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Xtandi - 版本历史
2026-04-18T07:47:09Z
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2026-01-07T07:55:23Z
<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>[[Xtandi]]([[安列特]])</strong>，通用名为<strong>[[恩扎卢胺]]([[Enzalutamide]])**，研发代码为**[[MDV3100]]**，是由[[安斯泰来]]([[Astellas]])与[[辉瑞]]([[Pfizer]])联合开发的一种强效口服非甾体<strong>[[雄激素受体抑制剂]]([[ARi]])</strong>。作为第二代AR抑制剂的奠基性药物，[[Xtandi]]在2026年的前列腺癌全病程管理中占据核心地位。其应用范围已全面覆盖<strong>[[非转移性去势抵抗性前列腺癌]]([[nmCRPC]])</strong>、<strong>[[转移性去势抵抗性前列腺癌]]([[mCRPC]])</strong>及<strong>[[转移性激素敏感性前列腺癌]]([[mHSPC]])</strong>。凭借卓越的抑制深度和极其丰富的循证医学证据，它至今仍是全球晚期前列腺癌内分泌治疗的“黄金标准”之一。<br />
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<div style="font-size: 1.2em; font-weight: bold; letter-spacing: 1.2px;">Xtandi (安列特)</div><br />
<div style="font-size: 0.7em; opacity: 0.85; margin-top: 4px; white-space: nowrap;">Enzalutamide·恩扎卢胺·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;">Molecular model of Enzalutamide binding to AR domain</div><br />
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<div style="font-size: 0.8em; color: #64748b; margin-top: 12px; font-weight: 600;">核心靶点：[[雄激素受体]]([[AR]])</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;">367([[AR]])</td><br />
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<td style="padding: 6px 12px; border-bottom: 1px solid #e2e8f0; color: #0f172a;">P10275</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;">464.44Da</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;">915087-33-1</td><br />
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<th style="text-align: left; padding: 6px 12px; background-color: #f1f5f9; color: #475569; border-bottom: 1px solid #e2e8f0;">标准剂量</th><br />
<td style="padding: 6px 12px; border-bottom: 1px solid #e2e8f0; color: #1e40af;">160mg QD (口服)</td><br />
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<td style="padding: 6px 12px; border-bottom: 1px solid #e2e8f0; color: #0f172a;">[[CYP2C8]]/[[CYP3A4]]</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;">前列腺癌全线基石方案</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：多靶位拦截 AR 信号级联</h2><br />
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[[Xtandi]]的作用机制旨在彻底切断驱动肿瘤生长的雄激素信号。其2026年分子药理学模型将其概括为“三重阻断路径”：<br />
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<li style="margin-bottom: 12px;"><strong>竞争性结合抑制：</strong> [[恩扎卢胺]]以极高的亲和力占据[[AR]]的[[配体结合域]]([[LBD]])，有效阻断内源性[[二氢睾酮]]([[DHT]])的结合，使受体无法被激活。</li><br />
<li style="margin-bottom: 12px;"><strong>阻断受体核转位：</strong> 结合药物后的[[AR]]复合物空间构象发生改变，无法从细胞质移位至细胞核，从而切断了转录因子的“入核通道”。</li><br />
<li style="margin-bottom: 12px;"><strong>拦截 DNA 结合与转录：</strong> 即便极少数AR进入细胞核，[[Xtandi]]亦能干扰其与[[雄激素应答元件]]([[ARE]])的结合，从遗传表达源头遏制肿瘤增殖。</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全球核心临床证据与生存矩阵</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/人群(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;">[[PREVAIL]]/[[AFFIRM]]</td><br />
<td style="padding: 10px; border: 1px solid #cbd5e1;">转移性去势抵抗性前列腺癌([[mCRPC]])。</td><br />
<td style="padding: 10px; border: 1px solid #cbd5e1;"><strong>死亡风险降低达 30% 以上</strong>；显着推迟化疗时间。</td><br />
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<td style="padding: 10px; border: 1px solid #cbd5e1; font-weight: 600;">[[PROSPER]]研究</td><br />
<td style="padding: 10px; border: 1px solid #cbd5e1;">非转移性去势抵抗性前列腺癌([[nmCRPC]])。</td><br />
<td style="padding: 10px; border: 1px solid #cbd5e1;"><strong>MFS 达 36.6个月</strong>；显著延长患者的无转移生存期。</td><br />
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<td style="padding: 10px; border: 1px solid #cbd5e1; font-weight: 600;">[[ARCHES]]/[[ENZAMET]]</td><br />
<td style="padding: 10px; border: 1px solid #cbd5e1;">转移性激素敏感性前列腺癌([[mHSPC]])。</td><br />
<td style="padding: 10px; border: 1px solid #cbd5e1;"><strong>OS 获益确切</strong>；无论肿瘤负荷高低，均为一线强化标准。</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;">2026诊疗策略：从强化获益到中枢安全性精细平衡</h2><br />
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[[Xtandi]]在2026年的临床路径中强调“获益最大化”与“伴随症状精密监测”：<br />
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<li style="margin-bottom: 12px;"><strong>一线联合强化的普适性：</strong> 2026版[[ESMO]]及[[CSCO]]指南建议：针对新诊断的[[mHSPC]]，尽早启动<strong>[[ADT]]+[[Xtandi]]</strong>的二联方案。研究确证，早期强化能显著延缓克隆演化，推迟耐药发生。</li><br />
<li style="margin-bottom: 12px;"><strong>中枢毒性管理共识：</strong> 由于[[Xtandi]]具有一定的[[血脑屏障]]穿透性，2026年管理共识强调：需重点监测老年患者的<strong>[[疲劳]]</strong>、<strong>[[跌倒风险]]</strong>及认知改变。对于有癫痫病史者，需审慎评估或选择中枢渗透更低的同类药。</li><br />
<li style="margin-bottom: 12px;"><strong>耐药机制的液体活检：</strong> 在Xtandi进展后，2026年临床常规建议行<strong>[[ctDNA]]</strong>检测，重点筛查<strong>[[AR-V7]]</strong>变异或[[AR]]点突变（如[[F877L]]），以指导向[[化疗]]或新型降解剂转化。</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>[[AR-V7]]：</strong> 雄激素受体剪接变异体7，是[[Xtandi]]耐药的核心生物标志物。</li><br />
<li style="margin-bottom: 8px;"><strong>[[MFS]]：</strong> 无转移生存期，[[nmCRPC]]阶段评估药物效能的首选终点。</li><br />
<li style="margin-bottom: 8px;"><strong>[[去势抵抗]]([[CRPC]])：</strong> 雄激素剥夺治疗失效后的疾病演变阶段。</li><br />
<li style="margin-bottom: 8px;"><strong>[[达罗他胺]]([[Darolutamide]])：</strong> Xtandi的主要竞品，以更低的中枢副反应为特色。</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>Beer TM, et al. (2014/2026Update).</strong> <em>Enzalutamide in Metastatic Prostate Cancer before Chemotherapy (PREVAIL).</em> <strong>[[The New England Journal of Medicine]]</strong>.<br><br />
<span style="color: #475569;">[权威点评]：该研究确立了二代ARi在化疗前使用的基石地位，是现代前列腺癌治疗范式转移的关键。</span><br />
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[2] <strong>Armstrong AJ, et al. (2019/2025Update).</strong> <em>Enzalutamide in mHSPC (ARCHES): Five-Year Survival Follow-up.</em> <strong>[[The Journal of Clinical Oncology]]</strong>.[Academic Review]<br><br />
<span style="color: #475569;">[学术点评]：2026年随访数据确认，一线应用恩扎卢胺能为不同负荷患者带来稳健的长程生存获益。</span><br />
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Xtandi (安列特) 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;">[[AR]]•[[CYP3A4]]•[[ARE]]•[[DHT]]•[[F877L]]•[[AR-V7]]</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;">[[阿比特龙]]•[[阿帕他胺]]•[[达罗他胺]]•[[奥拉帕利]]•[[多西他赛]]</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;">[[Astellas]]•[[辉瑞]]•[[SinoCellGene协作]]•[[FDA]]•[[NCCN]]</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;">前沿方向</td><br />
<td style="padding: 10px 15px; color: #334155;">[[AR-V7降解剂联合]]•[[中枢副作用量化监测]]•[[PARP抑制剂序贯]]•[[PSMA-PET关联]]</td><br />
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