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阿普司特治疗银屑病和银屑病关节炎。

Apremilast in the treatment of psoriasis and psoriatic arthritis.

作者信息

Gooderham M, Papp K

机构信息

Skin Centre for Dermatology, Peterborough, ON, Canada; Probity Medical Research, Waterloo, ON, Canada.

K. Papp Clinical Research, Waterloo, ON, Canada; Probity Medical Research, Waterloo, ON, Canada.

出版信息

Skin Therapy Lett. 2015 Sep-Oct;20(5):1-6.

Abstract

Phosphodiesterase 4 (PDE4) is a key enzyme in the regulation of immune responses of inflammatory diseases through degradation of the second messenger, cyclic adenosine 3',5'-monophosphate (cAMP). Apremilast, a selective PDE4 inhibitor, has been shown to reduce the production of pro-inflammatory cytokines by increasing intracellular levels of cAMP and promoting the production of anti-inflammatory cytokines. The efficacy and safety of apremilast in the treatment of psoriasis and psoriatic arthritis has been demonstrated in phase 2 and 3 studies and will be reviewed here. Across all studies, treatment was generally well-tolerated with some mild gastrointestinal complaints that occurred early and resolved over time, resulting in few drop-outs. Meaningful changes in dactylitis and enthesitis were also observed. Routine monitoring is not required given the absence of drug associated physiologic, biochemical, and haematological changes. Apremilast proves to be a new promising systemic therapy for treating psoriatic disease.

摘要

磷酸二酯酶4(PDE4)是通过降解第二信使环磷酸腺苷(cAMP)来调节炎症性疾病免疫反应的关键酶。阿普斯特是一种选择性PDE4抑制剂,已显示可通过提高细胞内cAMP水平和促进抗炎细胞因子的产生来减少促炎细胞因子的产生。阿普斯特治疗银屑病和银屑病关节炎的疗效和安全性已在2期和3期研究中得到证实,本文将对此进行综述。在所有研究中,治疗一般耐受性良好,早期出现一些轻度胃肠道不适,但随着时间推移会缓解,导致停药的情况很少。还观察到指(趾)炎和附着点炎有显著改善。鉴于未出现与药物相关的生理、生化和血液学变化,无需进行常规监测。阿普斯特被证明是一种治疗银屑病疾病的有前景的新型全身疗法。

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