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海南医学院药学院,海口 571199
Published:15 July 2024,
Received:02 November 2023,
Revised:20 June 2024,
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冯世权,秦贞苗,胡雪等.鲁索替尼的临床应用研究进展 Δ[J].中国药房,2024,35(13):1668-1672.
FENG Shiquan,QIN Zhenmiao,HU Xue,et al.Research progress on clinical application of ruxolitinib[J].ZHONGGUO YAOFANG,2024,35(13):1668-1672.
冯世权,秦贞苗,胡雪等.鲁索替尼的临床应用研究进展 Δ[J].中国药房,2024,35(13):1668-1672. DOI: 10.6039/j.issn.1001-0408.2024.13.21.
FENG Shiquan,QIN Zhenmiao,HU Xue,et al.Research progress on clinical application of ruxolitinib[J].ZHONGGUO YAOFANG,2024,35(13):1668-1672. DOI: 10.6039/j.issn.1001-0408.2024.13.21.
鲁索替尼是一种选择性靶向Janus激酶(JAK)的小分子抑制剂,可在JAK1、JAK2结构域与催化位点上的三磷酸腺苷竞争性结合,从而抑制JAK活化和信号转导及转录激活蛋白(STAT)磷酸化,阻止JAK-STAT信号通路的表达。口服鲁索替尼对骨髓纤维化和真性红细胞增多症展现出良好的疗效。外用的鲁索替尼乳膏是美国FDA批准的首个非节段型白癜风家庭治疗药物,目前虽尚未在我国上市,但已于2023年8月落地国内医疗先行区,有望成为白癜风治疗的新突破。鲁索替尼乳膏还被多项临床案例证明对特应性皮炎、斑秃等具有显著疗效,具有较大的应用前景。
Ruxolitinib, a small molecule inhibitor, selectively targets Janus kinase (JAK) by competitively binding to adenosine triphosphate on the catalytic site of the JAK1 and JAK2 domain, thereby inhibiting JAK activation and signal transducer and activator of transcription (STAT) phosphorylation and prevents the expressions of the JAK-STAT signaling pathway. Oral ruxolitinib has demonstrated promising efficacy for myelofibrosis and polycythemia vera. The topical Ruxolitinib cream, approved by the US FDA as the first non-segmental vitiligo home treatment drug, is set to be launched in domestic medical pioneer areas in August 2023 and is expected to bring about a breakthrough in the treatment of vitiligo. Clinical cases have also shown that Ruxolitinib cream has significant curative effects on atopic dermatitis, alopecia areata, and other conditions, indicating great application prospects.
鲁索替尼JAK-STAT信号通路JAK抑制剂骨髓纤维化真性红细胞增多症白癜风皮肤病
JAK-STAT signaling pathwayJAK inhibitorsmyelofibrosispolycythemia veravitiligoskin diseases
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