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新型磷酸二酯酶4抑制剂——阿瑞斯特

Novel phosphodiesterase-4 inhibitor——apremilast
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摘要 阿瑞斯特为一种新型口服小分子磷酸二酯酶4抑制剂,用于银屑病关节炎的治疗。本文在药效学、药动学和临床试验等方面对该药进行了介绍。 Apremilast is an oral small molecule inhibitor of phosphodiesterase-4, and it is developed for the treatment of psoriatic arthritis. This paper summarized the pharmacodynamics, pharmacokinetics, and therapeutic trials of this drug.
作者 杨君义
机构地区 临沂市沂水中心医院药学部
出处 《中国新药与临床杂志》 CAS CSCD 北大核心 2015年第5期343-345,共3页 Chinese Journal of New Drugs and Clinical Remedies
关键词 阿瑞斯特 磷酸二酯酶抑制剂 关节炎 牛皮癣 apremilast phosphodiesterase inhibitors arthritis,psoriatic
分类号 R976 [医药卫生—药品]
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参考文献12

  • 1GOTI'LIEB A, KORMAN NJ, GORDON KB, et al. Guidelinesof care for the management of psoriasis and psoriatic arthritis: Section 2. Psoriatic arthritis: overview and guidelines of care for treatment with an emphasis on the biologies [J]. J Am Acad Dermatol, 2008, 58(5): 851-864.
  • 2GAN EY, CHONG WS, TEY HL. Therapeutic strategies in psoriasis patients with psoriatic arthritis: focus on new agents[J]. Bio Drugs, 2013, 27(4): 359-373.
  • 3SCHAFER P. Apremilast mechanism of action and application to psoriasis and psoriatic arthritis[J]. Biochem Pharmacol, 2012, 83 (12) : 1583-1590.
  • 4SCHAFER PH, PARTON A, GANDHI AK, et al. Apremilast, a cAMP phosphodiesterase- 4 inhibitor, demonstrates anti- inflammatory activity in vitro and in a model of psoriasis[J]. Br J Pharmacol, 2010, 159(4): 842-855.
  • 5GOTTLIEB AB, MATHESON RT, MENTER A, et al. Efficacy, tolerability, and pharmacodynamics of apremilast in recalcitrant plaque psoriasis: a phase ]I open- label study [J]. J Drugs Dermato], 2013, 12(8): 888-897.
  • 6GOTFLIEB AB, STROBER B, KRUEGER JG, et ol. An open- label, singlearm pilot study in patients with severe plaque-type psoriasis treated with an oral anti- inflammatory agent, apremilast[J]. Curr Med Res Opin, 2008, 24(5): 1529-1538.
  • 7VARADA S, TINTLE S.I, GOITLIEB AB. Apremilast for the treatment of psoriatic arthritis [J]. Expert Rev Clin Pharmacol, 2014, 7(3): 239-250.
  • 8REYES J, BAI H, KONG L, et ol. Relative bioavailability of oral apremilast administered as a 40 mg tablet versus two 20 mg capsules with or without food in healthy males[J]. J Clin Pharmacol, 2011, 51(9): 1343-1344.
  • 9KAVANAUGH A, MEASE PJ, GOMEZ- REINO 3.1, et al. Treatment of psoriatic arthritis in a phase 3 randomised, placebo-controlled trial with apremilast, an oral phosphodiesterase 4 inhibitor[J]. Ann Rheum Dis, 2014, 73(6): 1020-1026.
  • 10CUTOLO M, MYERSON GE, FLEISCHMANN RM, et al. Long- term (52-week) results of a phase 3, randomized, controlled trial of apremilast, an oral phosphodiesterase 4 inhibitor, in patients with psoriatic arthritis (PALACE 2)[J]. Arthritis Rheum, 2013, 65(Suppl 10): $346-$347.
中国新药与临床杂志
2015年 第5期

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