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Drugs. 2017 Mar;77(4):459-472. doi: 10.1007/s40265-017-0709-1.
Apremilast (Otezla) is an orally administered, small molecule inhibitor of phosphodiesterase 4 (PDE4). Apremilast 30 mg twice daily reduced the severity of moderate to severe plaque psoriasis in the phase 3 ESTEEM trials, as well as improving difficult-to-treat nail, scalp and palmoplantar psoriasis. Most patient-reported outcomes, including pruritus and the total Dermatology Life Quality Index, also improved to a significantly greater extent with apremilast than with placebo, with significant improvements in pruritus and skin discomfort/pain visual analogue scale scores seen as early as week 2 with apremilast. Apremilast 30 mg twice daily improved signs and symptoms in both disease-modifying antirheumatic drug (DMARD)-naïve and DMARD-experienced patients with active psoriatic arthritis in the phase 3 PALACE trials. Enthesitis, dactylitis, physical function and fatigue were also improved with apremilast, and its efficacy was sustained for up to 208 weeks. Apremilast had an early onset of efficacy in patients with active psoriatic arthritis, with significantly more apremilast 30 mg twice daily than placebo recipients achieving a ≥20% improvement in modified American College of Rheumatology response criteria at week 2 in the phase 3b ACTIVE trial. Apremilast was generally well tolerated in patients with psoriasis and psoriatic arthritis; no laboratory monitoring is required. In conclusion, orally administered apremilast is an effective, generally well tolerated and convenient option for the treatment of psoriasis and psoriatic arthritis.
阿普司特（Otezla）是一种口服的、小分子磷酸二酯酶 4（PDE4）抑制剂。在 3 期 ESTEEM 试验中，阿普司特 30mg，每日两次，可减轻中重度斑块状银屑病的严重程度，改善治疗困难的指甲、头皮和掌跖部银屑病。大多数患者报告的结局，包括瘙痒和总皮肤病生活质量指数，也得到了显著改善，与安慰剂相比，阿普司特的改善程度更大，瘙痒和皮肤不适/疼痛视觉模拟评分在阿普司特治疗第 2 周就有显著改善。在 3 期 PALACE 试验中，阿普司特 30mg，每日两次，改善了初治和已接受过疾病修饰抗风湿药物（DMARD）治疗的活动性银屑病关节炎患者的体征和症状。附着点炎、指（趾）炎、身体功能和疲劳也得到改善，其疗效可持续长达 208 周。阿普司特在活动性银屑病关节炎患者中具有早期疗效，在 3 期 b ACTIVE 试验中，与安慰剂组相比，更多的阿普司特 30mg，每日两次的患者在第 2 周时达到改良美国风湿病学会反应标准≥20%改善的患者比例显著更高。阿普司特在银屑病和银屑病关节炎患者中通常具有良好的耐受性，无需进行实验室监测。总之，口服阿普司特是治疗银屑病和银屑病关节炎的一种有效、通常具有良好耐受性和方便的选择。
