预约演示
更新于：2026-08-31
Liradasertib
更新于：2026-08-31
概要
基本信息
原研机构 |
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- |
登录后查看时间轴
关联
9
项与 Liradasertib 相关的临床试验NCT06602193
A Phase 2a, Multicenter, Randomized, Double-Blind, Placebo-Controlled Study to Evaluate the Safety and Pharmacodynamic Effects of BIIB122 in Participants With LRRK2-Associated Parkinson's Disease (LRRK2-PD)
NCT06264440
A Phase 1, Open-Label, Crossover Study to Assess the Potential for Gastric pH-Dependent Drug-Drug Interactions of BIIB122 With a Proton Pump Inhibitor in Healthy Participants
NCT05418673
A Phase 3, Multicenter, Randomized, Double-Blind, Placebo-Controlled Study to Determine the Efficacy and Safety of BIIB122/DNL151 in Participants With Parkinson's Disease and Pathogenic LRRK2 Variants
100 项与 Liradasertib 相关的临床结果
登录后查看更多信息
100 项与 Liradasertib 相关的转化医学
登录后查看更多信息
100 项与 Liradasertib 相关的专利（医药）
登录后查看更多信息
4
项与 Liradasertib 相关的文献（医药）2023-12-01Bioorganic chemistry
Recent advances in targeting leucine-rich repeat kinase 2 as a potential strategy for the treatment of Parkinson’s disease
Review
作者: Longhui Sun ; Weihe Zhao ; Liyan Yuan ; Lei Shan ; Chunlei Wu ; Caiping Chen ; Chaojun Zhang ; Haopeng Sun ; Jing Wen ; Meiyang Xi ; Ruiwei Cao
Parkinson's disease (PD) is the second most common neurodegenerative disease. Several single gene mutations involved in PD have been identified such as leucine-rich repeat kinase 2 (LRRK2), the most common cause of sporadic and familial PD. Its mutations have attracted much attention to therapeutically targeting this kinase. To date, many compounds including small chemical molecules with diverse scaffolds and RNA agents have been developed with significant amelioration in preclinical PD models. Currently, five candidates, DNL201, DNL151, WXWH0226, NEU-723 and BIIB094, have advanced to clinical trials for PD treatment. In this review, we describe the structure, pathogenic mutations and the mechanism of LRRK2, and summarize the development of LRRK2 inhibitors in preclinical and clinical studies, trying to provide an insight into targeting LRRK2 for PD intervention in future.
2023-09-02Expert opinion on investigational drugs
DNL151, DNL201, and BIIB094: experimental agents for the treatment of Parkinson’s disease
Review
作者: Müller, Thomas
INTRODUCTION:
Pathogenic mutations of the abundant leucine-rich repeat kinase 2 gene support the onset of familial and sporadic forms of Parkinson's disease. These genetic variants catalyze kinase activity by substrate phosphorylation. They promote the nigrostriatal neurodegenerative process, i.e. characterized by Lewy body formation.
AREAS COVERED:
This narrative review discusses leucine-rich repeat kinase 2 inhibitors as therapeutic concept for beneficial disease modification following a literature search.
EXPERT OPINION:
Leucine-rich repeat kinase 2 gene function contributes to the onset of microglia inflammation, cellular, and mitochondrial dysfunction. Leucine-rich repeat kinase 2 inhibition with oral application of DNL151, respectively DNL201, and intrathecal administration of the antisense oligonucleotide BIIB094 in a single and multiple ascending dose study was safe and well tolerated. Approval of Leucine-rich repeat kinase 2 inhibitors in case of positive clinical study outcomes will introduce personalized medicine for beneficial modification of progression as the most unmet need for treatment of patients with Parkinson's disease. In addition to the currently, preponderantly performed clinical rating with established scales, further clinical trial endpoints, such as dosing of dopamine substitution, may be considered in study designs to demonstrate therapeutic effects on the progression of Parkinson's disease.
2023-03-01Movement disorders : official journal of the Movement Disorder Society
Article
作者: Ho, Carole ; Jennings, Danna ; Troyer, Matthew D. ; Heuberger, Jules A.A.C. ; Daryani, Vinay M. ; Scearce‐Levie, Kimberly ; Vissers, Maurits F.J.M. ; Maciuca, Romeo ; Huntwork‐Rodriguez, Sarah ; Henry, Anastasia G. ; Groeneveld, Geert Jan ; Chen, John J. ; van de Wetering de Rooij, Jeroen ; Fraser, Kyle ; Chin, Peter ; Diaz, Dolores ; Mabrouk, Omar S. ; De Vicente, Javier ; Cruz‐Herranz, Andrés ; Graham, Danielle ; Borin, Marie T. ; Goo, Marisa S.
Abstract:
Background:
Leucine‐rich repeat kinase 2 (LRRK2) inhibition is a promising therapeutic approach for the treatment of Parkinson's disease (PD).
Objective:
The aim of this study was to evaluate the safety, tolerability, pharmacokinetics, and pharmacodynamics of the potent, selective, CNS‐penetrant LRRK2 inhibitor BIIB122 (DNL151) in healthy participants and patients with PD.
Methods:
Two randomized, double‐blind, placebo‐controlled studies were completed. The phase 1 study (DNLI‐C‐0001) evaluated single and multiple doses of BIIB122 for up to 28 days in healthy participants. The phase 1b study (DNLI‐C‐0003) evaluated BIIB122 for 28 days in patients with mild to moderate PD. The primary objectives were to investigate the safety, tolerability, and plasma pharmacokinetics of BIIB122. Pharmacodynamic outcomes included peripheral and central target inhibition and lysosomal pathway engagement biomarkers.
Results:
A total of 186/184 healthy participants (146/145 BIIB122, 40/39 placebo) and 36/36 patients (26/26 BIIB122, 10/10 placebo) were randomized/treated in the phase 1 and phase 1b studies, respectively. In both studies, BIIB122 was generally well tolerated; no serious adverse events were reported, and the majority of treatment‐emergent adverse events were mild. BIIB122 cerebrospinal fluid/unbound plasma concentration ratio was ~1 (range, 0.7–1.8). Dose‐dependent median reductions from baseline were observed in whole‐blood phosphorylated serine 935 LRRK2 (≤98%), peripheral blood mononuclear cell phosphorylated threonine 73 pRab10 (≤93%), cerebrospinal fluid total LRRK2 (≤50%), and urine bis (monoacylglycerol) phosphate (≤74%).
Conclusions:
At generally safe and well‐tolerated doses, BIIB122 achieved substantial peripheral LRRK2 kinase inhibition and modulation of lysosomal pathways downstream of LRRK2, with evidence of CNS distribution and target inhibition. These studies support continued investigation of LRRK2 inhibition with BIIB122 for the treatment of PD. © 2023 Denali Therapeutics Inc and The Authors. Movement Disorders published by Wiley Periodicals LLC on behalf of International Parkinson and Movement Disorder Society.
230
项与 Liradasertib 相关的新闻（医药）2026-08-30
·葯融圈
2026-08-30
·微信
细胞疗法临床申请抗体药物偶联物siRNA免疫疗法
2026-08-30
·微信
细胞疗法临床申请抗体药物偶联物siRNA免疫疗法
100 项与 Liradasertib 相关的药物交易
登录后查看更多信息
研发状态
10 条进展最快的记录, 后查看更多信息
登录
| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 帕金森病 | 临床3期 | 美国 | 2022-08-26 | |
| 帕金森病 | 临床3期 | 美国 | 2022-08-26 | |
| 帕金森病 | 临床3期 | 法国 | 2022-08-26 | |
| 帕金森病 | 临床3期 | 法国 | 2022-08-26 | |
| 帕金森病 | 临床3期 | 德国 | 2022-08-26 | |
| 帕金森病 | 临床3期 | 德国 | 2022-08-26 | |
| 帕金森病 | 临床3期 | 意大利 | 2022-08-26 | |
| 帕金森病 | 临床3期 | 意大利 | 2022-08-26 | |
| 帕金森病 | 临床3期 | 西班牙 | 2022-08-26 | |
| 帕金森病 | 临床3期 | 西班牙 | 2022-08-26 |
登录后查看更多信息
临床结果
临床结果
适应症
分期
评价
查看全部结果
临床3期 | 7 | 顧鑰網艱選選艱廠糧鏇 = 選構願餘蓋壓廠廠遞構 鏇獵廠鏇選鬱繭淵獵蓋 (夢鹽觸醖蓋築製製醖艱, 蓋艱淵選鹽餘壓餘糧廠 ~ 夢壓餘簾廠艱範餘鹽選) 更多 | - | 2024-06-26 | |||
MDS2023 人工标引  | N/A | 222 | (healthy volunteers and Parkinson’s Participants) | 襯觸糧夢鬱鹽網鹽廠製(築鏇簾衊壓齋鹽鬱積網) = Reduction of urine BMP corresponded to ~80-90% of LRRK2 inhibition based on average concentrations. 淵蓋觸鹹糧壓構簾繭壓 (網壓積淵鏇顧繭製築襯 ) 更多 | 积极 | 2023-08-27 |
登录后查看更多信息
转化医学
使用我们的转化医学数据加速您的研究。
登录
或
药物交易
使用我们的药物交易数据加速您的研究。
登录
或
核心专利
使用我们的核心专利数据促进您的研究。
登录
或
临床分析
紧跟全球注册中心的最新临床试验。
登录
或
批准
利用最新的监管批准信息加速您的研究。
登录
或
特殊审评
只需点击几下即可了解关键药物信息。
登录
或
提出任何生物医药研究问题
让每一步生物医药决策都精准制胜
基于十亿级生物数据与全球情报的精准 AI，赋能早期药物发现
立即开始免费试用!
智慧芽新药情报库是智慧芽专为生命科学人士构建的基于AI的创新药情报平台，助您全方位提升您的研发与决策效率。
立即接入生物医药数据包
智慧芽新药库数据也通过智慧芽开放平台，以MCP或API服务形式对外开放。立即使用我们的MCP服务定制您的LLM智能体。
生物序列数据库
生物药研发创新
免费使用
化学结构数据库
小分子化药研发创新
免费使用