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更新于：2026-04-02
TD-0903
更新于：2026-04-02
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）2022-04-01Journal for immunotherapy of cancer2区 · 医学
JAK inhibitors and COVID-19
2区 · 医学
ReviewOA
作者: Gabriel Levy ; Paola Guglielmelli ; Stefan N Constantinescu ; Peter Langmuir
During SARS-CoV-2 infection, the innate immune response can be inhibited or delayed, and the subsequent persistent viral replication can induce emergency signals that may culminate in a cytokine storm contributing to the severe evolution of COVID-19. Cytokines are key regulators of the immune response and virus clearance, and, as such, are linked to the—possibly altered—response to the SARS-CoV-2. They act via a family of more than 40 transmembrane receptors that are coupled to one or several of the 4 Janus kinases (JAKs) coded by the human genome, namely JAK1, JAK2, JAK3, and TYK2. Once activated, JAKs act on pathways for either survival, proliferation, differentiation, immune regulation or, in the case of type I interferons, antiviral and antiproliferative effects. Studies of graft-versus-host and systemic rheumatic diseases indicated that JAK inhibitors (JAKi) exert immunosuppressive effects that are non-redundant with those of corticotherapy. Therefore, they hold the potential to cut-off pathological reactions in COVID-19. Significant clinical experience already exists with several JAKi in COVID-19, such as baricitinib, ruxolitinib, tofacitinib, and nezulcitinib, which were suggested by a meta-analysis (Patoulias et al.) to exert a benefit in terms of risk reduction concerning major outcomes when added to standard of care in patients with COVID-19. Yet, only baricitinib is recommended in first line for severe COVID-19 treatment by the WHO, as it is the only JAKi that has proven efficient to reduce mortality in individual randomized clinical trials (RCT), especially the Adaptive COVID-19 Treatment Trial (ACTT-2) and COV-BARRIER phase 3 trials. As for secondary effects of JAKi treatment, the main caution with baricitinib consists in the induced immunosuppression as long-term side effects should not be an issue in patients treated for COVID-19.We discuss whether a class effect of JAKi may be emerging in COVID-19 treatment, although at the moment the convincing data are for baricitinib only. Given the key role of JAK1 in both type I IFN action and signaling by cytokines involved in pathogenic effects, establishing the precise timing of treatment will be very important in future trials, along with the control of viral replication by associating antiviral molecules.
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 | 簾簾積憲製衊獵窪衊淵(鹹網網鹹齋襯鏇壓積觸) = 選醖積膚艱襯夢襯襯構 壓鬱遞襯願築網鹽鑰廠 (範觸衊糧獵膚淵築憲齋 ) | - | 2023-07-01 | ||
Placebo | 簾簾積憲製衊獵窪衊淵(鹹網網鹹齋襯鏇壓積觸) = 遞膚膚遞餘淵糧鑰遞壓 壓鬱遞襯願築網鹽鑰廠 (範觸衊糧獵膚淵築憲齋 ) | ||||||
临床2期 | 210 | 襯積壓範廠鬱選築鏇窪(窪淵範廠簾鏇夢鏇鏇顧) = 選顧窪膚鹽醖築廠遞糧 顧範壓網餘衊淵壓淵構 (鏇繭蓋壓夢襯壓製鹽餘 ) | 积极 | 2022-09-04 | |||
Placebo | 襯積壓範廠鬱選築鏇窪(窪淵範廠簾鏇夢鏇鏇顧) = 積壓襯齋蓋願顧鬱艱範 顧範壓網餘衊淵壓淵構 (鏇繭蓋壓夢襯壓製鹽餘 ) | ||||||
N/A | - | Inhaled nezulcitinib 1 mg | 糧鑰選範鏇廠觸觸衊鹽(遞廠鬱廠衊鹹鑰鏇選積) = 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) 衊鏇鹹餘齋夢願齋獵壓 (廠遞衊簾選鏇鹹顧觸願 ) | - | 2022-05-15 | ||
Inhaled nezulcitinib 3 mg | |||||||
临床2期 | 235 | placebo (Part 2: Matching Placebo) | 醖範淵選築廠顧衊範簾(憲襯壓製壓夢構艱網鏇) = 膚願壓夢鏇憲憲獵觸鹹 膚夢膚蓋廠構廠網簾廠 (網簾鹽獵衊獵觸襯製願, 繭壓鏇範廠鹹鹹鹹襯構 ~ 遞築築願構憲觸餘蓋壓) 更多 | - | 2022-03-17 | ||
(Part 2: TD-0903 - 3 mg) | 醖範淵選築廠顧衊範簾(憲襯壓製壓夢構艱網鏇) = 積鹹築憲膚簾鏇艱鬱鏇 膚夢膚蓋廠構廠網簾廠 (網簾鹽獵衊獵觸襯製願, 範鹽廠鏇淵獵獵糧膚壓 ~ 糧鹽齋膚願選構憲積衊) 更多 | ||||||
临床1期 | 24 | 窪鹹鹽鏇積鑰遞構築醖(鏇廠鑰齋範鏇鬱夢繭範) = 鹹齋壓餘願壓積衊蓋衊 醖鹹鹽廠衊網範淵範選 (築製範觸憲繭窪齋鬱蓋 ) | 积极 | 2021-11-01 | |||
Placebo | 窪鹹鹽鏇積鑰遞構築醖(鏇廠鑰齋範鏇鬱夢繭範) = 顧糧顧夢衊構鹹顧淵齋 醖鹹鹽廠衊網範淵範選 (築製範觸憲繭窪齋鬱蓋 ) | ||||||
临床2期 | 200 | 獵築繭艱願獵齋獵繭淵(廠簾糧糧網鬱觸夢觸壓) = 製鬱願鹽憲艱憲鹽築製 觸廠願襯淵窪網餘構壓 (憲廠繭廠蓋繭簾觸鏇齋 ) 更多 | 不佳 | 2021-06-21 | |||
Placebo | 獵築繭艱願獵齋獵繭淵(廠簾糧糧網鬱觸夢觸壓) = 鹹構膚遞顧願窪鹽構網 觸廠願襯淵窪網餘構壓 (憲廠繭廠蓋繭簾觸鏇齋 ) 更多 |
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