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Jaktinib - 版本历史
2026-04-18T08:41:41Z
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<strong>[[杰克替尼]]([[Jaktinib]])</strong>，盐酸盐形式为<strong>[[盐酸杰克替尼]]</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年血液肿瘤与自身免疫疾病领域的重磅药物，[[杰克替尼]]能同时抑制<strong>[[JAK1]]</strong>、<strong>[[JAK2]]</strong>、<strong>[[JAK3]]</strong>及<strong>[[TYK2]]</strong>激酶活性，从而阻断<strong>[[JAK-STAT]]</strong>信号通路。临床实践证明，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症状改善，且在<strong>[[重度斑秃]]</strong>、<strong>[[特应性皮炎]]</strong>等自免领域展现出代际级的疗效优势。2026年，[[杰克替尼]]已被正式纳入多项国家级诊疗共识。<br />
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<div style="font-size: 1.2em; font-weight: bold; letter-spacing: 1.2px;">杰克替尼 (Jaktinib)</div><br />
<div style="font-size: 0.7em; opacity: 0.85; margin-top: 4px; white-space: nowrap;">Zelgen Jacktinib·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 Molecular Docking with JAK2 Kinase Domain</div><br />
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<div style="font-size: 0.8em; color: #64748b; margin-top: 12px; font-weight: 600;">靶点涵盖：[[JAK1]]/[[2]]/[[3]]/[[TYK2]]</div><br />
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<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(HCl)</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状态</th><br />
<td style="padding: 12px; color: #1e40af;">MF/斑秃领域国产首创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：多靶点阻断与免疫调节</h2><br />
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[[杰克替尼]]的作用机制在于全方位封锁炎症因子的细胞内信号传导，2026年药理学研究精要如下：<br />
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<li style="margin-bottom: 12px;"><strong>JAK通路全覆盖：</strong> [[杰克替尼]]通过竞争性结合[[JAK]]家族成员激酶区的[[ATP]]结合口袋，阻断[[JAK1/2/3]]及[[TYK2]]的自磷酸化。这使得下游<strong>[[STAT]]</strong>蛋白无法活化并入核，从源头上切断了[[IL-6]]、[[IFN-γ]]等促炎因子的通路。</li><br />
<li style="margin-bottom: 12px;"><strong>抑制骨髓纤维化恶化：</strong> 针对[[MF]]患者中常见的<strong>[[JAK2 V617F]]</strong>突变引起的信号通路过度活跃，[[杰克替尼]]能有效降低骨髓异常增生并减轻脾大。2026年分子生物学证据指出，该药对<strong>[[骨髓微环境]]</strong>的纤维化进程有明显的逆转作用。</li><br />
<li style="margin-bottom: 12px;"><strong>皮肤免疫重塑：</strong> 在<strong>[[斑秃]]</strong>治疗中，[[杰克替尼]]通过阻断[[IFN-γ]]信号，诱导毛囊周围炎症反应消退，使毛囊从退行期重新进入<strong>[[生长期]]</strong>。</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%;">试验名称</th><br />
<th style="padding: 12px; border: 1px solid #cbd5e1; color: #475569;">适应症/干预(2026评价)</th><br />
<th style="padding: 12px; border: 1px solid #cbd5e1; color: #1e40af;">关键生存/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]]；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>。确立为国产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;">重度[[斑秃]]；150mg QD/BID。</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联合试验]]</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48小时。展现出卓越的[[EASI]]改善。</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：精准滴定与安全性平衡</h2><br />
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[[杰克替尼]]在2026年的临床应用路径强调“效能驱动、风险前置”：<br />
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<li style="margin-bottom: 12px;"><strong>剂量优化路径：</strong> 针对[[MF]]推荐剂量为[[100mg BID]]。2026规范建议：对于伴有血小板减少的患者，可采取[[75mg BID]]的个性化起始，待指标稳定后再行滴定。</li><br />
<li style="margin-bottom: 12px;"><strong>血液学毒性管理：</strong> 重点关注<strong>[[贫血]]</strong>与<strong>[[血小板减少]]</strong>。2026版专家共识明确：通过联用促红细胞生成素（[[EPO]]）或调整给药节律，可有效保障长程用药的持续性。</li><br />
<li style="margin-bottom: 12px;"><strong>自免领域的序贯：</strong> 2026年前沿实践提倡在[[斑秃]]治疗中，针对难治人群采用[[杰克替尼]]联合外用制剂或物理疗法，旨在通过协同效应降低系统给药的累积剂量。</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>[[JAK-STAT通路]]：</strong> 2026年最重要的促炎信号传导轴，多系统疾病的共同通路。</li><br />
<li style="margin-bottom: 8px;"><strong>[[骨髓纤维化]]：</strong> 一种罕见的骨髓增殖性肿瘤，杰克替尼的主战场。</li><br />
<li style="margin-bottom: 8px;"><strong>[[芦可替尼]]：</strong> 全球首个JAK抑制剂，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> 杰克替尼的原创孵化实体，中国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 Phase III, Randomized Trial.</em> <strong>[[The Journal of Clinical Oncology]]</strong>.<br><br />
<span style="color: #475569;">[权威点评]：杰克替尼在头对头研究中展示了更稳健的缩脾获益，成为MF精准治疗的新基准。</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.</em> [Academic Review]<br><br />
<span style="color: #475569;">[学术点评]：2026年证据分析确认，国产JAK抑制剂的高选择性为多重耐药或难治性患者提供了极佳的解救方案。</span><br />
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杰克替尼 (Jaktinib) · 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]]•[[STAT3/5]]</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;">治疗药物</td><br />
<td style="padding: 10px 15px; color: #334155;">[[泽悦]]•[[芦可替尼]]•[[巴瑞替尼]]•[[多纳非尼(联合)]]</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]]•[[特应性皮炎]]</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;">专业实体</td><br />
<td style="padding: 10px 15px; color: #334155;">[[泽璟制药]]•[[NMPA]]•[[SinoCellGene协作]]•[[ASCO]]</td><br />
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