Apremilast is a phosphodiesterase 4 (PDE4) inhibitor that reduces pro-inflammatory cytokine production. Recent studies demonstrate upregulation of PDE4 in human scalp lesions of AA patients and hair regrowth in a humanized AA mouse model upon apremilast treatment, suggesting a possible potential of apremilast in AA.

Apremilast is an inhibitor of the phosphodiesterase 4 (PDE4), which reduces inflammation. PDE4 has been found to be expressed in patients suffering with AA. There have been variable results reported in the literature up till now, including good hair regrowth and a study showing no treatment response. The main side effects are diarrhea, headache ...

2023年5月10日 · 磷酸二酯酶4 (phosphodiesterase4, PDE4)是磷酸二酯酶家族中重要成员之一，可特异性水解环磷酸腺苷 (cyclic adenosine monophosphate, cAMP)，通过改变cAMP浓度引发下游磷酸化级联反应，与多种疾病密切相关。 靶向PDE4的抑制剂临床研究包括呼吸系统疾病、自身免疫性疾病、中枢神经系统疾病及皮肤病等多种疾病领域。 但是在已上市的PDE4抑制剂临床研究中发现，大多数药物的恶心、呕吐等胃肠道不良反应发生率较高，限制了其临床应用。

A phosphodiesterase-4 inhibitor, commonly referred to as a PDE4 inhibitor, is a drug used to block the degradative action of phosphodiesterase 4 (PDE4) on cyclic adenosine monophosphate (cAMP). It is a member of the larger family of PDE inhibitors .

The present pilot study aimed to probe the efficacy of candidate anti-AA agent in the humanized mouse model of AA, the immunoinhibitory phosphodiesterase (PDE) 4 blocker, apremilast. Apremilast is a novel, orally administered small molecule that specifically targets PDE4 and

Apremilast, an oral small molecule inhibitor of phosphodiesterase 4 (PDE4), is in development for chronic inflammatory disorders, and has shown efficacy in psoriasis, psoriatic arthropathies, and Behçet's syndrome. In March 2014, the US Food and …

2021年1月1日 · Apremilast, a PDE4 inhibitor, has been approved by the US Food and Drug Administration (FDA) for the treatment of active psoriatic arthritis and moderate-to-severe plaque psoriasis since 2014 . As mentioned before, PDE4 is increased in AA lesions. A humanised mouse model of AA analysed the effect of apremilast on pro-inflammatory mediators.

2017年6月23日 · PDE4 is highly increased in human AA scalp lesions , representing a potential therapeutic target. Apremilast, an oral, small molecule PDE antagonist is FDA-approved for psoriasis and psoriatic arthritis, and is currently tested in AD patients.

2023年6月24日 · 治疗copd的pde4抑制剂和pde3/4双重抑制剂. pde4酶在与炎症反应相关的细胞中高度表达，包括嗜酸性粒细胞、单核细胞、巨噬细胞、肺动脉平滑肌细胞、气道上皮细胞和平滑肌细胞。因此，选择性pde4抑制剂能够抑制多种炎症细胞功能，并在治疗copd方面找到了应用。

2024年5月31日 · 在治疗AD方面，PDE4抑制剂展现出了显著的效果，因此，许多制药公司都将PDE4视为治疗慢性炎症相关疾病的关键靶点。 AmBeed持续跟踪PDE4靶点相关研究动向，本篇为读者就作用机制与抑制剂做一个综合性的解读。 特异性皮炎（Atopic Dermatitis，AD）是一种慢性、瘙痒性、炎症性皮肤病。 AD患者每天都被迫进入瘙痒-搔抓-更痒的恶性循环，进而损害皮肤屏障功能，加剧炎症发生，严重影响患者的身心健康和生活质量。 流行病研究显示 [1]，全球AD患 …