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更新于：2026-01-28
TD-0903
更新于：2026-01-28
概要
基本信息
药物类型 小分子化药 |
别名 Nezulcitinib、TD-0903、THRX-136377 |
作用方式 抑制剂 |
作用机制 JAK1抑制剂(酪氨酸蛋白激酶JAK1抑制剂)、JAK2抑制剂(酪氨酸蛋白激酶JAK2抑制剂)、JAK3抑制剂(酪氨酸蛋白激酶JAK3抑制剂) |
治疗领域 |
在研适应症 |
非在研机构- |
权益机构- |
最高研发阶段临床2期 |
首次获批日期- |
最高研发阶段(中国)- |
特殊审评- |
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结构/序列
分子式C30H37N7O2 |
InChIKeyVQIIUJSNIKEMCK-MHZLTWQESA-N |
CAS号2412496-23-0 |
关联
3
项与 TD-0903 相关的临床试验NCT05091723
Phase 1, Open-label Study to Assess the Pharmacokinetics and Safety of Inhaled Nezulcitinib (TD-0903) Administered in the Setting of Supplemental Oxygenation Scenarios in Healthy Participants
NCT04402866
A Phase 2, Randomized, Double-Blind, Placebo-Controlled, Parallel-group, Multi-center Study of an Inhaled Pan-Janus Kinase Inhibitor, TD-0903, to Treat Symptomatic Acute Lung Injury Associated With COVID-19
NCT04350736
A Phase 1, Double-blind, Randomized, Placebo-controlled, Sponsor-open, SAD and MAD Study in Healthy Subjects to Evaluate the Safety, Tolerability, and PK of Inhaled TD-0903, a Potential Treatment for ALI Associated With COVID-19
100 项与 TD-0903 相关的临床结果
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100 项与 TD-0903 相关的转化医学
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100 项与 TD-0903 相关的专利（医药）
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5
项与 TD-0903 相关的文献（医药）2023-07-01BMJ open respiratory research
Efficacy and safety of an inhaled pan-Janus kinase inhibitor, nezulcitinib, in hospitalised patients with COVID-19: results from a phase 2 clinical trial
Article
作者: Saggar, Rajeev ; Thompson, Corbin G ; Bogus, Maxim ; Nguyen, Tuan ; Singh, Dave ; Lombardi, David A ; Belperio, John ; Woo, Jacky ; Bourdet, David L ; Haumann, Brett ; Kaufman, Elad ; Pfeifer, Nathan D ; Moskalenko, Valentyn ; Moran, Edmund J
Background:
The inhaled lung-selective pan-Janus kinase inhibitor nezulcitinib had favourable safety and potential efficacy signals in part 1 of a phase 2 trial in patients with severe COVID-19, supporting progression to part 2.
Methods:
Part 2 was a randomised, double-blind phase 2 study (NCT04402866). Hospitalised patients aged 18–80 years with confirmed symptomatic COVID-19 requiring supplemental oxygen (excluding baseline invasive mechanical ventilation) were randomised 1:1 to nebulised nezulcitinib 3 mg or placebo for up to 7 days with background standard-of-care therapy (including corticosteroids). Efficacy endpoints included respiratory failure-free (RFF) days through day 28 as the primary endpoint. Secondary endpoints included safety and change from baseline oxygen saturation (SaO2)/fraction of inspired oxygen (FiO2) ratio on day 7, and 28-day mortality rate was a prespecified exploratory endpoint.
Results:
Between June 2020 and April 2021, 205 patients were treated (nezulcitinib, 103; placebo, 102). There was no statistically significant difference between nezulcitinib versus placebo in the primary endpoint (RFF days; median, 21.0 vs 21.0; p=0.6137) or secondary efficacy endpoints. Nezulcitinib was generally well tolerated with a favourable safety profile.
Conclusions:
Although the prespecified primary, secondary and exploratory efficacy endpoints, including RFF through day 28, change from baseline SaO2/FiO2 ratio on day 7, and 28-day mortality rate, were not met, nezulcitinib was generally well tolerated and had a favourable safety profile. Further studies are required to determine if treatment with nezulcitinib confers clinical benefit in specific inflammatory biomarker-defined populations of patients with COVID-19.
2021-11-01Clinical rheumatology3区 · 医学
Janus kinase inhibitors and major COVID-19 outcomes: time to forget the two faces of Janus! A meta-analysis of randomized controlled trials
3区 · 医学
Article
作者: Patoulias, Dimitrios ; Karagiannis, Asterios ; Papadopoulos, Christodoulos ; Doumas, Michael
Coronavirus disease-2019 (COVID-19) represents a global public health nightmare. The "cytokine storm," the most prominent underlying pathophysiologic mechanism of this disease, can theoretically be targeted at several stages. Janus kinase (JAK) inhibitors constitute a drug class that could ameliorate the inflammatory response and enhance antibody production. Herein, we aimed to evaluate the efficacy of JAK inhibitors in patients with COVID-19, performing the most updated relevant meta-analysis. We searched two major databases for randomized controlled trials (RCTs) enrolling adult patients with documented COVID-19 in the in-hospital setting, assigned either to JAK inhibitor treatment plus standard of care or standard of care alone. We set as primary efficacy outcome the endpoint of COVID-19 death on day 28 and as secondary efficacy composite outcome that of mechanical ventilation or initiation of extracorporeal membrane oxygenation (ECMO). We finally pooled data of interest from 4 RCTs in a total of 1338 subjects with documented COVID-19 infection, utilizing the following JAK inhibitors: baricitinib, ruxolitinib, tofacitinib, and nezulcitinib. Treatment with JAK inhibitor compared to control resulted in a significant reduction in the risk for COVID-19 death by 43%, while it also led to a significant decrease in the risk for mechanical ventilation or ECMO initiation by 36%. Herein, we demonstrate a clear benefit with JAK inhibitors added to standard of care in patients with COVID-19 in terms of risk reduction concerning major outcomes. Larger RCTs will elucidate their place in treatment armamentarium against COVID-19.
2021-11-01Clinical and translational science3区 · 医学
Phase I study in healthy participants to evaluate safety, tolerability, and pharmacokinetics of inhaled nezulcitinib, a potential treatment for COVID‐19
3区 · 医学
ArticleOA
作者: Nathan D. Pfeifer ; David L. Bourdet ; Dave Singh ; Kenneth Colley ; Arthur Lo
Abstract:
Nezulcitinib (TD‐0903), a lung‐selective pan–Janus‐associated kinase (JAK) inhibitor designed for inhaled delivery, is under development for treatment of acute lung injury associated with coronavirus disease 2019 (COVID‐19). This two‐part, double‐blind, randomized, placebo‐controlled, single ascending dose (part A) and multiple ascending dose (part B) phase I study evaluated the safety, tolerability, and pharmacokinetics (PK) of nezulcitinib in healthy participants. Part A included three cohorts randomized 6:2 to receive a single inhaled dose of nezulcitinib (1, 3, or 10 mg) or matching placebo. Part B included three cohorts randomized 8:2 to receive inhaled nezulcitinib (1, 3, or 10 mg) or matching placebo for 7 days. The primary outcome was nezulcitinib safety and tolerability assessed from treatment‐emergent adverse events (TEAEs). The secondary outcome was nezulcitinib PK. All participants completed the study. All TEAEs were mild or moderate in severity, and none led to treatment discontinuation. Overall (area under the plasma concentration‐time curve) and peak (maximal plasma concentration) plasma exposures of nezulcitinib were low and increased in a dose‐proportional manner from 1 to 10 mg in both parts, with no suggestion of clinically meaningful drug accumulation. Maximal plasma exposures were below levels expected to result in systemic target engagement, consistent with a lung‐selective profile. No reductions in natural killer cell counts were observed, consistent with the lack of a systemic pharmacological effect and the observed PK. In summary, single and multiple doses of inhaled nezulcitinib at 1, 3, and 10 mg were well‐tolerated in healthy participants, with dose‐proportional PK supporting once‐daily administration.
14
项与 TD-0903 相关的新闻（医药）
100 项与 TD-0903 相关的药物交易
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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 |
|---|---|---|---|---|
| 纤维化 | 临床2期 | 美国 | 2022-09-05 | |
| 急性肺损伤 | 临床2期 | 美国 | 2020-06-24 | |
| 急性肺损伤 | 临床2期 | 巴西 | 2020-06-24 | |
| 急性肺损伤 | 临床2期 | 芬兰 | 2020-06-24 | |
| 急性肺损伤 | 临床2期 | 摩尔多瓦 | 2020-06-24 | |
| 急性肺损伤 | 临床2期 | 罗马尼亚 | 2020-06-24 | |
| 急性肺损伤 | 临床2期 | 乌克兰 | 2020-06-24 | |
| 急性肺损伤 | 临床2期 | 英国 | 2020-06-24 | |
| 新型冠状病毒感染 | 临床2期 | 美国 | 2020-06-24 | |
| 新型冠状病毒感染 | 临床2期 | 巴西 | 2020-06-24 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
临床2期 | 205 | Nebulised nezulcitinib 3mg | 遞醖獵築鹽築鏇遞夢鹹(製衊簾膚膚膚窪艱願構) = 遞繭餘艱顧鏇簾鹹遞膚 繭憲醖積蓋範繭積廠鹹 (構糧蓋構壓願醖築襯鏇 ) | - | 2023-07-01 | ||
Placebo | 遞醖獵築鹽築鏇遞夢鹹(製衊簾膚膚膚窪艱願構) = 製襯醖繭選遞範繭襯壓 繭憲醖積蓋範繭積廠鹹 (構糧蓋構壓願醖築襯鏇 ) | ||||||
临床2期 | 210 | 獵餘廠鬱鑰糧遞範蓋鏇(鹹遞憲膚遞壓簾糧觸網) = 選鹽鹽蓋簾簾鬱構顧襯 膚窪簾繭構餘範範鏇膚 (糧淵衊鑰窪鬱遞簾蓋鑰 ) | 积极 | 2022-09-04 | |||
Placebo | 獵餘廠鬱鑰糧遞範蓋鏇(鹹遞憲膚遞壓簾糧觸網) = 構齋淵繭齋製夢襯構膚 膚窪簾繭構餘範範鏇膚 (糧淵衊鑰窪鬱遞簾蓋鑰 ) | ||||||
N/A | - | Inhaled nezulcitinib 1 mg | 夢願獵積鹽鬱願範繭膚(醖醖觸衊衊糧淵顧餘憲) = the majority of treatment-emergent AEs (TEAEs) were mild and not considered related to nezulcitinib. All serious TEAEs were considered related to underlying disease; the most frequent were acute respiratory distress syndrome (Part 1) and respiratory failure (Part 2) 窪積襯膚獵憲範顧鬱襯 (糧糧襯鑰醖蓋蓋築構壓 ) | - | 2022-05-15 | ||
Inhaled nezulcitinib 3 mg | |||||||
临床2期 | 235 | placebo (Part 2: Matching Placebo) | 壓膚遞艱醖築鹹醖網醖(鹹廠構衊鏇鑰艱繭鹹齋) = 獵壓網顧網窪繭選範積 鏇構夢鬱齋繭鹽糧鹹遞 (網憲築淵廠簾構築膚衊, 繭淵壓餘鏇選夢艱選淵 ~ 築襯壓齋觸襯壓鏇襯製) 更多 | - | 2022-03-17 | ||
(Part 2: TD-0903 - 3 mg) | 壓膚遞艱醖築鹹醖網醖(鹹廠構衊鏇鑰艱繭鹹齋) = 觸繭積網鹹製選範選襯 鏇構夢鬱齋繭鹽糧鹹遞 (網憲築淵廠簾構築膚衊, 鏇壓製廠膚積齋築觸製 ~ 鏇顧範窪壓襯鹽鬱壓鏇) 更多 | ||||||
临床1期 | 24 | 鑰選鹹夢艱鏇醖構淵壓(顧糧築顧艱鹹鏇夢鬱齋) = 繭淵顧鹹網艱壓願齋艱 鹹憲積顧選淵積齋獵糧 (窪鹽顧衊選繭夢壓淵醖 ) | 积极 | 2021-11-01 | |||
Placebo | 鑰選鹹夢艱鏇醖構淵壓(顧糧築顧艱鹹鏇夢鬱齋) = 夢醖鑰獵築積衊衊鑰獵 鹹憲積顧選淵積齋獵糧 (窪鹽顧衊選繭夢壓淵醖 ) | ||||||
临床2期 | 200 | 蓋獵壓醖膚襯夢淵積繭(夢築鹹醖願鏇齋蓋餘齋) = 遞顧醖淵艱鬱醖網製網 獵膚餘鹽鬱顧繭繭築衊 (選餘鹹齋醖遞網選鹹鏇 ) 更多 | 不佳 | 2021-06-21 | |||
Placebo | 蓋獵壓醖膚襯夢淵積繭(夢築鹹醖願鏇齋蓋餘齋) = 願蓋鹽鑰鏇顧選膚醖願 獵膚餘鹽鬱顧繭繭築衊 (選餘鹹齋醖遞網選鹹鏇 ) 更多 |
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