贝组替凡(Belzutifan) - 药物靶点：HIF-2α_在研适应症：转移性肾细胞癌，副神经节瘤，嗜铬细胞瘤_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Belzutifan (USAN/INN)、MK 6482、MK-6482

+ [5]

靶点

HIF-2α

作用方式

抑制剂

作用机制

HIF-2α抑制剂(内皮PAS结构域包含蛋白-1抑制剂)

治疗领域

肿瘤心血管疾病遗传病与畸形+ [6]

在研适应症

转移性肾细胞癌副神经节瘤嗜铬细胞瘤+ [30]

非在研适应症

终末期肾脏病肝损伤

原研机构

Merck Sharp & Dohme Corp.

在研机构

Merck Sharp & Dohme LLC

Merck Sharp & Dohme Corp.

默沙东研发（中国）有限公司

+ [7]

非在研机构-

权益机构

Exelixis, Inc.

Merck & Co., Inc.

Peloton Therapeutics, Inc.

最高研发阶段批准上市

首次获批日期

美国 (2021-08-13),

希佩尔·林道综合征

最高研发阶段(中国)批准上市

特殊审评优先审评 (美国)、突破性疗法 (美国)、加速批准 (美国)、孤儿药 (美国)、优先审评 (中国)、孤儿药 (日本)、孤儿药 (韩国)、附条件批准 (欧盟)、孤儿药 (澳大利亚)

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结构/序列

分子式C17H12F3NO4S

InChIKeyLOMMPXLFBTZENJ-ZACQAIPSSA-N

CAS号1672668-24-4

关联

36

项与贝组替凡相关的临床试验

NCT07593040

/ Not yet recruiting临床2期IIT

A Randomized Phase 2 Trial of Neoadjuvant Pembrolizumab Plus Belzutifan With or Without Lenvatinib in Patients With Localized Renal Cell Carcinoma

This study is designed to evaluate the efficacy of belzutifan in combination with pembrolizumab with or without lenvatinib in the neoadjuvant setting, followed by adjuvant pembrolizumab versus adjuvant pembrolizumab alone, as treatment for participants with intermediate-high and high risk clear cell renal cell carcinoma (ccRCC).

开始日期2026-06-01

申办/合作机构

Vall d'Hebron Institut d'Oncologia

NCT07489495

/ Recruiting临床3期

A Phase 3, Randomized, Double-blind, Study of Belzutifan + Zanzalintinib Versus Belzutifan + Placebo in Participants With Advanced RCC Who Have Progressed on or After Both PD-1/L1 and VEGF-TKI Therapies in Sequence or in Combination (LITESPARK-034)

Researchers are looking for new ways to treat advanced renal cell carcinoma (RCC).
A standard (usual) treatment for certain people with RCC is belzutifan (a study medicine), which is a targeted therapy. Targeted therapy is a treatment that works to control how specific types of cancer cells grow and spread. Researchers want to learn if adding another targeted therapy called zanzalintinib (another study medicine) can treat more people with advanced RCC than belzutifan alone.
The goal of this study is to learn if people who receive belzutifan and zanzalintinib live longer overall and without the cancer getting worse compared to people who receive belzutifan and placebo.

开始日期2026-04-09

申办/合作机构

Merck Sharp & Dohme LLC

[+1]

NCT07405164

/ Recruiting临床3期

A Multicenter, Open-label, Phase 3 Extension Study to Evaluate the Long-term Efficacy and Safety in Participants Who Are Currently on Treatment in a Belzutifan Study (LITESPARK-043)

Researchers are looking for new ways to treat advanced solid tumors and von Hippel-Lindau (VHL)-related tumors:
* Advanced means the cancer has spread to other parts of the body (metastatic) or cannot be removed with surgery
* Solid tumors are cancers mostly in body organs and tissues, not in the blood or other body liquids
* VHL-related tumors are tumors caused by VHL disease. VHL disease is passed down from parents to children and people with VHL disease have a higher chance of getting certain types of cancer
Researchers want to learn about the long-term effects of a trial medicine called belzutifan. Belzutifan, also called MK-6482, is designed to block a protein that helps tumors grow and survive. This is an extension trial, which means only people who were in certain other belzutifan trials (called parent trials) may be able to join. The goal of this trial is to learn how long people live after they start taking belzutifan.

开始日期2026-03-23

申办/合作机构

Merck Sharp & Dohme LLC

100 项与贝组替凡相关的临床结果

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100 项与贝组替凡相关的转化医学

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100 项与贝组替凡相关的专利（医药）

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209

项与贝组替凡相关的文献（医药）

2026-06-01·American journal of ophthalmology case reports

Very rapid response to belzutifan of VHL-related intracranial and retinal hemangioblastomas

Article

作者: Verrico, Antonio ; Hadjistilianou, Doris ; Piatelli, Gianluca ; Borzì, Leonardo ; Mercuri, Claudia ; Milanaccio, Claudia ; Gaggero, Gabriele ; Ramaglia, Antonia ; Molteni, Marta ; Piccolo, Gianluca ; Di Profio, Sonia ; Pagliara, Alessandra ; De Giuseppe, Sara ; Serafino, Massimiliano

Background:

Belzutifan, a hypoxia-inducible factor-2α (HIF-2α) inhibitor approved for von Hippel-Lindau (VHL) disease-related tumors, induces radiological responses in hemangioblastomas, but the timing and extent of early changes are not well defined.

Case presentation:

A 9-year-old girl was admitted with nausea, vomiting, and ataxia. Brain MRI showed a cystic cerebellar mass, which was fully resected; histology and genetic testing confirmed VHL. Follow-up revealed a small stable cerebellar residual. Two years later, she developed multiple retinal hemangioblastomas (RH) with major visual decline and new cerebellar nodules. Argon laser photocoagulation provided no lasting benefit, prompting initiation of belzutifan. The drug was well tolerated over the first six months, with only grade 1 anemia. Psychological assessments documented excellent adaptation, preserved quality of life, stable daily routines, and regular school attendance. MRI demonstrated a marked reduction in two of the three cerebellar nodules as early as day 15 of cycle 1, followed by progressive shrinkage and stabilization by cycle 4. No new RH emerged, and visual acuity improved within eight weeks of treatment and then remained stable.

Conclusions:

This case highlights an unusually rapid radiological response of VHL-associated cerebellar and retinal hemangioblastomas shortly after belzutifan initiation, suggesting that imaging performed soon after treatment onset may detect changes earlier than commonly reported. A slight but measurable improvement in visual acuity was also observed, despite the overall structural stability of the RH. These findings support the potential value of early radiological and functional assessment in selected patients receiving HIF-2α inhibitors.

2026-05-15·JOURNAL OF CLINICAL INVESTIGATION

Genome-wide CRISPR screen identifies a cytokine-enhancer circuit driving HIF-2α activation in renal cancer

Article

作者: Mani, Ram ; Brugarolas, James ; Zhou, Jin ; Bi, Xianju ; Liu, Hongyi ; Zhang, Cheng ; Simon, Jeremy M. ; Nathan, James A. ; Wang, Tao ; Gao, Yunpeng ; Fang, Jun ; Hu, Lianxin ; Adachi, Yayoi ; Liang, Qian ; Liao, Chengheng ; Zhang, Qing

Resistance to HIF-2α inhibitors such as belzutifan underscores the need to better understand how HIF-2α is transcriptionally regulated in clear cell renal cell carcinoma (ccRCC). Here, we uncover a cytokine-driven enhancer mechanism that sustains HIF-2α expression through the JAK1/STAT3 signaling pathway. Using a genome-wide CRISPR screen in von Hippel–Lindau–deficient (VHL-deficient) ccRCC cells, we identified SOCS3 as a key negative regulator of HIF-2α. Mechanistically, loss of SOCS3 activates JAK1/STAT3 signaling, leading to the recruitment of STAT3 to distal enhancers upstream of endothelial PAS domain-containing protein ( EPAS1 ) that physically loop to its promoter to drive HIF-2α transcription. This cytokine-enhancer circuit was recapitulated in samples from patients with ccRCC and functionally validated using CRISPR interference (CRISPRi), which disrupted enhancer-promoter looping and reduced tumor growth in HIF-2α–dependent models. SOCS3 overexpression or pharmacologic inhibition of JAK1/STAT3 markedly suppressed HIF-2α expression and tumor progression both in vitro and in vivo. Unlike prior studies focusing on VHL/HIF occupancy–driven enhancer activation, this work defines a trans -acting cytokine–JAK1/STAT3 pathway that transcriptionally controls EPAS1 . Together, these findings reveal a targetable enhancer mechanism that sustains HIF-2α expression and suggest that combined inhibition of JAK1/STAT3 and HIF-2α may overcome therapeutic resistance in kidney cancer. We discovered that cytokine signaling drives kidney cancer by activating a genetic circuit that boosts HIF-2α expression, offering new targets to overcome treatment resistance.

2026-05-04·JOURNAL OF EXPERIMENTAL MEDICINE

Targeting conserved domains of hypoxia-inducible factors for cancer therapy

Article

作者: Drehmer, Daiana ; Yang, Yongkang ; Wicks, Elizabeth E. ; Chen, Chelsey ; Jackson, Walter ; Lee, Sophia N. ; Salman, Shaima ; Semenza, Gregg L. ; Huang, Tina Y. ; Lyu, Yajing ; Datan, Emmanuel ; Dordai, Dominic ; Hwang, Yousang ; Prabhakar, Nanduri R. ; Peng, Ying-Jie ; Li, Oscar ; Kumar, Anmol ; Cho, Ellen ; MacKerell, Alexander D.

Hypoxia-inducible factors 1 and 2 (HIF-1/2) function as master regulators of cancer progression by regulating angiogenesis, cancer stem cell specification, epithelial–mesenchymal transition, immune evasion, tissue invasion, and metastasis. We utilized computer-aided drug discovery and cell-based reporter assays to identify dual HIF-1/2 inhibitors, which bind directly to highly conserved domains of HIF-1α and HIF-2α, disrupt dimerization with HIF-1β, and trigger proteasomal degradation, thereby inhibiting HIF-1/2 transcriptional activity. These inhibitors and derivative compounds block growth and vascularization of breast, colorectal, head/neck, melanoma, and prostate tumors as monotherapy, and overcome resistance to anti-CTLA-4 or anti-PD-1 immunotherapy, with an aggregate complete response rate of over 50%, through reprogramming of the tumor immune cell microenvironment. Compared with the HIF-2–selective inhibitors belzutifan and PT2385, dual HIF-1/2 inhibitor 1.21S9N showed superior activity against breast and colorectal cancer models, respectively. PT2385 caused breathing abnormalities, whereas 1.21S9N did not. The drugs are orally bioavailable, and no safety concerns were identified even after extended or supratherapeutic dosing.

491

项与贝组替凡相关的新闻（医药）

2026-06-16

·Firstwordpharma

FDA clears Merck & Co.'s Welireg, Keytruda combo in adjuvant kidney cancer

The FDA has approved a combination of Merck & Co.'s Keytruda (pembrolizumab) with the company's HIF-2α inhibitor Welireg (belzutifan) as an adjuvant treatment for adults with clear cell renal cell carcinoma (ccRCC) at risk of recurrence after surgery. The approval also applied to Keytruda's subcutaneous formulation, Keytruda Qlex (pembrolizumab/berahyaluronidase alfa-pmph). The decision, which follows a priority review, is based on the Phase III LITESPARK-022 trial, which enrolled 1841 patients with prior nephrectomy who were at intermediate-high or high risk of recurrence, or who had resected metastases with no evidence of disease. Patients were randomised to receive Welireg plus Keytruda as adjuvant therapy or Keytruda plus placebo. At a prespecified interim analysis, Welireg plus Keytruda was associated with a 28% benefit on the primary endpoint of disease-free survival (DFS), defined as time to recurrence, metastasis or death, with 186 events and 246 events in the Welireg and comparator arms, respectively. Median DFS wasn't reached in either arm, while overall survival (OS) data weren't mature at the interim analysis. Welireg already has a kidney cancer indication, having been approved in late 2023 for advanced RCC patients previously treated with PD-1/L1 and VEGF-targeted therapies (see – KOL Views Q&A: Welireg's safety will aid Merck & Co.'s upstream ambitions in RCC). Meanwhile, Friday's approval gives Keytruda it's fourth kidney cancer indication following two in the first-line advanced setting with Pfizer's Inlyta (axitinib) or Eisai's Lenvima (lenvatinib), and another in the post-nephrectomy setting based on results from the KEYNOTE-564 trial, where it showed a significant 38% improvement in OS in patients with high-risk disease. However, several experts interviewed by FirstWord for a Therapy Trends report last year indicated they planned to stick with Bristol Myers Squibb's Opdivo (nivolumab) for immuno-oncology combinations in RCC given the uncertainty around treatment sequencing (see – Spotlight On: Opdivo combos hold firm in RCC, despite growing pressure from Keytruda). The content above comes from the network. if any infringement, please contact us to modify.

临床结果上市批准优先审批免疫疗法

2026-06-15

·癌度

《癌度快报》：多款蛋白降解疗法公布积极数据，血液肿瘤治疗迎来新突破！

临床试验病友交流群（点击）一、新药快讯 1、多款蛋白降解疗法公布积极数据，血液肿瘤治疗迎来新突破！近日多项早期临床研究报道了蛋白降解剂在血液肿瘤中的积极进展：①潜在"best-in-class"BTK降解剂bexobrutideg治疗慢淋（CLL）的1期数据显示，中位无进展生存期22.1个月，客观缓解率83%，对BTK抑制剂耐药及中枢神经系统受累患者也有效；②IKZF1/3分子胶降解剂cemsidomide联合地塞米松治疗复发/难治性多发性骨髓瘤，推荐剂量下缓解率达53%，部分患者实现微小残留病阴性。此外，靶向BCR-ABL1的潜在"best-in-class"小分子抑制剂ELVN-001治疗慢粒（CML）的1期数据显示，80mg剂量组主要分子学缓解率达61%，停药率仅6%。蛋白降解疗法正在从概念走向临床，为耐药血液肿瘤患者带来新希望。 2、默沙东贝组替凡联合K药获美国FDA批准，用于肾癌术后辅助治疗！近日，跨国药企默沙东的HIF-2α抑制剂贝组替凡（Welireg）联合帕博利珠单抗（Keytruda）获FDA批准，用于肾切除术后复发风险增加的透明细胞肾细胞癌（ccRCC）患者的辅助治疗。这是首个在肾癌辅助治疗中证实优于K药单药的联合方案。数据显示，联合治疗将疾病复发或死亡风险降低28%，24个月无病生存率分别为81%和74%。贝组替凡是一款口服HIF-2α抑制剂，此前已在欧美日中获批用于VHL综合征相关肿瘤。联合方案的安全性可管理，最常见的≥3级不良事件为贫血、ALT升高和低氧血症。本次获批标志着HIF-2α抑制剂首次进入早期肾癌治疗领域，也为术后高危患者提供了一个潜在的新标准选择。 3、AKT抑制剂卡匹色替新适应症在美获批，用于PTEN缺陷型前列腺癌！近日，AKT抑制剂卡匹色替（Capivasertib）联合阿比特龙和泼尼松获FDA批准，用于PTEN缺陷型转移性雄激素通路调节初治或敏感型（即传统上的mHSPC）前列腺癌。这是首个也是目前唯一针对这一特定基因型前列腺癌的靶向治疗方案。此次获批基于III期CAPItello-281研究：卡匹色替联合组中位影像学无进展生存期达33.2个月，较对照组延长7.5个月，疾病进展或死亡风险降低19%。卡匹色替是全球首款获批的AKT抑制剂，此前已在美国、中国等地获批用于HR+/HER2-乳腺癌。安全方面，≥3级不良事件发生率67%，以皮疹和高血糖最常见。二、抗癌前沿 1、ASCO 2026：癌症治疗转向"精准加减法" 今年ASCO多项研究指向同一个方向：治疗强度不是越多越好，而是要和患者实际获益精准匹配。乳腺癌OPTIMA研究显示，67.8%临床高危患者通过基因检测可安全免除化疗，5年生存率几乎不变；结肠癌CIRCULATE研究发现，术后ctDNA阳性的II期患者如不化疗，3年无病生存率仅38%，化疗后升至77%；膀胱癌IMvigor011研究则证实ctDNA指导下的免疫治疗可显著延长MRD阳性患者生存；乳腺癌腋窝手术SENOMAC研究进一步表明，部分患者省略腋窝清扫，生存不变但上肢功能明显更好。癌症治疗正在从"多治一步更保险"转向"谁该加、谁该减"的精准时代。 “吉爱3000”惠民检项目，最低2000+可及的基因检测专属福利，全球新药临床试验免费用药、基因检测报告解读，详情微信“长按”下图扫码联系癌度王博进行咨询。另外，由于微信公众平台的机制调整，恳请各位粉丝朋友花一两秒钟帮我们点亮文章下方的【小手】和【爱心】，这对我们至关重要。谢谢大家！点亮小手爱心，送来温暖鼓励

2026-06-15

·耐心+等待+资金+勇气+读书+跑步

默沙东是怎么赚钱的？

默沙东（Merck & Co./MSD）是典型的研发驱动型创新药企，靠专利保护期内的高价原研药和疫苗赚取高额毛利，2025年总营收约650亿美元。 🏆 明星产品撑起半壁江山 Keytruda（K药/帕博利珠单抗）：全球"药王"，2025年销售额约317亿美元，占默沙东总营收近49%，靠覆盖数十种癌症适应症的PD-1抑制剂独家专利高价销售。 Gardasil/Gardasil 9（九价HPV疫苗）：第二大单品，约52亿美元，全球HPV疫苗市场近乎垄断。其他：Winrevair（肺动脉高压新药，~14亿）、Lynparza（奥拉帕利）、Januvia（已过专利期逐步下滑）等。 💰 盈利模式本质高研发投入→重磅专利药→全球高定价销售：每年R&D投入占营收约25%~27%，成功一款"重磅炸弹"（Blockbuster）药物靠专利期独占定价权赚回数十倍回报，毛利率常年80%+。渠道：卖给全球医院、药店、政府疾控（疫苗）、兽医渠道（动物保健）。风险与对策：极度依赖K药（近50%营收），2028年K药核心专利到期面临"专利悬崖"，默沙东正通过并购（Verona Pharma、Prometheus等）、拓展新适应症/皮下剂型、布局ADC/心血管新药来寻找接力产品。简单来说——默沙东主要就是靠Keytruda抗癌药和HPV疫苗在专利保护期内卖高价赚钱，辅以动物保健业务，再用赚来的现金流砸研发和并购养下一个重磅药。它的CEO有多少个？什么时候成立的？什么时候进入中国卖药的？他的未来发展和方向是什么？帮你汇总默沙东（Merck & Co./MSD）的基本情况和未来方向： 👔 CEO人数上市公司只有1位全球CEO——现任是罗伯特·戴维斯（Robert M. Davis），2021年上任，兼任董事长。 📅 成立与入华时间成立：1891年1月1日，由德裔移民乔治·默克（George Merck）在美国新泽西州创立，原为德国默克美国分公司，1953年与沙东（Sharp & Dohme）合并为Merck Sharp & Dohme（MSD）。进入中国：1992年正式进入中国大陆开展业务；1989年已将重组乙肝疫苗技术零利润转让给中国（建北京/深圳车间）。1994年与华东医药合资成立杭州默沙东制药。 🔮 未来发展与战略方向核心目标是应对2028年Keytruda专利悬崖，打造多引擎增长：延长K药生命周期：推皮下注射剂型、拓展早期癌症辅助治疗新适应症。肿瘤"超越PD-1"：重金布局ADC（收购/合作科伦博泰等）、双抗、个性化肿瘤疫苗，目标2030年肿瘤业务>250亿美元。第二增长曲线——心血管/代谢：以Winrevair（肺动脉高压）、口服PCSK9抑制剂、GLP-1受体激动剂为核心，目标心血管代谢业务约150亿美元。免疫/自免+抗感染：收购Prometheus（TL1A抑制剂）、同润生物（CD3/CD19双抗），布局自免与HIV新药。中国战略："三擎合一"（上海总部+北京研发中心+杭/甬/津工厂），未来5年预计40+新产品/新适应症在华获批，并从"产品引进"转向与中国Biotech合作共研（中国研发、全球共享）。简单说——默沙东正用K药赚的钱疯狂买管线和拓新赛道（ADC、心血管、自免），争取在K药专利到期后平稳过渡。我的理解是，卖人类药赚钱，可是没有人能长生不老，为什么你能不倒闭呢？它的卖些什么药？多少钱一瓶？谁需要？成本是多少？它的药攻克的是哪个方向？默沙东卖的主打产品、国内大致售价、适用人群、攻克方向和成本情况整理如下： 💊 默沙东核心产品速览（中国市场）其他还有乐卫玛 Lenvima（与卫材合作的肝癌/甲状腺癌靶向药）、择必达（丙肝）、普瑞明（巨细胞病毒预防）、肺炎球菌疫苗等。 🎯 攻克的疾病方向肿瘤免疫（核心）：PD-1抑制剂激活免疫系统识别并清除肿瘤细胞，覆盖肺癌/黑色素瘤/消化道肿瘤等多癌种。疫苗预防：HPV疫苗预防宫颈癌、肛门癌、生殖器疣；肺炎球菌疫苗防肺炎/脑膜炎。代谢/慢病：2型糖尿病（DPP-4）、血脂异常（依折麦布/益适纯）。感染/重症：碳青霉烯类抗生素、抗真菌（科赛斯）、抗病毒（HIV、CMV、新冠）。新拓展：肺动脉高压、HIF-2α抑制剂（肾癌/Welireg）、RSV单抗等。 💰 关于"成本" 药企不公开单品生产成本，且生物药/化药差异大：生物制剂（K药、Winrevair）：原材料（细胞培养、纯化）占比较低，主要成本是前期数十年R&D、失败损耗、临床试验（默沙东年R&D约300亿美元），单支边际生产成本远低于售价。小分子/疫苗（Januvia、HPV疫苗）：原料和灌装成本也只占售价极小比例，专利期内靠高价回收巨额研发投入。专利过期后仿制药价格可跌至原研10%~20%，侧面反映原研溢价主要来自研发摊销而非物料成本。我的理解是，癌细胞药30万，HPV疫苗2600一针，糖尿病药120元，三级高血压10万元，新冠药1500元，一个都不便宜。它的药是不是假的，为什么这么贵？它在中国的发展方向是什么？为什么会有这些疾病？怎么预防？然后这家药企就会倒闭？你一口气问了好几个点，我逐一给你说清楚： 💊 药是假的吗？为什么这么贵？正规渠道（医院/疾控中心）打的默沙东药绝对是真药，受NMPA严格监管。市面上偶有黑诊所拿生理盐水冒充HPV疫苗属于诈骗案件，跟默沙东无关。贵的原因：专利独占期：专利保护期内无仿制药竞争，可自由定价回收研发成本。研发沉没成本：一款新药平均耗资10亿+美元、耗时10余年，失败率约90%，成功药需摊薄失败项目的钱。生物工艺+冷链：K药（单抗）、HPV疫苗（病毒样颗粒）生产工艺极复杂，全程需超低温冷链储运。全球差别定价：发达国家（美欧）承担主要利润，发展中国家价格相对低，但中国此前未纳入国家免规仍以自费市场定价为主。 🦠 这些病怎么来的？怎么预防？ HPV相关疾病（宫颈癌/肛门癌/生殖器疣）：经性接触或皮肤黏膜接触感染人乳头瘤病毒（HPV），高危型持续感染使抑癌蛋白p53/pRb失活→细胞癌变。预防：接种HPV疫苗（默沙东九价）+定期宫颈筛查（TCT+HPV检测）。癌症（肺癌/黑色素瘤等）：基因突变、吸烟、病毒感染、环境致癌物致免疫细胞无法识别肿瘤。预防：戒烟、防晒、早筛（低剂量CT查肺癌等），晚期用K药免疫激活治疗。 2型糖尿病：遗传+肥胖+久坐致胰岛素抵抗。预防：控制体重、运动、低糖饮食。感染（细菌/真菌/新冠）：病原体入侵，预防：卫生习惯、必要时疫苗/抗病毒药物。 🇨🇳 默沙东在中国的发展方向推行"耀赢未来"和"三擎合一"战略：引入新品：2025—2029年计划向中国引入40+项新产品/新适应症，多款纳入医保。本土化合作：与科伦博泰（ADC抗肿瘤）、恒瑞、翰森制药License-in/out合作，"中国发现→全球应用"。研发+制造：北京研发中心+上海总部+杭州/宁波/天津工厂，推进本地化生产。适应集采：成熟药（西格列汀等）接受集采降价，聚焦创新药推广。 🏢 默沙东会倒闭吗？基本不可能倒闭，但会经历"专利悬崖"阵痛： K药（2028年专利到期）和HPV疫苗专利到期后仿制药上市，收入会大幅下滑（专利悬崖）。默沙东手持百亿现金，正通过并购（Acceleron/Prometheus/Verona等）、ADC管线（与科伦博泰/第一三共合作）、拓展Winrevair心血管新药、早期癌症新适应症来填坑。全球Top10药企，动物保健+疫苗+成熟药仍贡献稳定现金流，属典型"转型阵痛"而非破产风险。我的理解是，癌症，吸烟肺癌，久坐，吃糖，糖尿病，然后知道这些要死人，那就不去那里就好啦，那么，默沙东这家企业，不就倒闭了吗？哈哈哈。

100 项与贝组替凡相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D11954	-	-	DB15463

研发状态

批准上市

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
转移性肾细胞癌	日本	MSD KK (Tokyo)	2025-06-24
副神经节瘤	美国	Merck & Co., Inc.	2025-05-14
副神经节瘤	美国	Merck Sharp & Dohme Corp.	2025-05-14
嗜铬细胞瘤	美国	Merck Sharp & Dohme Corp.	2025-05-14
嗜铬细胞瘤	美国	Merck & Co., Inc.	2025-05-14
晚期肾细胞癌	澳大利亚	Merck Sharp & Dohme (Australia) Pty Ltd.	2022-12-22
血管母细胞瘤	澳大利亚	Merck Sharp & Dohme (Australia) Pty Ltd.	2022-12-22
胰腺神经内分泌肿瘤	澳大利亚	Merck Sharp & Dohme (Australia) Pty Ltd.	2022-12-22
肾细胞癌	加拿大	Merck Canada, Inc.	2022-07-11
希佩尔·林道综合征	美国	Merck Sharp & Dohme Corp.	2021-08-13

未上市

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
局部晚期透明细胞肾细胞癌	申请上市	欧盟	Merck & Co., Inc.	2024-12-12
不可切除的肾细胞癌	临床3期	美国	Merck Sharp & Dohme LLC	2025-11-26
不可切除的肾细胞癌	临床3期	阿根廷	Merck Sharp & Dohme LLC	2025-11-26
不可切除的肾细胞癌	临床3期	澳大利亚	Merck Sharp & Dohme LLC	2025-11-26
不可切除的肾细胞癌	临床3期	奥地利	Merck Sharp & Dohme LLC	2025-11-26
不可切除的肾细胞癌	临床3期	比利时	Merck Sharp & Dohme LLC	2025-11-26
不可切除的肾细胞癌	临床3期	巴西	Merck Sharp & Dohme LLC	2025-11-26
不可切除的肾细胞癌	临床3期	克罗地亚	Merck Sharp & Dohme LLC	2025-11-26
不可切除的肾细胞癌	临床3期	捷克	Merck Sharp & Dohme LLC	2025-11-26
不可切除的肾细胞癌	临床3期	丹麦	Merck Sharp & Dohme LLC	2025-11-26

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临床结果

适应症

分期

评价

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT07227402 (LITESPARK-033, ASCO2026)	临床3期	肾细胞癌辅助	904	Belzutifan plus zanzalintinib	網鑰膚醖鬱衊夢淵鹽鏇(獵鬱選衊廠衊鹹製獵淵) = 願糧積齋積蓋衊夢廠夢遞獵淵糧餘簾鏇糧醖蓋 (窪憲遞選糧膚選壓夢鏇 ) 更多	积极	2026-05-29
				Cabozantinib	網鑰膚醖鬱衊夢淵鹽鏇(獵鬱選衊廠衊鹹製獵淵) = 齋廠淵鏇餘鬱醖鬱顧鹹遞獵淵糧餘簾鏇糧醖蓋 (窪憲遞選糧膚選壓夢鏇 )
ASCO2026	N/A	希佩尔·林道综合征	9	Belzutifan	獵衊願鹹鏇鏇廠鹹齋顧(餘夢網醖積鬱網選膚餘) = 顧積鏇廠醖齋觸憲顧艱襯製選選選遞齋遞範齋 (鬱積餘範壓網膚襯廠顧, 42.1 ~ 99.6) 更多	积极	2026-05-29
LITESPARK-005 (ASCO2026)	N/A	晚期肾细胞癌 tobacco use \| sex \| BMI ... 更多	2,844	Belzutifan	廠窪獵製顧築簾糧餘蓋(齋淵醖窪簾廠淵鏇鹽醖) = 範窪鬱鹹夢鹹築淵餘積積構壓顧製獵憲鑰蓋觸 (網鹹艱夢憲鏇獵顧構壓 ) 更多	积极	2026-05-29
NCT02861573 (KEYNOTE-365, ASCO2026)	临床1/2期	转移性去势抵抗性前列腺癌 Hypoxia-inducible factor 2α (HIF-2α)	21	Belzutifan 120 mg	鏇醖壓鏇衊壓壓鹹獵憲(願膚衊糧獵網襯築蓋鏇) = 願願膚齋窪衊繭艱鑰繭願網鹽觸艱糧顧製積襯 (願餘積製遞構淵糧獵衊, 10.8 ~ NR) 更多	不佳	2026-05-29
ASCO2026	N/A	肾细胞癌	150	Belzutifan (Responder)	網鹹膚網糧積願獵簾鑰(積夢顧簾鑰網選積鬱糧) = 獵築鑰鑰窪構網鏇餘鬱窪醖遞膚鏇醖鏇構壓蓋 (鹹艱選憲製艱構鑰窪廠 ) 更多	积极	2026-05-29
				Belzutifan	網鹹膚網糧積願獵簾鑰(積夢顧簾鑰網選積鬱糧) = 鑰襯獵願鏇壓淵鹽窪壓窪醖遞膚鏇醖鏇構壓蓋 (鹹艱選憲製艱構鑰窪廠 ) 更多
ASCO2026	N/A	肾细胞癌一线	190	Cabozantinib	顧範繭觸鑰衊衊壓艱餘(鑰鏇餘鑰壓衊築鹽襯鹽) = 繭膚製積鹽憲繭鏇觸鹹淵選鬱構構齋糧繭網範 (夢鏇製餘獵餘鹹網膚鹹 ) 更多	积极	2026-05-29
				Belzutifan	顧範繭觸鑰衊衊壓艱餘(鑰鏇餘鑰壓衊築鹽襯鹽) = 淵淵餘遞網網簾艱膚艱淵選鬱構構齋糧繭網範 (夢鏇製餘獵餘鹹網膚鹹 ) 更多
AACR2026	N/A	希佩尔·林道综合征	14	Belzutifan	淵襯蓋繭網範範鹹積夢(製範鬱觸繭簾願膚蓋醖) = The most common AEs were anemia (35%), dizziness (21%), and headache (21%). 齋範壓憲鬱觸顧積糧構 (簾範繭築範鑰壓網鹹簾 ) 更多	积极	2026-04-21
NCT04586231 (LITESPARK-011, ASCO_GU2026) 人工标引	临床3期	晚期肾细胞癌	747	Belzutifan 120 mg + Lenvatinib 20 mg (IA1)	築鏇積衊醖窪衊艱製艱(鹹選鬱鏇壓夢襯憲壓鑰) = 鑰鏇壓築範繭簾衊觸構憲蓋齋範壓廠積齋鏇艱 (繭艱糧獵憲築蓋遞顧網, 11.1–16.6) 更多	积极	2026-02-26
				Cabozantinib 60 mg (IA1)	築鏇積衊醖窪衊艱製艱(鹹選鬱鏇壓夢襯憲壓鑰) = 廠選糧鑰糧製範網簾醖憲蓋齋範壓廠積齋鏇艱 (繭艱糧獵憲築蓋遞顧網, 9.2–11.1) 更多
NCT05239728 (LITESPARK-022, ASCO_GU2026) 人工标引	临床3期	肾细胞癌辅助	1,841	Pembrolizumab + belzutifan	糧積製膚鏇夢積窪鹽鬱(鹹願襯範鹽艱憲窪壓觸): HR = 0.72 (95% CI, 0.59 ~ 0.87), P-Value = 0.0003 更多	积极	2026-02-26
				Pembrolizumab + placebo
ASCO_GU2026	N/A	肾细胞癌	240	Belzutifan responders	齋積選廠範齋衊範鑰衊(鹽餘繭簾糧鹽淵築鏇願) = 窪鬱壓顧簾齋製淵衊遞醖範壓築獵積鹽餘蓋淵 (衊餘鬱鹽網範夢積廠淵 ) 更多	积极	2026-02-26
				Belzutifan non-responders	齋積選廠範齋衊範鑰衊(鹽餘繭簾糧鹽淵築鏇願) = 願製網壓鹹觸網積願淵醖範壓築獵積鹽餘蓋淵 (衊餘鬱鹽網範夢積廠淵 ) 更多