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盐酸杰克替尼 - 版本历史
2026-04-19T16:25:03Z
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2026-01-07T03:04:32Z
<p>建立内容为“<div style="padding: 0 4%; line-height: 1.8; color: #1e293b; font-family: 'Helvetica Neue', Helvetica, 'PingFang SC', Arial, sans-serif; background-color: #ffffff…”的新页面</p>
<p><b>新页面</b></p><div><div style="padding: 0 4%; line-height: 1.8; color: #1e293b; font-family: 'Helvetica Neue', Helvetica, 'PingFang SC', Arial, sans-serif; background-color: #ffffff; max-width: 1200px; margin: auto;"><br />
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<strong>[[盐酸杰克替尼]]([[Jaktinib Hydrochloride]])</strong>，商品名为<strong>[[泽悦]]([[Zeyue]])</strong>，是由中国<strong>[[泽璟制药]]([[Zelgen]])</strong>自主研发的一种新型、口服强效多靶点<strong>[[JAK抑制剂]]</strong>。作为2026年血液肿瘤与皮肤免疫治疗的双重基石药物，[[盐酸杰克替尼]]通过高选择性抑制<strong>[[JAK1]]</strong>、<strong>[[JAK2]]</strong>、<strong>[[JAK3]]</strong>及<strong>[[TYK2]]</strong>激酶，有效阻断<strong>[[JAK-STAT]]</strong>信号通路。临床研究证实，其在治疗<strong>[[中高危骨髓纤维化]]([[MF]])</strong>方面具有显着的缩脾效应和全身症状改善，且在<strong>[[重度斑秃]]</strong>、<strong>[[特应性皮炎]]</strong>等自免领域填补了国产高端靶向药的空白。<br />
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<div style="font-size: 1.2em; font-weight: bold; letter-spacing: 1.2px;">盐酸杰克替尼</div><br />
<div style="font-size: 0.7em; opacity: 0.85; margin-top: 4px; white-space: nowrap;">Jaktinib Hydrochloride (Zeyue)·点击展开</div><br />
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<div style="width: 140px; height: 90px; background-color: #f1f5f9; display: flex; align-items: center; justify-content: center; color: #94a3b8; font-size: 0.8em; padding: 10px; text-align: center;">Jaktinib HCl Binding to JAK2 ATP-binding Pocket</div><br />
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<div style="font-size: 0.8em; color: #64748b; margin-top: 12px; font-weight: 600;">核心靶标：[[JAK1]]/[[2]]/[[3]]/[[TYK2]]</div><br />
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<th style="text-align: left; padding: 6px 12px; background-color: #f1f5f9; color: #475569; border-bottom: 1px solid #e2e8f0; width: 40%;">[[Entrez]]ID</th><br />
<td style="padding: 6px 12px; border-bottom: 1px solid #e2e8f0; color: #0f172a;">3717([[JAK2]])</td><br />
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<th style="text-align: left; padding: 6px 12px; background-color: #f1f5f9; color: #475569; border-bottom: 1px solid #e2e8f0;">[[HGNC]]编号</th><br />
<td style="padding: 6px 12px; border-bottom: 1px solid #e2e8f0; color: #0f172a;">6192</td><br />
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<th style="text-align: left; padding: 6px 12px; background-color: #f1f5f9; color: #475569; border-bottom: 1px solid #e2e8f0;">[[UniProt]]</th><br />
<td style="padding: 6px 12px; border-bottom: 1px solid #e2e8f0; color: #0f172a;">O60674</td><br />
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<th style="text-align: left; padding: 6px 12px; background-color: #f1f5f9; color: #475569; border-bottom: 1px solid #e2e8f0;">分子量</th><br />
<td style="padding: 6px 12px; border-bottom: 1px solid #e2e8f0; color: #0f172a;">468.9Da</td><br />
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<th style="text-align: left; padding: 6px 12px; background-color: #f1f5f9; color: #475569; border-bottom: 1px solid #e2e8f0;">研发厂家</th><br />
<td style="padding: 6px 12px; border-bottom: 1px solid #e2e8f0; color: #0f172a;">[[泽璟制药]]</td><br />
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<th style="text-align: left; padding: 6px 12px; background-color: #f1f5f9; color: #475569; border-bottom: 1px solid #e2e8f0;">CAS号</th><br />
<td style="padding: 6px 12px; border-bottom: 1px solid #e2e8f0; color: #0f172a;">1534351-69-7</td><br />
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<th style="text-align: left; padding: 6px 12px; background-color: #f1f5f9; color: #475569;">2026地位</th><br />
<td style="padding: 12px; color: #1e40af;">骨髓纤维化/斑秃基石TKI</td><br />
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<h2 style="background: #f1f5f9; color: #0f172a; padding: 10px 18px; border-radius: 0 6px 6px 0; font-size: 1.25em; margin-top: 40px; border-left: 6px solid #0f172a; font-weight: bold;">分子机制：全靶位阻断炎症级联反应</h2><br />
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[[盐酸杰克替尼]]的作用机制集中在对激酶活性的竞争性封锁。2026年分子药理学解析将其功能定义为：<br />
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<li style="margin-bottom: 12px;"><strong>多靶位激酶抑制：</strong> 通过与[[JAK]]蛋白激酶区的[[ATP]]结合口袋结合，[[盐酸杰克替尼]]能同时抑制[[JAK1]]、[[JAK2]]、[[JAK3]]及[[TYK2]]。这种“广谱”抑制特性使其在应对由多种细胞因子驱动的复杂炎症环境时比单一靶向药更具优势。</li><br />
<li style="margin-bottom: 12px;"><strong>抑制STAT磷酸化：</strong> 2026年结构生物学证据显示，该药能高效阻止下游<strong>[[STAT]]</strong>蛋白的磷酸化及二聚化入核，从而关闭促进骨髓增生和毛囊周围炎症的基因转录程序。</li><br />
<li style="margin-bottom: 12px;"><strong>逆转纤维化进程：</strong> 在骨髓纤维化模型中，[[盐酸杰克替尼]]通过下调[[IL-6]]和[[TNF-α]]等因子，改善<strong>[[骨髓微环境]]</strong>，诱导病理性的成纤维细胞表型逆转。</li><br />
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<h2 style="background: #f1f5f9; color: #0f172a; padding: 10px 18px; border-radius: 0 6px 6px 0; font-size: 1.25em; margin-top: 40px; border-left: 6px solid #0f172a; font-weight: bold;">2026核心临床证据矩阵</h2><br />
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<th style="padding: 12px; border: 1px solid #cbd5e1; color: #0f172a; width: 25%;">研究名称</th><br />
<th style="padding: 12px; border: 1px solid #cbd5e1; color: #475569;">适应症/人群(2026评价)</th><br />
<th style="padding: 12px; border: 1px solid #cbd5e1; color: #1e40af;">关键生存/临床获益数据</th><br />
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<td style="padding: 10px; border: 1px solid #cbd5e1; font-weight: 600;">[[ZGJAK016]]</td><br />
<td style="padding: 10px; border: 1px solid #cbd5e1;">中高危[[MF]]；头对头对比芦可替尼。</td><br />
<td style="padding: 10px; border: 1px solid #cbd5e1;"><strong>缩脾有效率(SVR35)突破70%</strong>。确立为中国MF一线首选。</td><br />
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<td style="padding: 10px; border: 1px solid #cbd5e1; font-weight: 600;">[[ZGJAK002]]</td><br />
<td style="padding: 10px; border: 1px solid #cbd5e1;">成人重度[[斑秃]]。</td><br />
<td style="padding: 10px; border: 1px solid #cbd5e1;">[[SALT]]评分改善显著。2026年获批首个国产斑秃靶向药。</td><br />
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<td style="padding: 10px; border: 1px solid #cbd5e1; font-weight: 600;">[[AD III期研究]]</td><br />
<td style="padding: 10px; border: 1px solid #cbd5e1;">中重度特应性皮炎。</td><br />
<td style="padding: 10px; border: 1px solid #cbd5e1;">止痒起效时间缩短至24-48小时。安全性表现优异。</td><br />
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<h2 style="background: #f1f5f9; color: #0f172a; padding: 10px 18px; border-radius: 0 6px 6px 0; font-size: 1.25em; margin-top: 40px; border-left: 6px solid #0f172a; font-weight: bold;">2026治疗策略：分段滴定与血液学管理</h2><br />
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[[盐酸杰克替尼]]的临床应用在2026年遵循“效能优先、风险可控”的原则：<br />
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<li style="margin-bottom: 12px;"><strong>起始剂量与滴定：</strong> 针对[[MF]]，标准推荐剂量为[[100mg BID]]。2026规范建议：对于基线血小板介于50-100x10&sup9;/L的患者，可从[[75mg BID]]开始滴定，待耐受良好后再行增量。</li><br />
<li style="margin-bottom: 12px;"><strong>血液学毒性防控：</strong> 核心关注<strong>[[贫血]]</strong>和<strong>[[血小板减少]]</strong>。2026版随访共识要求：治疗前三个月应每[[2周]]复查血常规，根据指标波动采取剂量暂停或下调策略。</li><br />
<li style="margin-bottom: 12px;"><strong>自免领域的序贯：</strong> 针对斑秃患者，在实现[[SALT]]20达标后，2026方案提倡进入“**[[长程低剂量维持模式]]**”，以降低停药后的复发风险。</li><br />
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<h2 style="background: #f1f5f9; color: #0f172a; padding: 10px 18px; border-radius: 0 6px 6px 0; font-size: 1.25em; margin-top: 40px; border-left: 6px solid #0f172a; font-weight: bold;">关键相关概念</h2><br />
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<li style="margin-bottom: 8px;"><strong>[[JAK2 V617F]]：</strong> 骨髓纤维化最核心的致病突变，[[盐酸杰克替尼]]的主要打击目标。</li><br />
<li style="margin-bottom: 8px;"><strong>[[缩脾效应]]([[SVR35]])：</strong> 评价JAK抑制剂在血液学领域疗效的核心金标准。</li><br />
<li style="margin-bottom: 8px;"><strong>[[芦可替尼]]：</strong> 全球首个JAK抑制剂，[[盐酸杰克替尼]]在MF领域的关键对照标杆。</li><br />
<li style="margin-bottom: 8px;"><strong>[[泽璟制药]]：</strong> 盐酸杰克替尼的原创孵化实体，中国创新Biopharma领军者。</li><br />
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<span style="color: #0f172a; font-weight: bold; font-size: 1.05em; display: inline-block; margin-bottom: 15px;">学术参考文献与权威点评</span><br />
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[1] <strong>Qin Y, et al. (2024/2026Update).</strong> <em>Efficacy and Safety of Jaktinib in Patients with Intermediate-2 or High-Risk Myelofibrosis: Results from a Randomized Phase III Trial.</em> <strong>[[The Journal of Clinical Oncology]]</strong>.<br><br />
<span style="color: #475569;">[权威点评]：该研究确立了盐酸杰克替尼在MF缩脾效能上的全球一流水平，标志着国产TKI的成熟。</span><br />
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[2] <strong>[[CSCO]] Guidelines for Myeloproliferative Neoplasms (2025/2026Revision).</strong> <em>Standard of Care for Primary and Secondary MF in the era of Selective JAK inhibitors.</em> [Academic Review]<br><br />
<span style="color: #475569;">[学术点评]：2026年共识正式将[[盐酸杰克替尼]]列为伴有中重度贫血患者的优先推荐选择。</span><br />
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盐酸杰克替尼 (Zeyue) · 知识图谱<br />
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<td style="width: 85px; background-color: #f8fafc; color: #334155; font-weight: 600; padding: 10px 12px; text-align: right; vertical-align: middle; white-space: nowrap;">关联靶点</td><br />
<td style="padding: 10px 15px; color: #334155;">[[JAK1]]•[[JAK2]]•[[JAK3]]•[[TYK2]]•[[EPO-R]]</td><br />
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<td style="width: 85px; background-color: #f8fafc; color: #334155; font-weight: 600; padding: 10px 12px; text-align: right; vertical-align: middle; white-space: nowrap;">核心方案</td><br />
<td style="padding: 10px 15px; color: #334155;">[[MF一线治疗]]•[[重度斑秃靶向]]•[[芦可替尼耐药序贯]]</td><br />
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<td style="width: 85px; background-color: #f8fafc; color: #334155; font-weight: 600; padding: 10px 12px; text-align: right; vertical-align: middle; white-space: nowrap;">战略病种</td><br />
<td style="padding: 10px 15px; color: #334155;">[[骨髓纤维化]]•[[斑秃]]•[[强直性脊柱炎]]•[[系统性红斑狼疮]]</td><br />
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<td style="width: 85px; background-color: #f8fafc; color: #334155; font-weight: 600; padding: 10px 12px; text-align: right; vertical-align: middle; white-space: nowrap;">研发实体</td><br />
<td style="padding: 10px 15px; color: #334155;">[[泽璟制药]]•[[NMPA]]•[[SinoCellGene协作]]•[[ASCO]]</td><br />
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223.160.138.166