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艾拉司群 - 版本历史
2026-04-19T12:02:51Z
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223.160.139.141：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
2026-01-26T02:17:23Z
<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>[[艾拉司群]]</strong>（[[Elacestrant]]）是一种新型 <strong>[[选择性雌激素受体降解剂]]</strong>（[[SERD]]），也是首个获批用于临床的口服型 [[SERD]] 类药物。通过与 <strong>[[雌激素受体 α]]</strong>（[[ERα]]）结合，[[艾拉司群]] 不仅能拮抗雌激素的信号传导，还能诱导受体蛋白发生 <strong>[[蛋白酶体降解]]</strong>。在 <strong>[[EMERALD]]</strong> Ⅲ 期临床研究中，[[艾拉司群]] 显著延长了携带 <strong>[[ESR1 突变]]</strong> 的晚期 [[乳腺癌]] 患者的 <strong>[[无进展生存期]]</strong>（[[PFS]]），目前已成为 [[NCCN 指南]] 和 [[ASCO 指南]] 推荐的针对 [[内分泌耐药]] 患者的标准治疗方案。<br />
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<div style="font-size: 1.2em; font-weight: bold; letter-spacing: 1.2px;">[[艾拉司群]]</div><br />
<div style="font-size: 0.7em; opacity: 0.85; margin-top: 4px; white-space: nowrap;">[[Elacestrant]] / [[Orserdu]] (点击展开)</div><br />
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<div style="font-size: 0.8em; color: #64748b; margin-top: 12px; font-weight: 600;">[[艾拉司群]] 分子结构式</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%;">[[CAS 号]]</th><br />
<td style="padding: 6px 12px; border-bottom: 1px solid #e2e8f0; color: #0f172a;">722533-56-4</td><br />
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<th style="text-align: left; padding: 6px 12px; background-color: #f1f5f9; color: #475569; border-bottom: 1px solid #e2e8f0;">药物类型</th><br />
<td style="padding: 6px 12px; border-bottom: 1px solid #e2e8f0; color: #1e40af;">[[口服 SERD]]</td><br />
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<th style="text-align: left; padding: 6px 12px; background-color: #f1f5f9; color: #475569; border-bottom: 1px solid #e2e8f0;">化学式</th><br />
<td style="padding: 6px 12px; border-bottom: 1px solid #e2e8f0; color: #0f172a;">$C_{30}H_{34}N_{2}O_{2}$</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;">454.6 [[g/mol]]</td><br />
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<td style="padding: 6px 12px; border-bottom: 1px solid #e2e8f0; color: #b91c1c;">[[ESR1]] ([[ERα]])</td><br />
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<th style="text-align: left; padding: 6px 12px; background-color: #f1f5f9; color: #475569; border-bottom: 1px solid #e2e8f0;">批准状态</th><br />
<td style="padding: 6px 12px; border-bottom: 1px solid #e2e8f0; color: #166534;">[[FDA]] / [[EMA]] 获批</td><br />
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<th style="text-align: left; padding: 6px 12px; background-color: #f1f5f9; color: #475569;">给药方式</th><br />
<td style="padding: 6px 12px; color: #0f172a;">每日一次口服 (345mg)</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;">作用机制：双管齐下的内分泌打击</h2><br />
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与传统的 <strong>[[他莫昔芬]]</strong>（[[SERM]]）或 <strong>[[芳香化酶抑制剂]]</strong>（[[AI]]）不同，[[艾拉司群]] 具有独特的 <strong>[[SERD]]</strong> 机制：<br />
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<li style="margin-bottom: 12px;"><strong>竞争性抑制：</strong> [[艾拉司群]] 以极高亲和力结合 [[ERα]] 的 <strong>[[配体结合域]]</strong>，直接阻断雌激素与受体的结合。</li><br />
<li style="margin-bottom: 12px;"><strong>受体降解：</strong> 结合后诱导受体发生构象改变，标记为异常蛋白并触发 <strong>[[泛素-蛋白酶体途径]]</strong> 进行降解，从而从根源上清除信号源。</li><br />
<li style="margin-bottom: 12px;"><strong>克服突变：</strong> 针对 <strong>[[D538G]]</strong> 和 <strong>[[Y537S]]</strong> 等突变体，[[艾拉司群]] 依然能有效诱导其降解，这是传统 AI 药物无法实现的。</li><br />
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<h2 style="background: #fff1f2; color: #9f1239; padding: 10px 18px; border-radius: 0 6px 6px 0; font-size: 1.25em; margin-top: 40px; border-left: 6px solid #9f1239; font-weight: bold;">EMERALD 临床研究核心数据</h2><br />
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<th style="padding: 12px; border: 1px solid #cbd5e1; width: 30%;">评估指标</th><br />
<th style="padding: 12px; border: 1px solid #cbd5e1; width: 35%;">[[ESR1 突变]] 亚组获益</th><br />
<th style="padding: 12px; border: 1px solid #cbd5e1; width: 35%;">对照组 ([[标准治疗]])</th><br />
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<td style="padding: 10px; border: 1px solid #cbd5e1; font-weight: 600;">中位 [[PFS]]</td><br />
<td style="padding: 10px; border: 1px solid #cbd5e1; color: #166534; font-weight: bold;">3.8 个月</td><br />
<td style="padding: 10px; border: 1px solid #cbd5e1;">1.9 个月</td><br />
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<td style="padding: 10px; border: 1px solid #cbd5e1; font-weight: 600;">12 个月 [[无进展生存率]]</td><br />
<td style="padding: 10px; border: 1px solid #cbd5e1; color: #166534;">22.3%</td><br />
<td style="padding: 10px; border: 1px solid #cbd5e1;">9.4%</td><br />
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<td style="padding: 10px; border: 1px solid #cbd5e1; font-weight: 600;">[[风险比]] (Hazard Ratio)</td><br />
<td colspan="2" style="padding: 10px; border: 1px solid #cbd5e1;">0.55 (降低 45% 的疾病进展风险)</td><br />
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<h2 style="background: #f0fdf4; color: #166534; padding: 10px 18px; border-radius: 0 6px 6px 0; font-size: 1.25em; margin-top: 40px; border-left: 6px solid #166534; font-weight: bold;">治疗策略与适应症</h2><br />
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<h3 style="margin-top: 0; color: #14532d; font-size: 1.1em;">标准用药指引 (2026 版)</h3><br />
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<li><strong>适用人群：</strong> 经 [[FDA]] 批准的检测证明携带 [[ESR1 突变]]，且在接受至少一轮内分泌治疗后出现疾病进展的 [[ER+/HER2-]] 晚期或转移性 [[乳腺癌]] 患者。</li><br />
<li><strong>用药顺序：</strong> 通常在 <strong>[[CDK4/6 抑制剂]]</strong> 联合 [[AI]] 方案耐药后，作为后线单药治疗的首选。</li><br />
<li><strong>安全性：</strong> 常见不良反应包括恶心、肌肉骨骼疼痛、呕吐和食欲下降。相比肌注 [[氟维司群]]，口服给药极大提升了患者的 <strong>[[依从性]]</strong>。</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>Bidard FC, et al. (2022).</strong> <em>Elacestrant vs Standard Endocrine Therapy in Metastatic Breast Cancer (EMERALD).</em> <strong>[[Journal of Clinical Oncology]]</strong>.<br><br />
<span style="color: #475569;">[关键研究]：奠定了 [[艾拉司群]] 在 [[ESR1 突变]] 晚期乳腺癌中的二/三线标准治疗地位。</span><br />
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[2] <strong>FDA Approval News (2023).</strong> <em>FDA approves elacestrant for ER-positive, HER2-negative, ESR1-mutated advanced or metastatic breast cancer.</em><br><br />
<span style="color: #475569;">[监管动态]：标志着首个 [[口服 SERD]] 正式进入临床实践。</span><br />
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[[艾拉司群]] · 知识图谱<br />
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<td style="width: 90px; background-color: #f8fafc; color: #334155; font-weight: 600; padding: 10px 12px; text-align: right; vertical-align: middle;">[[药物类别]]</td><br />
<td style="padding: 10px 15px; color: #334155;"><strong>[[选择性雌激素受体降解剂]]</strong> ([[SERD]]) • [[口服制剂]]</td><br />
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<td style="width: 90px; background-color: #f8fafc; color: #334155; font-weight: 600; padding: 10px 12px; text-align: right; vertical-align: middle;">[[对标药物]]</td><br />
<td style="padding: 10px 15px; color: #334155;">[[氟维司群]] (肌注) • [[他莫昔芬]] • [[来曲唑]]</td><br />
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<td style="width: 90px; background-color: #f8fafc; color: #334155; font-weight: 600; padding: 10px 12px; text-align: right; vertical-align: middle;">[[核心关联]]</td><br />
<td style="padding: 10px 15px; color: #334155;">[[ESR1 突变]] • [[EMERALD 研究]] • [[内分泌耐药]]</td><br />
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