Department of Clinical and Molecular Medicine, S. Andrea University Hospital, "Sapienza" University, 00189 Rome, Italy.
Reumatologia, Dipartimento di Scienze Cliniche Internistiche, Anestesiologiche e Cardiovascolari, "Sapienza" Università di Roma, 00161 Rome, Italy.
Int J Mol Sci. 2021 Mar 5;22(5):2638. doi: 10.3390/ijms22052638.
Phosphodiesterases (PDEs) are a heterogeneous superfamily of enzymes which catalyze the degradation of the intracellular second messengers cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP). Among PDEs, PDE4 is the most widely studied and characterized isoenzyme. PDE4 blocking can lead to increased levels of intracellular cAMP, which results in down-regulation of inflammatory responses by reducing the expression of tumor necrosis factor (TNF), interleukin (IL)-23, IL-17, interferon-γ, while increasing regulatory cytokines, such as IL-10. Therefore, PDE4 has been explored as a therapeutic target for the treatment of different chronic inflammatory conditions such as psoriatic arthritis (PsA) and inflammatory bowel disease (IBD). PsA shares clinical, genetic, and pathogenic features with IBD such as ulcerative colitis (UC) and Crohn's disease (CD), and enteropathic spondyloarthritis (eSpA) represent a frequent clinical evidence of the overlap between gut and joint diseases. Current therapeutic options in PsA patients and underlying UC are limited to synthetic immunosuppressants and anti-TNF. Apremilast is an oral PDE4 inhibitor approved for the treatment of active PsA patients with inadequate response to synthetic immunosuppressants. The efficacy and a good safety profile observed in randomized clinical trials with apremilast in PsA patients have been confirmed by few studies in a real-life scenario. In addition, apremilast led to significant improvement in clinical and endoscopic features in UC patients in a phase II RCT. By now there are no available data regarding its role in eSpA patients. In view of the above, the use of apremilast in eSpA patients is a route that deserves to be deepened.
磷酸二酯酶(PDEs)是一个异构超家族的酶,其催化细胞内第二信使环磷酸腺苷(cAMP)和环鸟苷酸(cGMP)的降解。在 PDEs 中,PDE4 是研究最广泛和特征最明确的同工酶。PDE4 阻断可导致细胞内 cAMP 水平升高,从而通过减少肿瘤坏死因子(TNF)、白细胞介素(IL)-23、IL-17、干扰素-γ的表达,下调炎症反应,同时增加调节细胞因子,如 IL-10。因此,PDE4 已被探索作为治疗不同慢性炎症性疾病的治疗靶点,如银屑病关节炎(PsA)和炎症性肠病(IBD)。PsA 与 IBD 如溃疡性结肠炎(UC)和克罗恩病(CD)具有临床、遗传和发病特征,肠病性脊柱关节炎(eSpA)是肠病和关节病重叠的常见临床证据。目前 PsA 患者和潜在 UC 的治疗选择仅限于合成免疫抑制剂和抗 TNF。阿普米司特是一种口服 PDE4 抑制剂,批准用于治疗对合成免疫抑制剂反应不足的活动性 PsA 患者。阿普米司特在 PsA 患者中的随机临床试验中观察到的疗效和良好的安全性概况已被少数真实世界研究证实。此外,阿普米司特在 II 期 RCT 中导致 UC 患者的临床和内镜特征显著改善。到目前为止,尚无关于其在 eSpA 患者中的作用的可用数据。鉴于上述情况,阿普米司特在 eSpA 患者中的应用值得进一步研究。