Zanzalintinib

加利福尼亚州阿拉米达 ——2026 年 6 月 22 日 ——Exelixis, Inc.（纳斯达克代码：EXEL）今日公布 III 期关键性临床试验 STELLAR-303 双主要终点总生存期（OS）的最终分析数据，本次分析对象为无活动性肝转移（非肝转移，NLM）亚组患者。该试验对比 zanzalintinib 联合 atezolizumab（Tecentriq®）与 regorafenib，用于经治微卫星稳定型转移性结直肠癌（mCRC）患者。 数据显示，在非肝转移亚组人群中，联合治疗组总生存期呈现获益趋势，但不具备统计学显著性（分层风险比：0.83；95% 置信区间：0.66–1.05；P=0.1185）。zanzalintinib 联合 atezolizumab 组中位总生存期 15.9 个月，regorafenib 组为 12.7 个月。 非肝转移亚组中 zanzalintinib 联合 atezolizumab 的安全性特征与此前意向治疗（ITT）人群披露数据保持一致，未发现新的安全风险信号。 Exelixis 此前已公布，STELLAR-303 试验另一项双主要终点已达到，在意向治疗全人群中总生存期获得具有统计学意义的显著改善，意向治疗人群包含所有随机入组患者，无论是否存在活动性肝转移。意向治疗人群总生存期显著获益的完整研究数据已于 2025 年欧洲肿瘤内科学会年会公布，并发表于《柳叶刀》期刊。 2026 年 2 月，Exelixis 宣布美国食品药品监督管理局（FDA）受理 zanzalintinib 联合 atezolizumab 的新药上市申请，适应症为：既往接受过氟尿嘧啶、奥沙利铂、伊立替康化疗方案治疗的转移性结直肠癌患者；若患者为 RAS 野生型，还需既往接受过抗表皮生长因子受体（EGFR）药物治疗。FDA 依据《处方药使用者付费法案》设定目标审批截止日期为 2026 年 12 月 3 日。 关于 STELLAR-303 试验 STELLAR-303（试验编号 NCT05425940）是一项全球多中心、随机、开放标签 III 期临床研究，患者按 1:1 比例随机分组，zanzalintinib 联合 atezolizumab 组 451 例，regorafenib 组 450 例。入组人群为既往接受过系统治疗的微卫星稳定型转移性结直肠癌患者。 本试验设立两项共同主要终点：意向治疗全人群总生存期、无活动性肝转移亚组患者总生存期。意向治疗人群包含全部随机入组受试者，不区分是否合并肝转移；无肝转移亚组为研究者评估基线不存在活动性肝转移的患者。 次要终点包含意向治疗人群与无肝转移亚组的无进展生存期、客观缓解率以及缓解持续时间。更多试验详情可查阅 ClinicalTrials.gov 官网。 关于 Zanzalintinib Zanzalintinib 是一款全新口服激酶抑制剂，可抑制 TAM 激酶家族（TYRO3、AXL、MER）、MET 及血管内皮生长因子受体的活性。上述激酶在肿瘤发生发展进程中起到关键作用，参与肿瘤细胞增殖、远处转移、血管生成、耐药以及肿瘤免疫逃逸。 Zanzalintinib 临床开发项目包含多项正在开展及规划中的关键性临床试验，探索其在结直肠癌、透明细胞与非透明细胞肾细胞癌、神经内分泌肿瘤中的治疗潜力；另有早期临床研究探索其用于脑膜瘤、肺癌、去势抵抗性前列腺癌。 Zanzalintinib 目前仍处于在研阶段，尚未获批任何适应症，相关临床试验仍在推进。 关于结直肠癌（CRC） 结直肠癌是美国第三高发恶性肿瘤，也是癌症死亡主要诱因之一。1 2026 年美国预计新增约 159000 例确诊病例，约 55000 例患者死于该病。结直肠癌确诊高峰年龄段为 65 至 74 岁，男性、非西班牙裔美国印第安 / 阿拉斯加原住民群体发病率更高。近四分之一结直肠癌患者确诊时已发生远处转移，该阶段五年生存率仅约 15%。肝脏是结直肠癌最常见转移部位，肝转移会大幅缩短患者生存期；仅接受姑息化疗的肝转移患者中位五年生存率不足 14%。 关于 Exelixis Exelixis 是一家布局全球的肿瘤领域生物企业，深耕新一代抗肿瘤药物与联合治疗方案研发，走在肿瘤诊疗创新前沿。依托强大的药物发现与临床开发能力，公司持续丰富产品线，通过具备差异化临床价值的小分子药物与生物制剂管线，覆盖越来越多瘤种与适应症。 公司长期深耕基础科研、广泛开展行业合作，依托完善研发体系推进核心分子管线，其中包含全新口服激酶抑制剂 zanzalintinib；同时持续拓展核心商业化产品 CABOMETYX®（cabozantinib）的临床应用价值。 Exelixis 以突破性科研为驱动，致力于开发变革性疗法，为更多肿瘤患者带去生存希望。如需了解企业详情以及助力肿瘤患者更好康复、延长生存期的企业使命，可访问官网www.exelixis.com。 免责声明：所载内容来源互联网，仅供参考。转载稿件版权归原作者和机构所有，如有侵权，请联系我们删除。

ALAMEDA, Calif. --(BUSINESS WIRE)--Jun. 22, 2026-- Exelixis, Inc. (Nasdaq: EXEL) today announced results from the final analysis of the dual primary endpoint of overall survival ( OS) in the subset of patients without active liver metastases (non-liver metastases, NLM) in the phase 3 STELLAR-303 pivotal trial evaluating zanzalintinib in combination with atezolizumab (Tecentriq®) versus regorafenib in previously treated non-microsatellite instability (MSI)-high metastatic colorectal cancer (mCRC). The results showed a non-statistically significant trend in OS favoring the combination in the NLM subpopulation (stratified hazard ratio: 0.83; 95% confidence interval: 0.66–1.05; P=0.1185), with median OS values of 15.9 months with zanzalintinib in combination with atezolizumab, and 12.7 months with regorafenib. The safety profile of zanzalintinib in combination with atezolizumab in the NLM subgroup was consistent with that previously reported in the intention-to-treat (ITT) population, and no new safety signals were identified. Exelixis previously announced that STELLAR-303 met its other dual primary endpoint, demonstrating a statistically significant improvement in OS in the ITT population, which included all randomized patients regardless of the presence of active liver metastases. Detailed results demonstrating the statistically significant improvement in OS in the ITT population were presented at the 2025 European Society for Medical Oncology Congress and published in The Lancet . In February 2026 , Exelixis announced that the U.S. Food and Drug Administration (FDA) accepted the company’s New Drug Application (NDA) for zanzalintinib, in combination with atezolizumab, for the treatment of patients with mCRC who have been previously treated with fluoropyrimidine-, oxaliplatin- and irinotecan-based chemotherapy, and, if RAS wild-type, an anti-epidermal growth factor receptor (EGFR) therapy. The FDA assigned a Prescription Drug User Fee Act target action date of December 3, 2026 . Detailed findings from the NLM subgroup analysis will be submitted for presentation at an upcoming medical conference. About STELLAR-303 STELLAR-303 (NCT05425940) is a global, multicenter, randomized, phase 3, open-label study that randomized patients 1:1 to either zanzalintinib in combination with atezolizumab (n=451) or regorafenib (n=450). The study includes patients with previously treated non-MSI-high mCRC. The dual primary endpoints of the study are OS in the ITT population and in the NLM subgroup of patients. The ITT population consisted of all randomized patients, regardless of the presence of liver metastases. The NLM subgroup consisted of patients who did not have active liver metastases at baseline as determined by investigator assessment. Secondary endpoints include progression-free survival, objective response rate and duration of response in the ITT population and in the NLM subgroup of patients. More information about the trial is available at ClinicalTrials.gov. About Zanzalintinib Zanzalintinib is a novel oral kinase inhibitor that inhibits the activity of the TAM kinases (TYRO3, AXL, MER), MET and VEGF receptors. These kinases play important roles in oncogenic processes, including tumor cell proliferation, metastasis, angiogenesis, drug resistance and evasion of antitumor immunity. The zanzalintinib development program includes a series of ongoing and planned pivotal trials to explore its therapeutic potential in CRC, clear cell and non-clear cell renal cell carcinoma, and neuroendocrine tumors, as well as earlier-stage trials in meningioma, lung cancer and castration-resistant prostate cancer. Zanzalintinib is an investigational agent that is not approved for any use and is the subject of ongoing clinical trials. About CRC CRC is the third most common cancer and a leading cause of cancer-related deaths in the U.S .1 Approximately 159,000 new cases will be diagnosed in the U.S . in 2026, with around 55,000 expected deaths from the disease.1 CRC is most frequently diagnosed among people aged 65-74 and is more common in men and in people of non-Hispanic American Indian/Alaska Native descent.2 Nearly a quarter of CRC cases are diagnosed at the metastatic stage, at which point the five-year survival rate is around just 15%.1,2 The liver is the most common site for CRC metastasis. Liver metastases significantly impact survival, with a median five-year survival rate of less than 14% when treated with palliative chemotherapy.3 About Exelixis Exelixis is a globally ambitious oncology company innovating next-generation medicines and regimens at the forefront of cancer care. Powered by drug discovery and development excellence, we are rapidly evolving our product portfolio to target an expanding range of tumor types and indications with our clinically differentiated pipeline of small molecules and biotherapeutics. This comprehensive approach harnesses decades of robust investment in our science and partnerships to advance our pipeline of franchise molecules, including our novel oral kinase inhibitor zanzalintinib, and to extend the impact of our flagship commercial product, CABOMETYX® (cabozantinib). Exelixis is driven by a bold scientific pursuit to create transformational treatments that give more patients hope for the future. For information about the company and its mission to help cancer patients recover stronger and live longer, visit www.exelixis.com, follow @ExelixisInc on X (Twitter), like Exelixis, Inc. on Facebook and follow Exelixis on LinkedIn. Forward-Looking Statements This press release contains forward-looking statements, including, without limitation, statements related to: the presentation of detailed results from the STELLAR-303 NLM subgroup analysis at an upcoming medical conference and Exelixis’ scientific pursuit to create transformational treatments that give more patients hope for the future. Any statements that refer to expectations, projections or other characterizations of future events or circumstances are forward-looking statements and are based upon Exelixis’ current plans, assumptions, beliefs, expectations, estimates and projections. Forward-looking statements involve risks and uncertainties. Actual results and the timing of events could differ materially from those anticipated in the forward-looking statements as a result of these risks and uncertainties, which include, without limitation: the availability of data at the referenced times; complexities and the unpredictability of the regulatory review and approval processes in the U.S. and elsewhere, including with respect to Exelixis’ NDA for zanzalintinib for the treatment of patients with previously treated metastatic CRC, when used in combination with atezolizumab, including the risk that the FDA may not approve zanzalintinib as a treatment for metastatic CRC in a timely fashion, if at all; Exelixis’ continuing compliance with applicable legal and regulatory requirements; unexpected concerns that may arise as a result of the occurrence of adverse safety events or additional data analyses of clinical trials evaluating zanzalintinib; Exelixis’ dependence on third-party vendors for the development, manufacture and supply of zanzalintinib; Exelixis’ ability to protect its intellectual property rights; market competition; changes in economic and business conditions; and other factors affecting Exelixis and its development programs detailed from time to time under the caption “Risk Factors” in Exelixis’ most recent Annual Report on Form 10-K and subsequent Quarterly Reports on Form 10-Q, and in Exelixis’ future filings with the Securities and Exchange Commission. All forward-looking statements in this press release are based on information available to Exelixis as of the date of this press release, and Exelixis undertakes no obligation to update or revise any forward-looking statements contained herein, except as required by law. Exelixis, the Exelixis logo and CABOMETYX are registered U.S. trademarks of Exelixis. TECENTRIQ is a registered U.S. trademark of Genentech, a member of the Roche Group. View source version on businesswire.com: https://www.businesswire.com/news/home/20260621469249/en/ Investors Contact: Andrew Peters SVP, Strategy and Investor Relations Exelixis, Inc. 650-837-7248 apeters@exelixis.com Media Contact: Stekki Millman Senior Director, Public Affairs Exelixis, Inc. 650-837-7187 smillman@exelixis.com Source: Exelixis, Inc.