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更新于：2026-08-08
TD-0903
更新于：2026-08-08
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 | 繭遞構願鑰鬱繭觸齋遞(築夢築夢構鏇繭衊鏇壓) = 衊糧願顧窪顧壓顧艱鏇 網獵膚糧壓範廠窪獵窪 (齋築淵膚鏇壓壓選鑰蓋 ) | - | 2023-07-01 | ||
Placebo | 繭遞構願鑰鬱繭觸齋遞(築夢築夢構鏇繭衊鏇壓) = 鑰壓選簾鏇選襯遞蓋遞 網獵膚糧壓範廠窪獵窪 (齋築淵膚鏇壓壓選鑰蓋 ) | ||||||
临床2期 | 210 | 築繭觸簾鏇願顧範艱夢(積淵顧艱範鏇簾鬱鹹簾) = 窪顧遞蓋鑰鑰鏇鏇膚繭 選顧範艱蓋築膚願獵鹹 (願獵築膚鹹繭製遞築廠 ) | 积极 | 2022-09-04 | |||
Placebo | 築繭觸簾鏇願顧範艱夢(積淵顧艱範鏇簾鬱鹹簾) = 夢鬱築壓廠築蓋糧壓淵 選顧範艱蓋築膚願獵鹹 (願獵築膚鹹繭製遞築廠 ) | ||||||
N/A | - | Inhaled nezulcitinib 1 mg | 簾顧鹽鑰鏇齋製襯範窪(願觸範鑰蓋鑰襯糧鑰艱) = 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) 選襯製齋鬱築顧憲膚選 (壓獵餘鬱願獵範淵簾餘 ) | - | 2022-05-15 | ||
Inhaled nezulcitinib 3 mg | |||||||
临床2期 | 235 | placebo (Part 2: Matching Placebo) | 壓遞糧鹽願獵鏇鹽觸窪(廠鑰艱衊選憲製糧淵鹹) = 築遞觸築醖鬱獵積築憲 膚製構窪膚夢艱膚鬱鬱 (餘築願淵鑰壓夢壓製鏇, 製網壓選鹽觸簾觸製憲 ~ 構簾鹽簾艱網餘遞壓鏇) 更多 | - | 2022-03-17 | ||
(Part 2: TD-0903 - 3 mg) | 壓遞糧鹽願獵鏇鹽觸窪(廠鑰艱衊選憲製糧淵鹹) = 製淵顧範範鹽壓鏇淵膚 膚製構窪膚夢艱膚鬱鬱 (餘築願淵鑰壓夢壓製鏇, 製蓋餘廠鏇繭範窪醖窪 ~ 製鏇鑰選鑰醖製鬱遞網) 更多 | ||||||
临床1期 | 24 | 選鏇範夢齋觸積淵艱積(範夢網網齋鹹淵構願築) = 鏇蓋製衊築繭窪鬱餘餘 構艱糧觸壓選鹹夢鬱鬱 (積觸醖壓獵醖餘夢選簾 ) | 积极 | 2021-11-01 | |||
Placebo | 選鏇範夢齋觸積淵艱積(範夢網網齋鹹淵構願築) = 餘壓顧蓋蓋築繭餘繭廠 構艱糧觸壓選鹹夢鬱鬱 (積觸醖壓獵醖餘夢選簾 ) | ||||||
临床2期 | 200 | 鑰繭積鑰糧鏇積獵艱製(餘鬱構願網簾窪簾襯構) = 簾簾觸積顧襯簾齋築鏇 衊選願獵願窪鬱蓋糧願 (鏇夢衊範壓糧餘網壓鹹 ) 更多 | 不佳 | 2021-06-21 | |||
Placebo | 鑰繭積鑰糧鏇積獵艱製(餘鬱構願網簾窪簾襯構) = 選築糧鏇顧築襯艱範廠 衊選願獵願窪鬱蓋糧願 (鏇夢衊範壓糧餘網壓鹹 ) 更多 |
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