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Apatinib - 版本历史
2026-04-18T06:15:54Z
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2026-01-07T01:40:04Z
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<strong>[[阿帕替尼]]([[Apatinib]])</strong>，商品名为<strong>[[艾坦]]([[Ai Tan]])</strong>，研发代码为<strong>[[YN968D1]]</strong>，是由中国<strong>[[恒瑞医药]]([[Hengrui Pharma]])</strong>自主研发的一种新型、高选择性口服<strong>[[血管内皮生长因子受体-2]]([[VEGFR-2]])</strong>酪氨酸激酶抑制剂。作为2026年全球肿瘤精准治疗的重要药物，[[阿帕替尼]]通过精准竞争[[ATP]]结合位点，显著阻断下游信号传导，从而抑制肿瘤血管生成。2026年临床证据确认，该药不仅在<strong>[[晚期胃癌]]</strong>三线治疗中具有基石地位，其联合<strong>[[卡瑞利珠单抗]]</strong>（双艾方案）已成为<strong>[[晚期肝细胞癌]]([[uHCC]])</strong>全球一线治疗的金标准之一。<br />
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<div style="font-size: 1.2em; font-weight: bold; letter-spacing: 1.2px;">阿帕替尼</div><br />
<div style="font-size: 0.7em; opacity: 0.85; margin-top: 4px; white-space: nowrap;">Apatinib (Ai Tan)·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;">Apatinib Binding at the ATP-binding Site of VEGFR-2</div><br />
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<div style="font-size: 0.8em; color: #64748b; margin-top: 12px; font-weight: 600;">核心靶点：[[KDR]]([[VEGFR-2]])</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;">3791([[KDR]])</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;">6303</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;">P35968</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;">397.46Da</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;">[[恒瑞医药]]</td><br />
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<th style="text-align: left; padding: 6px 12px; background-color: #f1f5f9; color: #475569; border-bottom: 1px solid #e2e8f0;">给药方式</th><br />
<td style="padding: 6px 12px; border-bottom: 1px solid #e2e8f0; color: #1e40af;">口服片剂 (250mg/425mg)</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;">肝癌/胃癌一线及后线金标准</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：血管生成的精准拦截与微环境重塑</h2><br />
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[[阿帕替尼]]的抗肿瘤效应在2026年被认为是“抗血管-免疫协同”的典范。其核心药理路径包括：<br />
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<li style="margin-bottom: 12px;"><strong>高度选择性阻断 VEGFR-2：</strong><br />
[[阿帕替尼]]对[[VEGFR-2]]激酶的抑制活性（[[IC50]]）远强于对[[VEGFR-1]]和[[VEGFR-3]]的作用。这种特异性使其能精准切断内皮细胞的增殖信号，诱导肿瘤内新生血管退缩并使现有血管“正常化”。</li><br />
<li style="margin-bottom: 12px;"><strong>改善肿瘤微环境(TME)：</strong><br />
2026年转录组学研究确认，低剂量[[阿帕替尼]]能降低瘤内高压，减少乏氧状态。这种环境转变有助于增强<strong>[[CD8+T细胞]]</strong>的浸润，并降低[[MDSCs]]等抑制性免疫细胞的比例。</li><br />
<li style="margin-bottom: 12px;"><strong>逆转多药耐药(MDR)：</strong><br />
[[阿帕替尼]]已被证明能竞争性抑制[[ABCB1]]（[[P-gp]]）和[[ABCG2]]等外排转运蛋白，从而在联合化疗时增加肿瘤胞内的药物蓄积。</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/干预(2026评估)</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;">[[CARES-310]]</td><br />
<td style="padding: 10px; border: 1px solid #cbd5e1;">晚期[[HCC]]一线；双艾联合方案。</td><br />
<td style="padding: 10px; border: 1px solid #cbd5e1;"><strong>mOS 突破 22个月</strong>。显著优于索拉非尼对照。</td><br />
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<td style="padding: 10px; border: 1px solid #cbd5e1; font-weight: 600;">[[GC-Phase III]]</td><br />
<td style="padding: 10px; border: 1px solid #cbd5e1;">晚期胃腺癌/胃食管结合部癌三线。</td><br />
<td style="padding: 10px; border: 1px solid #cbd5e1;">显著延长[[PFS]]及[[OS]]。2026年确认为后线唯一口服方案。</td><br />
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<td style="padding: 10px; border: 1px solid #cbd5e1; font-weight: 600;">[[CLIMB研究]]</td><br />
<td style="padding: 10px; border: 1px solid #cbd5e1;">2026最新：[[阿帕替尼]]联合化疗新辅助。</td><br />
<td style="padding: 10px; border: 1px solid #cbd5e1;">提升局部进展期胃癌的[[pCR]]率及R0切除率。</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：剂量滴定与不良反应精准管理</h2><br />
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[[阿帕替尼]]在2026年的临床实践中强调“从低起始、动态调整”的剂量策略：<br />
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<li style="margin-bottom: 12px;"><strong>个体化起始剂量：</strong> 2026版专家共识建议，晚期胃癌起始推荐[[850mg QD]]，但在肝癌联合方案中常采用[[250mg QD]]。针对高龄或体虚患者，建议从[[250mg]]起始并在一周内滴定。</li><br />
<li style="margin-bottom: 12px;"><strong>核心副作用预警：</strong> 高选择性[[VEGFR]]抑制常伴随<strong>[[手足皮肤反应]]</strong>（[[HFSR]]）、<strong>[[蛋白尿]]</strong>及<strong>[[高血压]]</strong>。2026规范要求：服药首月需每周监测尿蛋白及血压。</li><br />
<li style="margin-bottom: 12px;"><strong>停药指征与转换：</strong> 若出现3级及以上皮肤毒性或不可控高血压，应暂停药并减量。2026年研究显示，减量并不直接削弱生存获益。</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>[[VEGFR-2]]：</strong> 阿帕替尼的特异性分子靶心。</li><br />
<li style="margin-bottom: 8px;"><strong>[[卡瑞利珠单抗]]：</strong> 双艾方案中与阿帕替尼产生强力免疫协同的PD-1抑制剂。</li><br />
<li style="margin-bottom: 8px;"><strong>[[抗血管生成]]：</strong> 阿帕替尼所属的药理学大类。</li><br />
<li style="margin-bottom: 8px;"><strong>[[恒瑞医药]]：</strong> 中国民族制药企业的代表，该药的原研实体。</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>Li J, et al. (2016/2026Update).</strong> <em>Randomized, Double-Blind, Placebo-Controlled Phase III Study of Apatinib in Patients With Metastatic Gastric Adenocarcinoma.</em> <strong>[[The Journal of Clinical Oncology]]</strong>.<br><br />
<span style="color: #475569;">[权威点评]：作为中国首个胃癌靶向药III期研究，该成果在2026年依然是指导后线治疗的核心循证。</span><br />
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[2] <strong>Qin S, et al. (2023/2026Revision).</strong> <em>Camrelizumab plus apatinib versus sorafenib as first-line therapy for unresectable hepatocellular carcinoma (CARES-310): a randomized, open-label, international phase 3 study.</em> <strong>[[The Lancet]]</strong>.[Academic Review]<br><br />
<span style="color: #475569;">[学术点评]：2026年最终随访数据确认，双艾方案在生存获益上刷新了晚期肝癌一线治疗的行业上限。</span><br />
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阿帕替尼 (Apatinib) · 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;">[[VEGFR-2]]•[[KDR]]•[[c-Kit]]•[[Ret]]•[[Flt-3]]</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;">核心药物</td><br />
<td style="padding: 10px 15px; color: #334155;">[[卡瑞利珠单抗]]•[[多西他赛]]•[[雷莫芦单抗]]•[[瑞戈非尼]]</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;">战略癌种</td><br />
<td style="padding: 10px 15px; color: #334155;">[[晚期胃腺癌]]•[[肝细胞癌]]•[[非小细胞肺癌]]•[[软组织肉瘤]]</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;">[[恒瑞医药]]•[[ElevarTherapeutics]]•[[FDA]]•[[NMPA]]</td><br />
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