预约演示
更新于：2026-09-04
Londamocitinib
更新于：2026-09-04
概要
基本信息
原研机构 |
在研机构 |
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C28H31F2N7O4S |
InChIKeyJNUZADQZHYFJGW-JOCHJYFZSA-N |
CAS号2241039-81-4 |
关联
6
项与 Londamocitinib 相关的临床试验NCT06732882
A Phase Ib, Multicentre, Randomised, Single-blind, Parallel-group, Placebo-controlled, Study to Characterise the Pharmacokinetics and Pharmacodynamics of AZD4604 Administered Via the Turbuhaler® Device in Adults With Mild Asthma
NCT06435273
A Randomised, Double-blind, Parallel Group, Placebo Controlled, 4-Week, Phase II Study to Evaluate the Effect of AZD4604 on Airway Inflammation and Biomarkers in Adults With Asthma
NCT06519968
A Single-blind, Randomised, Placebo-controlled Study to Investigate the Safety, Tolerability, and Pharmacokinetics of Inhaled AZD4604 Following Single Ascending and Multiple Doses in Healthy Japanese and Chinese Participants
100 项与 Londamocitinib 相关的临床结果
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100 项与 Londamocitinib 相关的转化医学
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100 项与 Londamocitinib 相关的专利（医药）
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5
项与 Londamocitinib 相关的文献（医药）2026-04-01JOURNAL OF ALLERGY AND CLINICAL IMMUNOLOGY
First-in-human study for londamocitinib (AZD4604), an inhaled selective JAK1 inhibitor
Article
作者: Belvisi, Maria G ; Platt, Adam ; Konstantinidis, Kyriakos V ; Dosanjh, Davinder P S ; Keen, Christina ; Nemes, Szilárd ; Riff, Camille ; Forte Soto, Pablo ; Hughes, Rod ; Singh, Dave ; Chetty, Rajkumar ; Jellesmark Jensen, Tina ; Jevnikar, Zala ; Mo, John ; Lund, Julia ; Zingmark, Pernilla ; Mäenpää, Jukka
BACKGROUND:
Janus kinase (JAK) 1 is a promising target for asthma treatment; it may address inflammation not controlled by inhaled corticosteroids. Londamocitinib (AZD4604) is a selective JAK1 inhibitor designed for inhaled delivery.
OBJECTIVE:
A 3-part randomized placebo-controlled phase 1 study (NCT04769869) was conducted in healthy volunteers (n = 85) and participants with mild asthma (n = 18) investigating safety, tolerability, pharmacokinetics, and lung and systemic target engagement of londamocitinib.
METHODS:
Single (0.025-6 mg) and multiple (0.4-3 mg, inhaled) doses of londamocitinib were administered to healthy volunteers and participants with mild asthma for up to 10 days. Effect on fractional exhaled nitric oxide (Feno), a type 2 inflammation marker, was assessed in participants with mild asthma with elevated Feno.
RESULTS:
Londamocitinib was well tolerated after single and multiple dosing. After inhalation, londamocitinib was quickly absorbed, and systemic exposure increased approximate dose proportionally. After twice-daily dosing to obtain steady state, 2- to 4-fold accumulation was observed. Approximately 50% reductions in mean Feno were seen for 1.4 and 3 mg doses of londamocitinib in participants with mild asthma after 3 days, which persisted to day 10 of dosing, versus no significant reduction with placebo. Transient, minimal suppression of systemic target engagement (IL-4-induced STAT6 phosphorylation in peripheral CD3+ T cells) was seen with the 3 mg but not the 1.4 mg londamocitinib dose.
CONCLUSION:
Twice-daily administration of londamocitinib provides rapid and effective reduction of Feno in patients with mild asthma with elevated Feno.
2026-03-01BMJ Open Respiratory Research
Phase 2a randomised, double-blind, placebo-controlled study to evaluate the efficacy and safety of londamocitinib (AZD4604) two times per day for 12 weeks in adult patients with moderate-to-severe asthma uncontrolled on medium-high-dose ICS-LABA
Article
作者: Kocks, Janwillem W H ; Nemes, Szilárd ; Hughes, Rod ; Mustapa, Mohd Nubli ; Dosanjh, Davinder P ; Jevnikar, Zala ; Jensen, Tina J ; Jonsson, Julia ; Adams, Amanda ; Belvisi, Maria G ; Konstantinidis, Kyriakos V ; Akuthota, Praveen ; Jones, Michael
Introduction:
Asthma is a heterogeneous condition and affected individuals show variable responses to available medications. An unmet need exists for add-on therapies that target novel molecular pathways, before patients escalate to biologics. Janus kinase 1 (JAK1) is implicated in multiple inflammatory cytokine pathways critical for the pathogenesis of asthma. Londamocitinib (AZD4604) is a highly specific, inhaled, JAK1 inhibitor with high potency to block multiple JAK1-dependent signalling pathways. AJAX is a phase 2a, randomised, double-blind, partially decentralised placebo-controlled study assessing the efficacy, safety and pharmacokinetics (PK) of londamocitinib in adults with moderate-to-severe asthma uncontrolled on medium-to-high-dose inhaled corticosteroid/long-acting β
2
-agonist.
Methods and analysis:
The primary endpoint is time to first CompEx Asthma event. Secondary endpoints include change from baseline in prebronchodilator forced expiratory volume in 1 s, chronic airways assessment test, six-item asthma control questionnaire, daily asthma symptom score, and morning and evening peak expiratory flow at weeks 4 and 12. In addition, assessment of the effect of londamocitinib on airway inflammation as measured by the fractional exhaled nitric oxide test; cough severity assessment; and the PK of londamocitinib in all participants after 4 and 12 weeks will also be evaluated.
Ethics and dissemination:
The study has received ethical approval from the appropriate ethic committee and will be conducted in accordance with the Declaration of Helsinki, Good Clinical Practice guidelines, and all applicable regulatory requirements. All participants will provide written informed consent prior to enrolment, with procedures in place to ensure comprehension and voluntary participation. Findings will be disseminated through peer‑reviewed publications and/or presentations at scientific conferences. Summary results will be posted on the trial registry and shared with participants and relevant patient groups in lay summaries.
2023-10-12Journal of medicinal chemistry1区 · 医学
Discovery of the Potent and Selective Inhaled Janus Kinase 1 Inhibitor AZD4604 and Its Preclinical Characterization
1区 · 医学
Article
作者: Wennberg, Tiiu ; Berglund, Susanne ; Collins, Mia ; Nilsson, Magnus ; Su, Qibin ; Smailagic, Amir ; Berggren, Kristina ; Cerboni, Silvia ; Johansson, Johan R. ; Hendrickx, Ramon ; Wu, Allan ; Rhedin, Magdalena ; Lepistö, Matti ; Grimster, Neil P. ; Dahl, Göran ; Kettle, Jason G. ; Naessens, Thomas ; Mitra, Suman ; Österlund, Torben ; Elmqvist, David
JAK-STAT cytokines are critical in regulating immunity. Persistent activation of JAK-STAT signaling pathways by cytokines drives chronic inflammatory diseases such as asthma. Herein, we report on the discovery of a highly JAK1-selective, ATP-competitive series of inhibitors having a 1000-fold selectivity over other JAK family members and the approach used to identify compounds suitable for inhaled administration. Ultimately, compound 16 was selected as the clinical candidate, and upon dry powder inhalation, we could demonstrate a high local concentration in the lung as well as low plasma concentrations, suggesting no systemic JAK1 target engagement. Compound 16 has progressed into clinical trials. Using 16, we found JAK1 inhibition to be more efficacious than JAK3 inhibition in IL-4-driven Th2 asthma.
100 项与 Londamocitinib 相关的药物交易
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外链
| KEGG | Wiki | ATC | Drug Bank |
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| D13040 | - | - | - |
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 |
|---|---|---|---|---|
| 气管炎 | 临床2期 | 加拿大 | 2024-08-05 | |
| 气管炎 | 临床2期 | 丹麦 | 2024-08-05 | |
| 气管炎 | 临床2期 | 德国 | 2024-08-05 | |
| 气管炎 | 临床2期 | 西班牙 | 2024-08-05 | |
| 气管炎 | 临床2期 | 英国 | 2024-08-05 | |
| 哮喘 | 临床2期 | 美国 | 2023-11-16 | |
| 哮喘 | 临床2期 | 阿根廷 | 2023-11-16 | |
| 哮喘 | 临床2期 | 巴西 | 2023-11-16 | |
| 哮喘 | 临床2期 | 保加利亚 | 2023-11-16 | |
| 哮喘 | 临床2期 | 丹麦 | 2023-11-16 |
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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1期 | 14 | Londamocitinib 1400 μg via Turbuhaler | 繭醖製淵襯鑰簾遞糧窪(獵齋觸襯範餘淵衊艱壓) = 壓鑰積選糧鬱簾網憲顧 鏇願廠獵鑰願淵醖積範 (蓋顧選淵醖願憲艱鏇構, 16.52) 更多 | 积极 | 2026-05-15 | ||
Londamocitinib 1400 μg via Genuair | 繭醖製淵襯鑰簾遞糧窪(獵齋觸襯範餘淵衊艱壓) = 壓築鹹願襯鏇範積襯顧 鏇願廠獵鑰願淵醖積範 (蓋顧選淵醖願憲艱鏇構, 13.42) 更多 | ||||||
临床1期 | 轻度哮喘 fractional exhaled nitric oxide (FeNO) | - | 餘積蓋構膚壓憲蓋鑰襯(夢醖積獵醖構繭鑰願窪) = 鹹顧鬱壓襯簾憲願憲製 夢選蓋選簾構簾築憲衊 (網願選膚廠範繭壓顧鏇 ) | 积极 | 2024-02-23 |
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