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A Phase IIa, Proof of Concept Study to Evaluate the Reduction in Inflammatory Biomarkers and Assess Airway Function Following Administration of IMD-1041 in Patients With Chronic Obstructive Pulmonary Disease (COPD)

COPD is a lung disease in which the lung is damaged, making it hard to breathe. In COPD, the airways/tubes that carry air in and out of the lungs are partly obstructed, making it difficult to get air in and out. COPD gets gradually worse over time. At the moment there is no cure for COPD. The best way to slow the disease is to stop smoking. Current medications are used to alleviate shortness of breath and cough, and to treat infections of the lungs that can worsen COPD.
Institute of Medicinal Molecular Design, Inc. (IMMD), a Japanese Drug Discovery Company is developing a compound code named IMD-1041. IMD-1041 is an investigational drug, meaning it is not yet on the market. It is an IKKb inhibitor developed for the treatment of COPD. Unlike most other medications used for COPD currently, IMD-1041 is in capsule form and needs to be taken twice a day. It is also unlike all other drugs in use because it treats the underlying cause of the symptoms.
The purpose of this study is to see if IMD-1041 has the ability to reduce inflammatory derived symptoms and airway remodelling (changes) by looking at certain changes in chemical levels in the blood and sputum (phlegm).

开始日期2008-07-01

申办/合作机构

IMMD, Inc.

EUCTR2008-001889-81-GB / Not yet recruitingN/A

A Phase IIa, Proof of Concept Study to Evaluate the Reduction in Inflammatory Biomarkers and Assess Airway Function Following Administration of IMD-1041 in Patients with Chronic Obstructive Pulmonary Disease (COPD)

开始日期2008-06-24

申办/合作机构

IMMD, Inc.

EUCTR2007-000190-28-GB / Not yet recruitingN/A

A Single Centre, Double-blind, Randomised Study To Investigate a Single Oral Dose of IMD-1041 in A Nasal Allergen Challenge (NAC) Model

开始日期2007-03-22

申办/合作机构

IMMD, Inc.

100 项与 IMMD, Inc. 相关的临床结果

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0 项与 IMMD, Inc. 相关的专利（医药）

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42

项与 IMMD, Inc. 相关的文献（医药）

2023-03-01·Bioorganic & Medicinal Chemistry

Discovery and structure-activity relationship study of 2-piperazinyl-benzothiazole derivatives as potent and selective PPARδ agonists

Article

作者: Tokuyama, Ryukou ; Naya, Noriyuki ; Fukasawa, Hiroshi ; Fukao, Keita ; Ohara, Takafumi ; Suzuki, Naoyuki ; Muto, Susumu ; Matsumura, Ken-Ichi ; Kato, Terukazu ; Itai, Akiko

Peroxisome proliferator-activated receptor δ (PPARδ) is considered to be a target for treating metabolic syndrome, whereas there is no PPARδ agonist in clinical use. Previously, we have reported the discovery of 2-(1-piperidinyl)-1,3-benzothiazole derivatives as a new series of PPARδ agonists using docking-based virtual screening techniques. In this study, we performed the further optimization study of the lead compound 1 focusing on improvement of hydrophobic interactions in the binding site to enhance agonist efficacy for PPARδ and subtype selectivity, thereby discovering a novel PPARδ agonist 5g which exhibited high in vitro agonist activity (hPPARδ, EC₅₀ = 4.1 nM) and sufficiently high selectivity ratio over PPARα and PPARγ. Moreover, 5g revealed a significant upregulation of high-density lipoprotein cholesterol level in vivo.

2022-03-01·Bioorganic & Medicinal Chemistry Letters4区 · 医学

Discovery and structure-based design of a new series of potent and selective PPARδ agonists utilizing a virtual screening method

4区 · 医学

Article

作者: Muto, Susumu ; Ohara, Takafumi ; Matsumura, Ken-Ichi ; Mizutani, Miho ; Tokuyama, Ryukou ; Fukasawa, Hiroshi ; Suzuki, Naoyuki ; Itai, Akiko ; Kato, Terukazu

Novel PPARδ agonists, 2-(1-piperidinyl)-1,3-benzothiazole derivatives were discovered by our proprietary docking-based virtual screening technique. Compound 1 as the initial hit was effectively modified to acquire PPARδ agonist activity, resulting in the discovery of compound 12 with high agonistic potency for PPARδ and selectivity over PPARα and PPARγ. Compound 12 also had good ADME profiles and showed in vivo efficacy as a lead.

2019-11-27·Oxidative Medicine and Cellular Longevity2区 · 生物学

IKKβ Inhibitor IMD-0354 Attenuates Radiation Damage in Whole-body X-Irradiated Mice

2区 · 生物学

ArticleOA

作者: Miura, Shuta ; Waga, Kengo ; Itai, Akiko ; Nishida, Teruki ; Kashiwakura, Ikuo ; Yamaguchi, Masaru ; Nakanishi, Reiko

Nuclear factor-kappa B (NF-κB) transcription factor plays a critical role in regulating radiation-induced inflammatory and immune responses. Intracellular reactive oxygen species generation induces the activation of NF-κB via the inhibitor of κB (IκB) kinase (IKK) complex signaling. Previous studies have reported that the inhibition of IKK-driven NF-κB activation offers a therapeutic strategy for managing inflammatory disorders and various cancers, but it has additionally been reported that treatment targeting NF-κB also shows a radioprotective effect. IMD-0354 is an IKKβ inhibitor that blocks IκBα phosphorylation in the NF-κB pathway. This compound is known to exert anti-inflammatory and antitumor effects, but its radioprotective effects are unclear. Therefore, in the present study, we examined whether or not IMD-0354 has a mitigative effect on radiation-induced damages in mice. IMD-0354 was dissolved in soybean oil and subcutaneously administered to C57BL/6J Jcl mice for 3 consecutive days after 7 Gy of whole-body X-irradiation. The survival rate on day 30 and the NF-κB p65 and IκBα in bone marrow and spleen cells based on flow cytometry were assessed. IMD-0354 administration significantly suppressed the lethality induced by whole-body X-irradiation, and the survival rate increased by 83%. The NF-κB p65 and IκBα in bone marrow and spleen cells were significantly lower in IMD-0354-treated mice than in irradiated mice, suggesting that the IKKβ inhibitor IMD-0354 exerts a radiomitigative effect by suppressing the NF-κB.

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药物(靶点)	适应症	全球最高研发状态

IMD-2560 ( IKKβ )	骨质疏松症更多	临床1期
IMD-0354 ( IKKβ x NF-κB )	特应性皮炎更多	临床1期
IMD-4482 ( PAI-1 )	阿尔茨海默症更多	临床前
IMMD-21 ( PPARδ )	动脉粥样硬化更多	临床前
IMD-1041 ( IKKβ x NFKB1 x PAI-1 )	糖尿病并发症更多	临床前