新型糖皮质激素制剂用于类风湿关节炎:现状与发展
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摘要
类风湿关节炎(rheumatoidarthritis,RA)是以关节滑膜慢性炎症为特征的系统性自身免疫性疾病。糖皮质激素因其强抗炎、起效快、价廉等特点,在RA治疗中发挥重要"桥梁"作用。由于传统糖皮质激素的不良反应相对较多,一定程度上限制了在RA的临床应用。新型糖皮质激素制剂的研究探索旨在保留激素优点的同时,减少其相关的不良反应,具备重要的潜在临床价值。本文综述新型糖皮质激素制剂在RA治疗的研究现状,旨在为国内风湿免疫科医师提供最新研究进展的信息。
Rheumatoid arthritis(RA) is a chronic inflammatory joint disease, which can cause bone damage and disability. Glucocorticoids are highly regarded as "bridge" therapy in the management of RA for long time because of its potent anti-inflammatory effects, low cost, and accessibility. However, a range of adverse reactions induced by glucocorticoids have largely limited its application in daily practice. In recent years, several new preparations and drug delivery systems are being developed in order to improve risk-benefit ratio. In this review, we provide a detailed overview of the progress of these novel glucocorticoids-based therapies in the management of RA.
Rheumatoid arthritis(RA) is a chronic inflammatory joint disease, which can cause bone damage and disability. Glucocorticoids are highly regarded as "bridge" therapy in the management of RA for long time because of its potent anti-inflammatory effects, low cost, and accessibility. However, a range of adverse reactions induced by glucocorticoids have largely limited its application in daily practice. In recent years, several new preparations and drug delivery systems are being developed in order to improve risk-benefit ratio. In this review, we provide a detailed overview of the progress of these novel glucocorticoids-based therapies in the management of RA.
引文
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[24]Schcke H,Zollner TM,D9cke WD,et al.Characterization of ZK 245186,a novel,selective glucocorticoid receptor agonist for the topical treatment of inflammatory skin diseases[J].Br JPharmacol,2009,158:1088-1103.
[25]Baiula M,Spampinato S.Mapracorat,a novel non-steroidal selective glucocorticoid receptor agonist for the treatment of allergic conjunctivitis[J].Inflamm Allergy Drug Targets,2014,13:289-298.
[26]Hu X,Du S,Tunca C,et al.The antagonists but not partial agonists of glucocorticoid receptor ligands show substantial side effect dissociation[J].Endocrinology,2011,152:3123-3134.
[27]Conrado DJ,Krishnaswami S,Shoji S,et al.Predicting the probability of successful efficacy of a dissociated agonist of the glucocorticoid receptor from dose-response analysis[J].J Pharmacokinet Pharmacodyn,2016,43:325-341.
[28]Paul-Clark MJ,Mancini L,Del Soldato P,et al.Potent antiarthritic properties of a glucocorticoid derivative,NCX-1015,in an experimental model of arthritis[J].Proc Natl Acad Sci USA,2002,99:1677-1682.
[29]Paul-Clark MJ,Roviezzo F,Flower RJ,et al.Glucocorticoid receptor nitration leads to enhanced anti-inflammatory effects of novel steroid ligands[J].J Immunol,2003,171:3245-3252.
[30]Oliveira MS,de O Barreto E,Zamuner S,et al.Suppressive effects of nitric oxide-releasing prednisolone NCX-1015 on the allergic pleural eosinophil recruitment in rats[J].Clin Exp Allergy,2008,38:1830-1837.
[31]Lühder F,Reichardt HM.Novel drug delivery systems tailored for improved administration of glucocorticoids[J].Int J Mol Sci,2017,18:pii:E1836.
[32]Quan L,Zhang Y,Crielaard BJ,et al.Nanomedicines for inflammatory arthritis:head-to-head comparison of glucocorticoidcontaining polymers,micelles,and liposomes[J].ACS Nano,2014,8:458-466.
[33]Strehl C,Gaber T,L9wenberg M,et al.Origin and functional activity of the membrane-bound glucocorticoid receptor[J].Arthritis Rheum,2011,63:3779-3788.
[34]Jafari S,Maleki-Dizaji N,Barar J,et al.Methylprednisolone acetate-loaded hydroxyapatite nanoparticles as a potential drug deliverysystem for treatment of rheumatoid arthritis:In vitro and in vivo evaluations[J].Eur J Pharm Sci,2016,91:225-235.
[2]Burmester GR,Pope JE.Novel treatment strategies in rheumatoid arthritis[J].Lancet,2017,10;389:2338-2348.
[3]Smolen JS,LandewéR,Bijlsma J,et al.EULAR recommendations for the management of rheumatoid arthritis with synthetic and biological disease-modifying antirheumatic drugs:2016update[J].Ann Rheum Dis,2017,76:960-977.
[4]Wilson JC,Sarsour K,Gale S,et al.Incidence and risk of glucocorticoid-associated adverse effects in patients with rheumatoid arthritis[J].Arthritis Care Res(Hoboken),2018-06-01.[Epub ahead of print]
[5]Buttgereit F,Doering G,Schaeffler A,et al.Efficacy of modified-release versus standard prednisone to reduce duration of morning stiffness of the joints in rheumatoid arthritis(CAPRA-1):a double-blind,randomised controlled trial[J].Lancet,2008,371:205-214.
[6]Buttgereit F,Doering G,Schaeffler A,et al.Targeting pathophysiological rhythms:prednisone chronotherapy shows sustained efficacy in rheumatoid arthritis[J].Ann Rheum Dis,2010,69:1275-1280.
[7]Buttgereit F,Mehta D,Kirwan J,et al.Low-dose prednisone chronotherapy for rheumatoid arthritis:a randomised clinical trial(CAPRA-2)[J].Ann Rheum Dis,2013,72:204-210.
[8]Cutolo M,Iaccarino L,Doria A,et al.Efficacy of the switch to modified-release prednisone in rheumatoid arthritis patients treated with standard glucocorticoids[J].Clin Exp Rheumatol,2013,31:498-505.
[9]Alten R,Grahn A,Holt RJ,et al.Delayed-release prednisone improves fatigue and health-related quality of life:findings from the CAPRA-2 double-blind randomised study in rheumatoid arthritis[J].RMD Open,2015,1:e000134.
[10]Krasselt M,Baerwald C.Efficacy and safety of modified-release prednisone in patients with rheumatoid arthritis[J].Drug Des Devel Ther,2016,10:1047-1058.
[11]Alten R,Holt R,Grahn A,et al.Morning stiffness response with delayed-release prednisone after ineffective course of immediaterelease prednisone[J].Scand J Rheumatol,2015,44:354-358.
[12]Ursini F,Naty S,Bruno C,et al.Old But Good:Modified-release prednisone in rheumatoid arthritis[J].Rev Recent Clin Trials,2017,12:124-128.
[13]Alten R,D9ring G,Cutolo M,et al.Hypothalamus-pituitary-adrenal axis function in patients with rheumatoid arthritis treated with nighttime-release prednisone[J].J Rheumatol.2010;37:2025-2031.
[14]Madni A,Sarfraz M,Rehman M,et al.Liposomal drug delivery:a versatile platform for challenging clinical applications[J].JPharm Pharm Sci,2014,17:401-426.
[15]van der Goes MC,Jacobs JW,Bijlsma JW.Rediscovering the therapeutic use of glucocorticoids in rheumatoid arthritis[J].Curr Opin Rheumatol,2016,28:289-296.
[16]Metselaar JM,Wauben MH,Wagenaar-Hilbers JP,et al.Complete remission of experimental arthritis by joint targeting of glucocorticoids with long-circulating liposomes[J].Arthritis Rheum,2003,48:2059-2066.
[17]Metselaar JM,van den Berg WB,Holthuysen AE,et al.Liposomal targeting of glucocorticoids to synovial lining cells strongly increases therapeutic benefit in collagen type II arthritis[J].Ann Rheum Dis,2004,63:348-353.
[18]余静.地塞米松棕榈酸酯脂肪乳注射液的制备[J].中国药师,2016,12:2262-2266.
[19]黄建林,徐莉,罗敏琪,等.地塞米松棕榈酸酯注射液膝关节腔注射治疗类风湿关节炎疗效和安全性观察[J].广东医学,2010,11:1474-1475.
[20]梁雁,许俊羽,赵侠,等.地塞米松棕榈酸酯注射液在中国健康受试者的药代动力学研究[J].中国临床药理学杂志,2015,16:1613-1617.
[21]郭军华,黄烽,张江林,等.两种地塞米松棕榈酸酯注射液治疗类风湿关节炎的多中心随机双盲对照观察[J].中华风湿病学杂志,2012,6:393-397.
[22]Berger M,Rehwinkel H,Schmees N,et al.Discovery of new selective glucocorticoid receptor agonist leads[J].Bioorg Med Chem Lett,2017,27:437-442.
[23]Reichardt HM,Kaestner KH,Tuckermann J,et al.DNAbinding of the glucocorticoid receptor is not essential for survival[J].Cell,1998,93:531-541.
[24]Schcke H,Zollner TM,D9cke WD,et al.Characterization of ZK 245186,a novel,selective glucocorticoid receptor agonist for the topical treatment of inflammatory skin diseases[J].Br JPharmacol,2009,158:1088-1103.
[25]Baiula M,Spampinato S.Mapracorat,a novel non-steroidal selective glucocorticoid receptor agonist for the treatment of allergic conjunctivitis[J].Inflamm Allergy Drug Targets,2014,13:289-298.
[26]Hu X,Du S,Tunca C,et al.The antagonists but not partial agonists of glucocorticoid receptor ligands show substantial side effect dissociation[J].Endocrinology,2011,152:3123-3134.
[27]Conrado DJ,Krishnaswami S,Shoji S,et al.Predicting the probability of successful efficacy of a dissociated agonist of the glucocorticoid receptor from dose-response analysis[J].J Pharmacokinet Pharmacodyn,2016,43:325-341.
[28]Paul-Clark MJ,Mancini L,Del Soldato P,et al.Potent antiarthritic properties of a glucocorticoid derivative,NCX-1015,in an experimental model of arthritis[J].Proc Natl Acad Sci USA,2002,99:1677-1682.
[29]Paul-Clark MJ,Roviezzo F,Flower RJ,et al.Glucocorticoid receptor nitration leads to enhanced anti-inflammatory effects of novel steroid ligands[J].J Immunol,2003,171:3245-3252.
[30]Oliveira MS,de O Barreto E,Zamuner S,et al.Suppressive effects of nitric oxide-releasing prednisolone NCX-1015 on the allergic pleural eosinophil recruitment in rats[J].Clin Exp Allergy,2008,38:1830-1837.
[31]Lühder F,Reichardt HM.Novel drug delivery systems tailored for improved administration of glucocorticoids[J].Int J Mol Sci,2017,18:pii:E1836.
[32]Quan L,Zhang Y,Crielaard BJ,et al.Nanomedicines for inflammatory arthritis:head-to-head comparison of glucocorticoidcontaining polymers,micelles,and liposomes[J].ACS Nano,2014,8:458-466.
[33]Strehl C,Gaber T,L9wenberg M,et al.Origin and functional activity of the membrane-bound glucocorticoid receptor[J].Arthritis Rheum,2011,63:3779-3788.
[34]Jafari S,Maleki-Dizaji N,Barar J,et al.Methylprednisolone acetate-loaded hydroxyapatite nanoparticles as a potential drug deliverysystem for treatment of rheumatoid arthritis:In vitro and in vivo evaluations[J].Eur J Pharm Sci,2016,91:225-235.
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