro, Chiara ; Mouledous, Lionel ; D'Oliveira da Silva, Flora ; Calo, Girolamo ; Guarino, Annunziata

Nociceptin/orphanin FQ (N/OFQ) is the endogenous ligand of an inhibitory G protein coupled receptor named N/OFQ peptide receptor (NOP). Clinical and preclinical findings suggest that the blockade of the NOP signaling induces antidepressant-like effects. Additionally, the blockade of the NOP receptor during inescapable stress exposure prevented the acquisition of the helplessness phenotype, suggesting that NOP antagonists are able to increase stress resilience. BTRX-246040 (aka LY2940094) is a NOP receptor antagonist with high affinity, potency and selectivity for the NOP over classical opioid receptors. BTRX-246040 is under development for the treatment of depression, eating disorders and alcohol abuse and it already entered clinical trials. In the present study, the antidepressant effects of BTRX-246040 were evaluated in mice subjected to the forced swimming test and to the learned helplessness model of depression. Additionally, the ability of BTRX-246040 to prevent the development of the helpless behavior and to modulate adult hippocampal neurogenesis has been investigated. BTRX-246040 (30 mg/kg, i.p.) produced antidepressant-like effects in the forced swimming test and in the learned helplessness model. More interestingly, when given before the stress induction sessions it was able to prevent the development of the helplessness behavior. Under these experimental conditions, BTRX-246040 did not modulate adult hippocampal neurogenesis, neither in naive nor in stressed mice. This study, performed with a clinically viable ligand, further corroborates growing evidence indicating that the blockade of the NOP signaling may provide an innovative strategy for the treatment of stress related psychopathologies.

项与 LY-2940094 相关的新闻（医药）

2024-09-12

·药精通Bio

全球在研小分子抗抑郁症新药盘点

Apimostinel CAS : 1421866-48-9 机理：NMDA受体部分激动剂状态：II期（IV）和I期（口服）临床试验开发者：Allergan 也称为NRX-1074，是一种最初由Naurex开发的用于治疗抑郁症的药物-但目前正在由Naurex和Allergan（收购Naurex）共同研究。该药物对NMDA受体具有选择性的部分激动剂的功能，特别是在甘氨酸结合位点的变构位点。虽然Apimostinel表现出GLYX-13（另一种正在由Naurex开发的药物）相似的作用机制，但它与GLYX-13的不同之处在于其重量更显着。一项比较分析表明，按重量计，Apimostinel的效力是GLYX-13的数千倍。之前我已经讨论了使用NRX-1074来治疗抑郁症的潜在好处，并提到它起效快，没有拟精神病作用并且似乎耐受良好。初步证据表明，服用Apimostinel后，抑郁症状可能在24小时内消失。此外，Apimostinel的情绪增强作用似乎是剂量依赖性的，因此更高剂量的抗抑郁作用更为明显。值得一提的是，在早期试验中，单剂量的Apimostinel提供的缓解抑郁症状的症状要比SSRIs持续数周的缓解率更高。 BTRX-246040 CAS : 1307245-86-8 机理: NOC 受体拮抗剂状态: Phase II 开发者: BlackThorn Therapeutics 该药物最初由礼来公司进行研究，但现在似乎与黑刺李疗法联系在一起，并有了一个新的化学名称。2016年发表的一项概念验证研究报告称，LY-2940094(40毫克)是安全的，耐受性好，对治疗人类抑郁症有效——持续时间超过8周。它作为一种抗抑郁药物的初步疗效通过格里-汉密尔顿抑郁评分量表(GRID-Hamilton Depression Rating scale)从基线到8周的17个总分的显著变化得到证明。此外，研究还发现LY-2940094在治疗的第一周内改变了对情绪刺激的处理——在情绪测试系列中，对积极面部表情相对于消极面部表情的认知增强就是证据。LY-2940094的初步调查数据是第一批显示NOP受体拮抗剂治疗抑郁症的潜力的数据。关于BTRX-246040是否将继续用于治疗重度抑郁症，还是将其作为治疗其他神经系统疾病的治疗手段而接受调查，还存在一些争议。然而，与大多数抗抑郁药物相比，BTRX-246040表现出独特的作用机制。拮抗NOC受体似乎能增加大脑几个区域的单胺浓度，增强神经发生，并调节下丘脑-垂体-肾上腺轴的激活。 CERC-301 CAS : 808732-98-1 机理: NMDA 受体 (NR2B-selective) 拮抗剂状态: Phase II 开发者: Cerecor 2013年，FDA授予CERC-301“快速通道指定”，作为抑郁症和自杀意念的潜在辅助治疗药物。药效学研究表明，CERC-301对NMDA受体NR2B亚基具有高选择性拮抗作用。它对NMDA受体NR2B亚基的选择性亲和性被认为可以最大限度地降低与其他非选择性NMDA受体拮抗剂共同发生的拟精神分裂效应(如药物诱导的精神病)的可能性。 CERC-301的显影剂Cerecor表明，CERC-301具有快速的抗抑郁活性，从而在给药几分钟或几小时内就能缓解抑郁症状，而不是几天或几周。来自CERC-301试验的初步数据表明，该药物耐受性良好且安全。许多人认为，CERC-301是正在开发的治疗抑郁症的NMDA拮抗剂中最有前途的。 CERC-501 CAS : 1174130-61-0 机理: KOR 拮抗剂状态: Phase III 开发者: Janssen CERC-501是美国礼来公司首次研发的药物，名为LY-2456302。然而，在2015年2月，礼来公司将LY-2456302卖给了Cerecor公司，后者将其更名为CERC-501。2016年，CERC-501作为一种抗抑郁II期临床试验难治性抑郁症患者达到效果。截至2017年8月，Cerecor将CERC-501出售给了Janssen Pharmaceuticals，后者正在继续开发其作为抑郁症的辅助疗法和药物滥用障碍的干预疗法。药效学评估显示，CERC-501是一种选择性的、短效的KOR (kappa阿片受体)拮抗剂。研究表明，激活kappa类阿片受体(KORs)会引发烦躁、幻觉和精神幻像效应——同时也会强化神经化学系统，与奖赏缺乏综合症、慢性压力和重度抑郁症有关。用CERC-501拮抗kappa阿片受体(KOR)可能通过抵消已有的kappa阿片受体激活而促进抗抑郁效果。CERC-501与其他抗抑郁药(如SSRIs)联合使用可产生协同情绪增强作用(或比单独使用任何一种药物效果更好)。有报道称，在三期临床试验中，CERC-501的副作用不严重。 Liafensine (DB104) CAS:1198790-53-2 机理: SNDRI 状态: Phase II 开发者: Denovo Biopharma Liafensine (DB104)，原名BMS-820836，是一种SNDRI(5 -羟色胺-去甲肾上腺素-多巴胺再摄取抑制剂)或三层再摄取抑制剂，最初由AMRI开发，授权给百时美施贵宝治疗重度抑郁症。通过二期临床试验，该药物表现出与依西酞普兰(即依地普仑)和度洛西汀(即欣百达)相似的疗效。但百时美施贵宝终止其开发，主要原因是其疗效并不明显优于依地普乐和欣百达。它的疗效相对于副作用和滥用潜力可能是Liafensine 被百时美施贵宝停止开发的原因。2017年，Denovo Biopharma获得了Liafensine的许可权，三重再摄取抑制剂的二期临床试验仍在继续。 JNJ-39393406 CAS : 953428-73-4 机理: Alpha-7 nAChR 调制器状态: Phase II 开发者: Janssen JNJ-39393406用于治疗重度抑郁症和戒烟。与目前市场上大多数抗抑郁药相比，JNJ-39393406的独特之处在于，它仅作为-7烟碱乙酰胆碱受体的选择性正变构调制器(PAM)。药效学研究表明，该药物不会与-4-beta-2或-3-beta-4尼古丁乙酰胆碱受体或- 5-HT3受体相互作用。更重要的是，药物似乎并没有与62种受体和酶相互作用。截至2018年2月，JNJ-39393406正在进行治疗重度抑郁症和尼古丁戒断的II期临床试验。JNJ-39393406以前被研究作为阿尔茨海默病和精神分裂症的干预措施，但是，经评估后被放弃了。 Ansofaxine (LY03005) CAS : 916918-84-8 机理: SNDRI 状态: Phase I 开发者: 绿叶制药盐酸Ansofaxine(LY03005)是绿叶制药集团开发的用于治疗中重度抑郁症的三重摄取抑制剂(5 -羟色胺-去甲肾上腺素-多巴胺)。对Ansofaxine的药效学评价表明，它具有SNDRI的作用，是去文拉法辛的前药。然而，与去文拉法辛(即Pristiq)相比，Ansofaxine在同时调节血清素和去甲肾上腺素的同时，具有显著的多巴胺能效应。到目前为止，Ansofaxine已经在两个人体试验中进行了评估，分别有72名和48名参与者。从现有的I期试验数据来看，Ansofaxine在40毫克至160毫克的剂量下似乎具有良好的耐受性和安全性。绿叶制药集团认为，与目前市面上的抗抑郁药相比，这种新药的副作用更少，起效更快。 MIN-117 CAS : 310392-93-9 机理: SDRI 状态: Phase II 开发者: Minerva Neurosciences MIN-117是一种血清素-多巴胺调制器，由Minerva神经科学公司开发用于治疗重度抑郁症。其作用机制针对受体和转运体的结合，包括:α- 1a受体;α-1B受体;5-HT2A受体;SERT(羟色胺转运体);和DAT(多巴胺转运体)。具体来说，MIN-117被证明是一种5-HT1A和5-HT2A拮抗剂;血清素和多巴胺再摄取抑制剂;α- 1a和α- 1b肾上腺素能受体调节剂。 Minerva神经科学提示MIN-117旨在解决重性抑郁症伴有共病焦虑或焦虑症状的患者的未控制症状。开发人员推测MIN-117将比目前市场上的大多数抗抑郁药物反应更快、更安全、耐受性更好。目前MIN-117作为干预抑郁症的临床试验正处于II期。 Seltorexant (MIN-202) CAS : 1293281-49-8 机理: Orexin-2 拮抗剂状态: Phase II (complete) 开发者: Minerva Neurosciences & Janssen Seltorexant，又称MIN-202 (Minerva)和JNJ-42847922或JNJ-922 (Janssen)，是一种正在研究中的小分子、选择性orexin受体拮抗剂，由Minerva神经科学和Janssen开发。临床试验正在评估Seltorexant对重度抑郁症和失眠的治疗效果。据开发人员介绍，Seltorexant可以阻断大脑中促进觉醒的神经元的激活，特别是通过与orexin 2 (Orx-2)受体结合。 NSI-189 CAS : 1270138-40-3 机理: 神经发生诱导物状态: Phase III (?) 开发者: Neuralstem Inc. NSI-189是由Neuralstem公司开发的一种实验性药物，用于治疗重度抑郁症、认知障碍和神经退行性疾病。NSI-189是通过超过10000个化合物筛选，以确定哪些在体外(细胞)诱导最大程度的神经发生。NSI-189在体外和啮齿类动物中都表现出了疗效，随后将在患有重度抑郁症的人身上进行测试。在II期临床试验中，NSI-189通过降低220名重性抑郁症患者的MADRS评分而未能达到其主要终点。NSI-189仍将继续接受神经系统和中枢神经系统疾病的治疗评估，包括:神经病、缺血性中风和认知障碍。 Rapastinel (GLYX-13) CAS : 117928-94-6 机理: NMDA 受体调制器状态: Phase III 开发者: Allergan Rapastinel(原名GLYX-13)是Allergan公司开发的一种药物(在收购Allergan之前由Naurex公司进行测试)，作为治疗耐药性抑郁症(或对2种或2种以上一线干预无效的抑郁症)的辅助干预手段。这种药物在口服时是不活跃的，而在静脉注射时是特别设计的。它在NMDA受体复合物的甘氨酸亚基的变构位点起选择性、适度的局部激动剂(混合拮抗剂/激动剂)的作用。初步证据表明Rapastinel作用快速，并产生长期的抗抑郁反应。此外，Rapastinel似乎是通过抑制和增强NMDA受体介导的信号转导而增强认知功能的。无论动物年龄多大，给动物服用Rapastinel能增强记忆和学习能力，还能促进神经保护作用。 Rapastinel被归类为一种glyxin化合物，来源于修改单克隆抗体的结构，调节NMDA受体，称为“B6B21”。基于初步的试验数据，Rapastinel是治疗难治性抑郁症最有希望的治疗手段之一。 SAGE-217 CAS : 1632051-40-1 机理: GABAA受体调制器状态: Phase III 开发者: Sage Therapeutics Sage -217是由Sage Therapeutics公司研发的一种研究性化学药物，用于治疗重度抑郁症和产后抑郁症，以及帕金森病、失眠和癫痫的原发性震颤。据Sage Therapeutics公司介绍，Sage -217是一种合成的孕烷神经类固醇，它是GABAA受体的一种正变构调制器。SAGE-217的目标是改进并继承Brexanolone ——另一种圣人治疗抑郁症的药物，目前已进入临床试验阶段。在用于治疗女性产后抑郁症(PPD)患者的3期试验ROBIN中，达到了试验的主要和次要终点。重症抑郁三期失败。 Travivo (Gepirone ER) CAS:83928-66-9;83928-76-1 机理: 5-HT1A 选择性部分激动剂状态: 等待 FDA 批准开发者: Fabre-Kramer Pharmaceuticals Travivo (Gepirone ER)是一种抗抑郁药物，最初因疗效问题被FDA多次拒绝。它第一次被否决是在2004年，然后在2007年再次被否决。FDA在2015年审查了Gepirone的数据，推翻了他们最初对该药物的排斥——给予了有利的评价。2016年3月FDA对Travivo (Gepirone ER)治疗重度抑郁症的疗效进行了有利的规定。参考原文：30+ New Antidepressants (2018): Drugs In Clinical Trials TIS2024第四届自免疾病细胞疗法与干细胞疗法论坛重磅来袭，点击图片查看重磅嘉宾，合作详询：王晨 180 1628 8769 （扫码立即报名获取TIS2024免费票）

临床2期快速通道临床1期并购

2018-05-31

·BioSpace

A Look at A Few Hot New Approaches and News in the Research Imaging Market

Advances in data storage and processing, as well as biomarker identification, has led to cutting-edge breakthroughs in clinical and research imaging technology. Here’s a look at just a few of these stories. Advances in data storage and processing, as well as biomarker identification, has led to cutting-edge breakthroughs in clinical and research imaging technology. Here’s a look at just a few of these stories. Netherlands-based MILabs installed a VECTor 5 PET/SPECT/OI/CT system at the Chair of Pharmaceutical Radiochemistry at the Technical University Munich (TUM) Campus in Garching, Germany. The institute has a well-known radiopharmaceutical research program made up of fundamental tracer development, innovative radiolabeling strategies, and the preclinical and clinical assessment of new tracers. “We have been waiting for a long time for a system like the MILabs VECTor-OI-CT that offers the capabilities to support all aspects of our various research projects on multimodal theranostics tracer technology,” said HJ Wester, chair of Pharmaceutical Radiochemistry at the university, in a statement. “As evidenced by recent developments, such as PSMA-inhibitors, CXCR4-ligands, multimodal intraoperative probes, plus the renaissance of 99m Tc-tracers or the new radiohybrid technology, modern tracer development has become more and more multidimensional.” LexaGene Holdings , based in Beverly, Massachusetts, inked a deal with the Stanford University School of Medicine supplying targeted sequencing technology in combination with LexaGene’s microfluidic instrument. The sequencing technology was developed in the laboratory of Hanlee Ji, an associate professor of medicine at Stanford. LexaGene develops fully automated pathogen detection systems, specifically the open-access LX6. This system allows end-users to load their own real-time PCR assays into the instrument for customized pathogen detection. It can process six samples at a time and return results in about one hour. Jack Regan, chief executive officer of LexaGene, said in a statement, “LexaGene’s technology was originally designed for pathogen detection across very large markets—I’m thrilled to report that we are working to expand our technology’s capability to include cancer diagnostics and Next Generation Sequencing.” Late last year, Seattle-based Blaze Bioscience raised $16.1 million in a Series B-1 financing, bringing its total raise to $33 million. The company’s lead product candidate is BLZ-100, a genetically engineered peptide used to “paint” different types of tumor cells. The peptide is chemically linked to a fluorescent beacon, which is injected into tumor tissue in a surgical site. The surgeon is then able to visualize the illuminated tumor next to healthy tissue with the assistance of a fluorescent imaging camera. The company was founded in 2010 and spun out of the Fred Hutchinson Cancer Research Center. BlackThorn Therapeutics spun out of Scripps Research Institute in 2013 and came out of stealth mode in 2016 with a $40 million Series A financing round. Most psychiatric disorders lack reliable biological markers. Diagnosis is typically performed based on symptoms, usually behavioral or subjective descriptions of moods and emotions. Clinical trial results are typically based on those observations, often with a doctor using a standardized questionnaire. BlackThorn’s approach is to link objective assessment tools that quantify emotion, behavior and cognition with functional imaging technology. Its technology platform is dubbed INFORM. In December 2017, BlackThorn presented data on its lead program, BTRX-246040, a first-in-class antagonist of the nociception receptor (NOPR) being evaluated in a Phase IIa trial in major depressive disorder (MDD), at the American College of Neuropsychopharmacology (ACNP) Annual Meeting. Relay Therapeutics , based in Cambridge, Massachusetts, closed on a $63 million Series B financing in December 2017. The company focuses on developing therapeutics based on protein motion. For decades, the technology hasn’t been available or affordable to completely evaluate the movement of proteins, which in the body are in constant motion. Sanjiv Patel , Relay’s president and chief executive officer, told BioSpace in 2017, “Relay was formed based on that premise, visualizing protein motion, and understanding how they move, using technology with experimentation as well as computation to create consensus movies to design better drugs. So, we have a very powerful experimentation part using emerging techniques that allow us to visualize motion, such as X-ray crystallography and cryo-electron microscopy, which was the winner of this year’s Nobel for Chemistry. One of the other challenges is the amount of data that’s involved in visualizing motion. Earlier, it would have taken several years and been cost-prohibitive. But the cost has come down, so the experimental techniques and the increasing power of computation allows us for the first time to visualize proteins moving in the body and using that insight to design better drugs.” These are just five examples of companies working on the very cutting edge of imaging technology.

临床2期

2016-10-20

·BioSpace

Bay Area’s BlackThorn Therapeutics Comes Out of Stealth Mode With $40 Million to Push New Neuroscience Drugs Into Trials

October 20, 2016 By Mark Terry , BioSpace.com Breaking News Staff South San Francisco – BlackThorn Therapeutics announced that it had closed on a Series A financing round worth $40 million. The round was led by ARCH Venture Partners and supported by Johnson & Johnson Innovation – JJDC , as well as Altitude Life Science Ventures , Mercury Fund , Alexandria Real Estate Equities , and an undisclosed crossover fund. Blackthorn is working in the difficult area of neurological and psychological diseases. Its lead drug, BTRX-246040 , was licensed from Eli Lilly and Co. . At Lilly, it had failed two clinical trials, which led to Lilly essentially abandoning the neuroscience development area. “The risk associated with drug development in this arena has always been driven by lumping a lot of conditions together,” Mark Corrigan , the company’s executive chairman, told the San Francisco Business Times. As reported by Xconomy, “This year alone, antipsychotic drugs developed by Alkermes , Intra-Cellular Therapies , and the now-defunct FORUM Pharmaceuticals have failed Phase III trials, and all three cited a high level of placebo effect in the control group as a significant problem.” And most psychiatric disorders lack reliable biological markers—they’re usually diagnosed with symptoms. And as a result, a clinical trial’s results are based on observations of mood or behavior, often with a doctor using a standardized questionnaire. “There is no such toolkit for [neurobehavioral diseases] yet,” Scott Forrest , BlackThorn’s vice president of corporate development told Xconomy. “It’s emerging from clinical research.” But BlackThorn, which spun out of Scripps Research Institute in 2013, thinks the time might be ripe. It has a technology platform called INFORM, which, according to the company, “supports the discovery and development of targeted treatments by linking brain physiology to behavior using advanced functional imaging and objective assessment tools that quantify emotion, behavior and cognition while relying less on traditional qualitative clinical observations.” Which sounds a lot like questionnaires tied into some sort of brain imaging technology. Its lead program, BTRX-246060, is a first-in-class antagonist of the nociception receptor (NOPR), which has been tied to several neurobehavioral disorders. It is currently starting Phase II clinical trials. BlackThorn also has a pipeline of small molecules for other neurological disorders. BTRX-246060 has been evaluated in approximately 200 people, and is projected to start mid-stage trials in 2017. The company also plans to start another compound in an early-stage trial late next year in patients with bipolar disorder and other conditions. BlackThorn currently has 13 employees and 20 contractors. It indicates it plans to double in size—whether that means 26 employees or 66 is not clear—and it is currently searching for a chief executive officer. The company is currently located in Johnson & Johnson ’s JLabs incubator space in South San Francisco, but is looking for a permanent site in San Francisco. The company is currently being led by Mark Corrigan . Prior to BlackThorn, Corrigan was chief executive officer of Zalicus , and executive vice president of Research and Development at Sepracor . He is serves on the boards of CoLucid , Cardiome , Quartet and Nabriva . Bill Martin is the company’s chief scientific officer. He was previously executive director at Theravance Biopharma . Annette Madrid is BlackThorn’s chief medical officer. She was the chief medical officer at Balance Therapeutics and Jazz Pharmaceuticals . Scott Forrest is the vice president of operations and corporate development. He was previously vice president of business at The Scripps Research Institute.

临床2期临床3期高管变更

100 项与 LY-2940094 相关的药物交易

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KEGG	Wiki	ATC	Drug Bank
-	LY-2940094	-	DB16048

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适应症	最高研发状态	国家/地区	公司	日期
精神运动障碍	临床2期	美国	BlackThorn Therapeutics, Inc.	2018-08-31
帕金森病	临床2期	美国	BlackThorn Therapeutics, Inc.	2018-08-31
快感缺乏	临床2期	美国	BlackThorn Therapeutics, Inc.	2017-06-12
酗酒	临床2期	美国	BlackThorn Therapeutics, Inc.	2013-07-01
重度抑郁症	临床2期	美国	BlackThorn Therapeutics, Inc.	2012-11-01

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT03608371 (CTgov)	临床2期	精神运动障碍 \| 帕金森病	24	BTRX-246040 (BTRX-246040 Cohort 1)	製鬱醖糧構壓憲顧醖糧(顧膚餘構遞築襯齋顧餘) = 簾憲觸範膚壓淵廠簾鏇築鏇製簾獵齋選選選鹽 (廠積願簾選願襯齋艱夢, 7.01) 更多	-	2025-06-24
				BTRX-246040 (BTRX-246040 Cohort 2)	製鬱醖糧構壓憲顧醖糧(顧膚餘構遞築襯齋顧餘) = 鹹鑰窪築網築構蓋餘鹹築鏇製簾獵齋選選選鹽 (廠積願簾選願襯齋艱夢, 4.68) 更多
NCT03193398 (CTgov)	临床2期	快感缺乏 \| 重度抑郁症	104	BTRX-246040 oral capsule(s) (BTRX-246040)	鏇鏇範繭構鹹獵鏇糧製(繭選範廠積繭鏇齋範製) = 願淵構憲範網鬱製窪糧窪糧淵選鏇築窪膚壓鹹 (簾遞鏇選淵齋獵鬱廠醖, 1.73) 更多	-	2021-05-11
				Placebo oral capsule(s) (Placebo)	鏇鏇範繭構鹹獵鏇糧製(繭選範廠積繭鏇齋範製) = 範觸製糧憲蓋齋糧艱醖窪糧淵選鏇築窪膚壓鹹 (簾遞鏇選淵齋獵鬱廠醖, 1.79) 更多