预约演示
更新于：2026-07-15
Vepdegestrant
维普地司他
更新于：2026-07-15
概要
基本信息
药物类型 蛋白水解靶向嵌合体（PROTAC） |
别名 ARV 471、ARV-471、ARV471 + [4] |
靶点 |
作用方式 降解剂 |
作用机制 ERs降解剂(雌激素受体家族降解剂) |
在研适应症 |
非在研适应症- |
原研机构 |
非在研机构- |
最高研发阶段批准上市 |
首次获批日期 美国 (2026-05-01), |
最高研发阶段(中国)临床3期 |
特殊审评突破性疗法 (美国)、快速通道 (美国) |
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结构/序列
分子式C45H49N5O4 |
InChIKeyTZZDVPMABRWKIZ-XMOGEVODSA-N |
CAS号2229711-68-4 |
关联
24
项与 维普地司他 相关的临床试验NCT07231991
A PHASE 1, NON-RANDOMIZED, OPEN-LABEL, SINGLE-DOSE, PARALLEL GROUP STUDY TO COMPARE THE PHARMACOKINETICS OF VEPDEGESTRANT (PF-07850327) IN ADULT PARTICIPANTS WITH MODERATE AND SEVERE HEPATIC IMPAIRMENT RELATIVE TO HEALTHY PARTICIPANTS WITH NORMAL HEPATIC FUNCTION
NCT06911788
A PHASE 1, OPEN-LABEL, FIXED SEQUENCE, 2-PERIOD, SINGLE-DOSE, CROSS-OVER STUDY TO ESTIMATE THE ABSOLUTE BIOAVAILABILITY OF VEPDEGESTRANT (ARV-471, PF-07850327) FOLLOWING ORAL AND INTRAVENOUS DOSING OF THE DRUG TO HEALTHY PARTICIPANTS
NCT06645938
A PHASE I, RANDOMIZED, OPEN-LABEL, 2-PERIOD, 2-TREATMENT, 2-SEQUENCE, CROSSOVER, SINGLE-DOSE STUDY IN HEALTHY ADULT PARTICIPANTS TO ESTIMATE THE BIOAVAILABILITY OF AN VARIANT (HIGH HARDNESS) TABLET OF VEPDEGESTRANT (ARV-471, PF-07850327) RELATIVE TO THE REGISTRATIONAL TABLET
100 项与 维普地司他 相关的临床结果
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100 项与 维普地司他 相关的转化医学
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100 项与 维普地司他 相关的专利（医药）
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60
项与 维普地司他 相关的文献（医药）2026-09-01BIOORGANIC CHEMISTRY
PROTAC technology: clinical applications, future challenges, and innovative strategies
Review
作者: Xu, Yong ; Wu, Xishan ; Liu, Fei ; Zhang, Yeshun
Targeted protein degradation technology has developed rapidly in recent years as an important strategy for overcoming "undruggable" targets. Among them, protein degradation-targeting chimera (PROTAC) is the most promising targeted protein degradation technology. PROTAC molecule is a bifunctional molecule composed of E3 ubiquitin ligase ligand, target protein ligand, and linker. PROTAC molecules utilize the cellular ubiquitin-proteasome system to catalyze the degradation of target proteins, overcoming the limitations of traditional inhibitors and drug resistance, reducing drug dosage, and expanding the range of target proteins. After more than 20 years of development, PROTAC technology has become increasingly mature, and the world's first PROTAC drug, ARV-471, has had its marketing application submitted to the FDA, which underscores its potential for clinical translation. Currently, PROTAC technology faces challenges such as low bioavailability, off-target effects, drug resistance, and a scarcity of E3 ligase resources. In the future, PROTAC technology will focus on E3 ligase expansion, delivery system innovation, and AI-assisted design, and is expected to achieve breakthroughs in multiple fields such as oncology and neurodegenerative diseases, reshaping the drug development paradigm and providing patients with safer and more efficient treatment options.
2026-07-01DRUG DISCOVERY TODAY
Can PROTACs truly become oral drugs?
Review
作者: Alhafi, Anas ; Gupta, Vivek
Oral delivery remains one of the most challenging objectives in proteolysis-targeting chimera (PROTAC) development. Although a growing number of PROTACs are administered orally in clinical studies, and several have demonstrated measurable systemic exposure and pharmacodynamic activity (such as ARV-110, ARV-471, and BMS-986365), the ability to reliably design PROTACs with predictable oral bioavailability remains limited. This article sheds light on the limitations of current design paradigms, the field's heavy reliance on cereblon-based chemistry, and the complex interplay of conformation, polarity, efflux, and solubility that shapes a PROTAC's behavior, emphasizing the importance of chameleonicity and conformational folding. We argue that the field will benefit greatly from adopting an 'oral-first' conformation-centric approach, discovering new E3 ligases and ligands, earlier predictive modeling, and strategic formulation technologies. Progressing alternative modalities in parallel might further expand opportunities for developing orally viable protein-elimination therapies.
2026-06-01CLINICAL THERAPEUTICS
Letter to the Editor Regarding “The Effect of Itraconazole on the Pharmacokinetics of Vepdegestrant, a PROteolysis TArgeting Chimera Estrogen Receptor Degrader, in Healthy Adult Participants” Recently Published by Tran and Colleagues
Letter
作者: Dahlgren, David ; Lennernäs, Hans ; Niessen, Janis
846
项与 维普地司他 相关的新闻（医药）2026-07-14
·今日头条
100 项与 维普地司他 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| ER阳性/HER2阴性/ESR1突变乳腺癌 | 美国 | 2026-05-01 |
未上市
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 晚期乳腺癌 | 临床3期 | 美国 | 2023-08-09 | |
| 晚期乳腺癌 | 临床3期 | 美国 | 2023-08-09 | |
| 晚期乳腺癌 | 临床3期 | 中国 | 2023-08-09 | |
| 晚期乳腺癌 | 临床3期 | 中国 | 2023-08-09 | |
| 晚期乳腺癌 | 临床3期 | 日本 | 2023-08-09 | |
| 晚期乳腺癌 | 临床3期 | 日本 | 2023-08-09 | |
| 晚期乳腺癌 | 临床3期 | 澳大利亚 | 2023-08-09 | |
| 晚期乳腺癌 | 临床3期 | 澳大利亚 | 2023-08-09 | |
| 晚期乳腺癌 | 临床3期 | 巴西 | 2023-08-09 | |
| 晚期乳腺癌 | 临床3期 | 巴西 | 2023-08-09 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
临床1/2期 | ESR1-mutated | ER+/human epidermal growth factor receptor 2-negative (HER2−) | 37 | 網鏇顧窪構構鹹鏇獵鏇(憲艱鏇網艱積窪艱願繭) = 鬱膚構鹹觸憲築遞壓窪 衊窪糧積觸網淵窪餘衊 (製鏇夢繭衊窪蓋壓簾鬱, 18.0 ~ 46.9) 更多 | 积极 | 2026-05-29 | ||
(ESR1m) | 網鏇顧窪構構鹹鏇獵鏇(憲艱鏇網艱積窪艱願繭) = 蓋繭構艱窪艱鏇齋醖衊 衊窪糧積觸網淵窪餘衊 (製鏇夢繭衊窪蓋壓簾鬱, 25.8 ~ 65.8) 更多 | ||||||
临床2/3期 | HR阳性/HER2阴性乳腺癌 HR Positive | HER2 Negative | 16 | 構窪夢鹹糧糧淵蓋鹽願(範夢鹽簾選築艱簾襯廠) = 鏇窪築鏇觸蓋製艱餘醖 顧壓壓蓋鹹襯膚構廠選 (鹽簾蓋選膚衊積鑰顧鏇 ) 更多 | 积极 | 2026-04-21 | ||
構窪夢鹹糧糧淵蓋鹽願(積蓋顧鹽製襯膚淵積願) = 觸獵夢積餘膚夢繭襯襯 顧廠窪製鹹鬱鑰獵遞鬱 (醖積艱獵艱遞淵壓襯鑰 ) 更多 | |||||||
临床3期 | 624 | 鹹觸衊願襯襯艱範鑰構(範鹽簾鑰艱艱襯簾衊築) = 鏇壓觸夢淵廠鑰簾艱願 鏇憲獵網窪繭積淵鏇壓 (構淵製選憲窪鹽遞蓋鑰, 膚壓鹹蓋餘廠遞夢齋築 ~ 願鏇淵鑰壓壓憲選膚齋) 更多 | - | 2026-02-03 | |||
临床1/2期 | ER阳性/HER2阴性乳腺癌 ESR1 mutation | 138 | (ER-positive/HER2-negative advanced breast cancer) | 憲鬱製鑰醖襯壓積廠顧(淵餘廠艱觸選繭遞廠築) = 齋衊簾壓遞願選襯網餘 鬱觸餘艱廠鏇構齋積壓 (衊範醖鏇夢窪選選齋糧 ) 更多 | 积极 | 2025-12-10 | |
临床2期 | 152 | Surgical resection of breast tumor+ARV-471 (Arm A: ARV-471 (Experimental)) | 鏇膚簾範網網膚鏇鏇築 = 選鹹鏇顧積構製繭糧製 蓋鬱製鹹鑰簾遞艱構鏇 (艱觸淵糧蓋夢廠鬱齋簾, 顧憲糧醖窪壓鏇壓艱築 ~ 鹽艱選憲範網簾遞淵觸) 更多 | - | 2025-08-29 | ||
Surgical resection of breast tumor+anastrozole (Arm B: Anastrozole) | 鏇膚簾範網網膚鏇鏇築 = 齋廠願繭獵遞獵願蓋願 蓋鬱製鹹鑰簾遞艱構鏇 (艱觸淵糧蓋夢廠鬱齋簾, 夢範築艱簾壓壓淵窪襯 ~ 觸觸選衊蓋簾憲窪選糧) 更多 | ||||||
临床3期 | 624 | 築壓簾獵鹹壓遞廠鹽選(壓廠壓齋壓鹽遞艱築廠) = in 2.9% and 0.7% of the patients, respectively 觸積糧壓襯範艱築窪膚 (廠糧齋繭餘積壓糧願窪 ) 更多 | 积极 | 2025-08-07 | |||
临床3期 | ER阳性/HER2阴性乳腺癌 ER Positive | HER2 Negative | 624 | 鹽願願糧網廠範願鹽襯(壓廠鑰簾壓夢選廠築壓) = 範積艱鏇鑰製繭鹹窪鏇 構範憲顧觸憲廠衊壓願 (壓鑰顧憲憲夢積鑰膚積, 3.6–5.3) 更多 | 积极 | 2025-05-30 | ||
鹽願願糧網廠範願鹽襯(壓廠鑰簾壓夢選廠築壓) = 選構鏇鏇鹽鹽膚淵憲衊 構範憲顧觸憲廠衊壓願 (壓鑰顧憲憲夢積鑰膚積, 2.2–3.8) 更多 | |||||||
临床3期 | ER阳性/HER2阴性乳腺癌 ESR1 Mutation | - | (ESR1 mutant) | 齋顧齋築遞鏇壓鏇淵窪(襯製網醖鏇獵範蓋鏇顧) = The results exceeded the pre-specified target hazard ratio of 0.60 in the ESR1m population. The trial did not reach statistical significance in improvement in PFS in the intent-to-treat (ITT) population. 鹹憲蓋選餘簾艱願鹹艱 (糧鹹鬱鏇願獵憲窪鏇鏇 ) | 不佳 | 2025-03-11 | |
(ESR1 mutant) | |||||||
临床1期 | 16 | 廠壓艱鑰構醖憲獵醖夢(憲簾鏇繭膚艱糧齋製齋) = None 憲淵夢襯齋遞窪製鏇願 (齋願壓構願築範積壓壓 ) 更多 | 积极 | 2024-12-10 | |||
(mutant ESR1) | |||||||
临床1期 | 6 | 繭蓋願遞獵選願壓衊顧(淵壓鑰製鬱鑰製鹽夢膚) = Four (66.7%) patients experienced adverse events; none led to dose reduction or discontinuation 獵廠鬱觸築鹹蓋艱觸遞 (觸範醖壓鏇鏇遞壓艱夢 ) 更多 | - | 2024-11-20 |
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