盐酸吉卡昔替尼片在骨髓纤维化治疗中的应用

Application of gecacitinib hydrochloride tablets in treatment of myelofibrosis

盐酸吉卡昔替尼片(简称吉卡昔替尼,曾用名"盐酸杰克替尼片")是一种新型的JAK和ACVR1抑制剂,其不仅能通过抑制JAK1、JAK2、JAK3和TYK2活性阻断JAK-STAT信号转导通路,从而缓解炎症和脾大症状,还能通过抑制ACVR1活性降低铁调素转录,从而改善铁代谢失衡和贫血。Ⅱ、Ⅲ期临床试验数据提示,吉卡昔替尼既能改善JAK抑制剂初治或芦可替尼经治的骨髓纤维化(MF)患者脾大、体质性症状,也能改善MF患者的贫血。文章就吉卡昔替尼治疗MF的作用机制、药代动力学特点、临床疗效及治疗相关不良反应等方面进行阐述,为该药在MF中的合理应用提供参考。

Gecacitinib hydrochloride tablets(gecacitinib for short,and formerly known as"jaktinib hydrochloride tablets")is a novel JAK and ACVR1 inhibitor,which not only blocks the JAK-STAT signaling pathway by inhibiting the activities of JAK1,JAK2,JAK3,and TYK2,thereby alleviating inflammation and splenomegaly symptoms,but also reduces hepcidin transcription by inhibiting ACVR1 activity,thereby improving iron metabolism imbalance and anemia.Data from phasesⅡandⅢclinical trials suggest that gecacitinib can both alleviate splenomegaly and reduce constitutional symptoms in patients with myelofibrosis(MF)who are na?ve to JAK inhibitors or have been exposed to ruxolitinib,as well as improve anemia in patients with MF.This article describes the mechanisms of action,pharmacokinetic characteristics,clinical efficacy,and treatment-related adverse effects of gecacitinib in the treatment of MF,providing references for the rational application of this drug in MF.