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Infigratinib - 版本历史
2026-04-18T13:26:02Z
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<strong>[[英非拉替尼]]([[Infigratinib]])</strong>，商品名为<strong>[[Truseltiq]]</strong>，研发代码为<strong>[[BGJ398]]</strong>，是由[[QED Therapeutics]]（[[BridgeBio]]旗下）研发的一种强效、口服、高选择性的<strong>[[FGFR1-3抑制剂]]</strong>。作为精准肿瘤学中针对成纤维细胞生长因子受体（FGFR）异常的核心药物，[[英非拉替尼]]通过特异性阻断<strong>[[FGFR]]</strong>激酶活性，抑制肿瘤细胞的增殖与存活。临床上，该药主要被批准用于治疗携带<strong>[[FGFR2基因融合]]</strong>或重排的局部晚期或转移性<strong>[[肝内胆管癌]]</strong>（[[iCCA]]），并正在探索其在<strong>[[尿路上皮癌]]</strong>及<strong>[[骨骼发育异常]]</strong>疾病中的应用潜力。<br />
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<div style="font-size: 1.2em; font-weight: bold; letter-spacing: 1.2px;">英非拉替尼 (Infigratinib)</div><br />
<div style="font-size: 0.7em; opacity: 0.85; margin-top: 4px; white-space: nowrap;">Truseltiq·BGJ398·点击展开</div><br />
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<div style="display: inline-block; background: #ffffff; border: 1px solid #e2e8f0; border-radius: 12px; padding: 20px; box-shadow: 0 4px 10px rgba(0,0,0,0.04);"><br />
<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;">Infigratinib: ATP-competitive inhibitor of FGFR1-3 kinases</div><br />
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<div style="font-size: 0.8em; color: #64748b; margin-top: 12px; font-weight: 600;">核心靶标：[[FGFR1]] / [[FGFR2]] / [[FGFR3]]</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;">2263([[FGFR2]])</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;">P21802</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;">560.5 g/mol</td><br />
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<th style="text-align: left; padding: 6px 12px; background-color: #f1f5f9; color: #475569; border-bottom: 1px solid #e2e8f0;">给药途径</th><br />
<td style="padding: 6px 12px; border-bottom: 1px solid #e2e8f0; color: #1e40af;">口服 (125mg QD)</td><br />
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<th style="text-align: left; padding: 6px 12px; background-color: #f1f5f9; color: #475569; border-bottom: 1px solid #e2e8f0;">周期方案</th><br />
<td style="padding: 6px 12px; border-bottom: 1px solid #e2e8f0; color: #0f172a;">服21天/停7天</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]]ID</th><br />
<td style="padding: 6px 12px; border-bottom: 1px solid #e2e8f0; color: #0f172a;">3689</td><br />
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<th style="text-align: left; padding: 6px 12px; background-color: #f1f5f9; color: #475569;">研究热点</th><br />
<td style="padding: 12px; color: #16a34a;">高磷血症管理/耐药克服</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：选择性支路阻断与信号级联关断</h2><br />
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[[英非拉替尼]]的分子药理学核心在于其对 <strong>[[FGFR]]</strong> 激酶域的高度亲和力与特异性：<br />
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<li style="margin-bottom: 12px;"><strong>ATP 竞争性激酶抑制：</strong> 该药物分子精准嵌入 FGFR1-3 的 <strong>[[激酶结构域]]</strong> ATP 结合口袋，通过竞争性抑制受体自磷酸化，阻断促癌信号的起始。</li><br />
<li style="margin-bottom: 12px;"><strong>针对 FGFR2 融合的特异性打击：</strong> 在胆管癌中，由基因易位形成的 <strong>[[FGFR2-BICC1]]</strong> 等融合蛋白会导致受体持续活化。[[英非拉替尼]]能有效纠正此信号异常，抑制下游 <strong>[[MAPK]]</strong>、<strong>[[PI3K/AKT]]</strong> 通路。</li><br />
<li style="margin-bottom: 12px;"><strong>生物标志物相关效应：</strong> 药物导致的 <strong>[[高磷血症]]</strong> 被视为靶向系统受抑的药理学替代指标，反映了其对肾脏磷排泄调节轴（FGF23）的有效干扰。</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;">核心临床研究与应答获益矩阵</h2><br />
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<th style="padding: 12px; border: 1px solid #cbd5e1; color: #0f172a; width: 25%;">试验名称/方案</th><br />
<th style="padding: 12px; border: 1px solid #cbd5e1; color: #475569;">人群背景</th><br />
<th style="padding: 12px; border: 1px solid #cbd5e1; color: #1e40af;">关键指标获益 (ORR/DCR)</th><br />
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<td style="padding: 10px; border: 1px solid #cbd5e1; font-weight: 600;">[[NCT02150967]]</td><br />
<td style="padding: 10px; border: 1px solid #cbd5e1;">含铂化疗进展后的 FGFR2 融合 iCCA。</td><br />
<td style="padding: 10px; border: 1px solid #cbd5e1;"><strong>客观缓解率 (ORR) 23.1%</strong>；疾病控制率 (DCR) 达 84.3%。奠定二线治疗地位。</td><br />
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<td style="padding: 10px; border: 1px solid #cbd5e1; font-weight: 600;">[[PROOF]] 研究</td><br />
<td style="padding: 10px; border: 1px solid #cbd5e1;">对比一线常规化疗。</td><br />
<td style="padding: 10px; border: 1px solid #cbd5e1;">探索 FGFR 抑制剂在 <strong>[[一线治疗]]</strong> 中的获益潜力（虽受商业策略调整影响，但数据具学术参考价值）。</td><br />
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<td style="padding: 10px; border: 1px solid #cbd5e1; font-weight: 600;">安全性评估总结</td><br />
<td style="padding: 10px; border: 1px solid #cbd5e1;">汇总安全性数据。</td><br />
<td style="padding: 10px; border: 1px solid #cbd5e1;"><strong>高磷血症</strong> (77%)、口腔炎及指甲改变。总体毒性谱与同类药一致。</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;">诊疗策略：精准筛选与代谢安全性管理</h2><br />
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[[英非拉替尼]]的临床应用遵循“<strong>[[分子分型引领与特异性 AE 管控]]</strong>”：<br />
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<li style="margin-bottom: 12px;"><strong>分子准入强制要求：</strong> 启动治疗前必须通过 <strong>[[NGS]]</strong> 或 <strong>[[FISH]]</strong> 确认 FGFR2 融合或重排状态。仅有点突变的患者在该药中的获益数据相对受限。</li><br />
<li style="margin-bottom: 12px;"><strong>阶梯式降磷管控：</strong> 治疗期间需严格监测 <strong>[[血清磷]]</strong>。若磷水平超过 7.0 mg/dL，应启动低磷饮食及 <strong>[[磷酸盐结合剂]]</strong> 处理，并视情况进行剂量调整。</li><br />
<li style="margin-bottom: 12px;"><strong>眼科并发症监控：</strong> 针对潜在的 <strong>[[中心性浆液性脉络膜视网膜病变]] (CSR)</strong> 风险，建议在基线及用药期间定期进行眼科 OCT 检查。</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>[[FGFR2基因融合]]：</strong> 肝内胆管癌的关键分子亚型，英非拉替尼的主要靶向群体。</li><br />
<li style="margin-bottom: 8px;"><strong>[[高磷血症]]：</strong> 典型的类效应，反映了 FGFR 信号轴的生物学受抑制强度。</li><br />
<li style="margin-bottom: 8px;"><strong>[[肝内胆管癌]] (iCCA)：</strong> 具有高度纤维间质特征的胆道恶性肿瘤。</li><br />
<li style="margin-bottom: 8px;"><strong>[[BGJ398]]：</strong> 该药在学术界更广为人知的原研实验室代码。</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>Javle M, et al. (2021).</strong> <em>Infigratinib (BGJ398) in previously treated patients with advanced cholangiocarcinoma containing FGFR2 fusions or rearrangements.</em> <strong>[[The Lancet Gastroenterology & Hepatology]]</strong>.<br><br />
<span style="color: #475569;">[权威点评]：该研究确立了英非拉替尼在难治性胆管癌中的显著有效性，推动了其在全球的上市进程。</span><br />
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[2] <strong>Schram AM, et al. (2022).</strong> <em>Targeting FGFR in Cholangiocarcinoma: Clinical Perspectives.</em> <strong>[[Hepatology]]</strong>.[Academic Review]<br><br />
<span style="color: #475569;">[学术点评]：综述详尽阐述了以英非拉替尼为代表的选择性抑制剂在胆管癌精准治疗版图中的价值与挑战。</span><br />
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英非拉替尼 (Truseltiq) 诊疗生态 · 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;">[[FGFR2]]•[[FGFR1]]•[[FGFR3]]•[[BICC1]]•[[RAS/MAPK]]</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;">同类竞品</td><br />
<td style="padding: 10px 15px; color: #334155;">[[Pemigatinib]] (达伯坦)•[[Balversa]] (厄达替尼)•[[Lytgobi]] (福替替尼)</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;">战略实体</td><br />
<td style="padding: 10px 15px; color: #334155;">[[BridgeBio]]•[[LianBio]]•[[SinoCellGene协作]]•[[FDA]]•[[NMPA]]</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;">研究前沿</td><br />
<td style="padding: 10px 15px; color: #334155;">[[辅助治疗探索]]•[[克服耐药突变V564F]]•[[软骨发育不全适应症]]•[[液态活检监测]]</td><br />
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