预约演示
更新于：2025-10-04
Olomorasib
奥洛莫拉西布
更新于：2025-10-04
概要
基本信息
原研机构 |
在研机构 |
非在研机构- |
最高研发阶段临床3期 |
首次获批日期- |
最高研发阶段(中国)临床3期 |
特殊审评突破性疗法 (美国)、孤儿药 (美国)、孤儿药 (日本) |
登录后查看时间轴
结构/序列
分子式C25H19ClF2N4O3S |
InChIKeyOZUPICRWMLEFCS-UHFFFAOYSA-N |
CAS号2771246-13-8 |
关联
15
项与 奥洛莫拉西布 相关的临床试验NCT07124013
An Open-Label, Phase 1 Study to Investigate the Comparability of the Pharmacokinetics of Olomorasib (LY3537982) Between Two Capsule Formulations and to Evaluate the Food Effect in Healthy Japanese Participants
NCT07137689
Pharmacokinetics of LY3537982 Following a Single Dose in Participants With Renal Impairment Compared With Participants With Normal Renal Function
NCT07044271
An Open-Label, Randomized, 3-Way Crossover Study Comparing the Pharmacokinetics of Multiple Olomorasib (LY3537982) Capsules
100 项与 奥洛莫拉西布 相关的临床结果
登录后查看更多信息
100 项与 奥洛莫拉西布 相关的转化医学
登录后查看更多信息
100 项与 奥洛莫拉西布 相关的专利（医药）
登录后查看更多信息
6
项与 奥洛莫拉西布 相关的文献（医药）2025-07-01CRITICAL REVIEWS IN ONCOLOGY HEMATOLOGY
KRAS G12C inhibitors as monotherapy or in combination for metastatic colorectal cancer: A proportion and comparative meta-analysis of efficacy and toxicity from phase I-II-III trials
Review
作者: Öksüz, Nejat Emre ; Akkus, Erman ; Erul, Enes
BACKGROUND:
1-2 % of metastatic colorectal cancers (mCRC) harbor an activating KRAS-G12C mutation. This study aims to pool the results of available clinical trials of KRAS-G12C inhibitors, comparing monotherapy and combinations.
METHODS:
A systematic literature search was conducted in the MEDLINE database and ESMO/ASCO meeting abstracts. Phase I-II-III trials that investigated a KRAS-G12C inhibitor in patients with mCRC were included. The primary endpoints were objective response rate (ORR) and progression-free survival (PFS). Pooled proportions and comparative subgroup analyses for monotherapy and combinations were presented with the random effects model.
RESULTS:
596 patients with previously treated mCRC in 14 study cohorts treated with one of sotorasib, adagrasib, divarasib, or olomorasib as monotherapy or in combination with cetuximab/panitumumab were included. Combination treatment revealed an ORR of 33.9 % (95 %CI: 20.7-48.4) (I2: 87.1), which is significantly higher than monotherapy [16.7 %, (95 %CI: 8.3-27.3) (I2: 73.2)] (p = 0.045). Median PFS was significantly longer with the combination [5.7 months (95 %CI: 4.4-7.1) (I2: 80.8) vs. 4.2 months (95 %CI: 3.6-4.7) (I2:0.0), p = 0.027]. Grade 3-4 treatment-related adverse events (TRAEs) were significantly more frequent with the combination [32.8 % (95 %CI: 26.4-39.6) (I2:42.5) vs.16.5 % (95 %CI: 4.9-33.1) (I2: 84.2), p = 0.047]. Common adverse events specific to the combinations were skin toxicities, paronychia, and hypomagnesemia.
CONCLUSION:
This analysis suggests that KRAS-G12C inhibitors in combination with anti-EGFR agents may provide a doubled ORR and 1.5-month PFS benefit compared to monotherapy in previously treated mCRC patients, but with a doubled grade 3-4 TRAEs, including skin toxicities, paronychia, and hypomagnesemia. Treatment preferences should be individualized in these highly pretreated patients.
2025-03-27JOURNAL OF MEDICINAL CHEMISTRY
Discovery of Elironrasib (RMC-6291), a Potent and Orally Bioavailable, RAS(ON) G12C-Selective, Covalent Tricomplex Inhibitor for the Treatment of Patients with RAS G12C-Addicted Cancers
Article
作者: Liu, Yang ; Jiang, Jingjing ; Ling, Yun ; Wang, Zhengping ; Marquez, Abby ; Knox, John E. ; Flagella, Michael ; Zhao, Ruiping ; Pota, Kristof ; Yang, Yu Chi ; Schulze, Christopher J. ; Cregg, James ; Wang, Zhican ; Smith, Jacqueline A. M. ; Singh, Mallika ; Tomlinson, Aidan C. A. ; Nichols, Robert ; Yano, Jason ; Koltun, Elena S. ; Seamon, Kyle J. ; Huang, Yue ; Gill, Adrian L. ; Wildes, David ; Holderfield, Matthew ; Zhuang, Yongxian ; Wei, Xing
The discovery of elironrasib (RMC-6291) represents a significant breakthrough in targeting the previously deemed undruggable GTP-bound, active KRASG12C. To target the active state of RAS (RAS(ON)) directly, we have employed an innovative tri-complex inhibitor (TCI) modality involving formation of a complex with an inhibitor, the intracellular chaperone protein CypA, and the target protein KRASG12C in its GTP-bound form. The resulting tri-complex inhibits oncogenic signaling, inducing tumor regressions across various preclinical models of KRASG12C mutant human cancers. Here we report structure-guided medicinal chemistry efforts that led to the discovery of elironrasib, a potent, orally bioavailable, RAS(ON) G12C-selective, covalent, tri-complex inhibitor. The investigational agent elironrasib is currently undergoing phase 1 clinical trials (NCT05462717, NCT06128551, NCT06162221), with preliminary data indicating clinical activity in patients who had progressed on first-generation inactive state-selective KRASG12C inhibitors.
2024-10-01Nature Chemical Biology
Direct RAS inhibitors turn 10
Article
作者: Ostrem, Jonathan M L ; Peters, Ulf ; Shokat, Kevan M
RAS proteins, central drivers of cancer, appeared ′undruggable′ for almost 30 years.Here we provide a personal perspective on the effort leading to our initial report of KRASG12C inhibitors in 2013, and the decade of discoveries that followed.
100 项与 奥洛莫拉西布 相关的药物交易
登录后查看更多信息
研发状态
10 条进展最快的记录, 后查看更多信息
登录
| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| KRAS G12C突变非小细胞肺癌 | 临床3期 | 美国 | 2023-12-21 | |
| KRAS G12C突变非小细胞肺癌 | 临床3期 | 中国 | 2023-12-21 | |
| KRAS G12C突变非小细胞肺癌 | 临床3期 | 日本 | 2023-12-21 | |
| KRAS G12C突变非小细胞肺癌 | 临床3期 | 澳大利亚 | 2023-12-21 | |
| KRAS G12C突变非小细胞肺癌 | 临床3期 | 奥地利 | 2023-12-21 | |
| KRAS G12C突变非小细胞肺癌 | 临床3期 | 比利时 | 2023-12-21 | |
| KRAS G12C突变非小细胞肺癌 | 临床3期 | 巴西 | 2023-12-21 | |
| KRAS G12C突变非小细胞肺癌 | 临床3期 | 加拿大 | 2023-12-21 | |
| KRAS G12C突变非小细胞肺癌 | 临床3期 | 捷克 | 2023-12-21 | |
| KRAS G12C突变非小细胞肺癌 | 临床3期 | 丹麦 | 2023-12-21 |
登录后查看更多信息
临床结果
临床结果
适应症
分期
评价
查看全部结果
| - | 78 | Olomorasib+Pembrolizumab+Platinum containing dual drug chemotherapy | 鬱願網鹽夢構糧構願襯(觸窪鬱襯鬱鏇簾鹽鏇積) = 築廠鏇積鑰積蓋窪獵膚 膚蓋構鏇膚製鬱顧齋鬱 (艱襯構襯蓋築簾壓鹹醖 ) 更多 | 积极 | 2025-09-08 | ||
Olomorasib+Pembrolizumab+Platinum containing dual drug chemotherapy (PD-L1< 1%) | 鬱願網鹽夢構糧構願襯(觸窪鬱襯鬱鏇簾鹽鏇積) = 糧夢壓廠簾窪範憲蓋蓋 膚蓋構鏇膚製鬱顧齋鬱 (艱襯構襯蓋築簾壓鹹醖 ) 更多 | ||||||
| - | 85 | 夢簾製築簾築遞選鏇觸(鹽簾醖餘顧網憲廠鏇獵) = 築衊壓糧窪廠築鏇廠壓 鑰遞艱製鑰築鬱餘淵鹽 (憲廠膚鏇製壓積憲鬱製 ) 更多 | 积极 | 2025-09-07 | |||
夢簾製築簾築遞選鏇觸(鹽簾醖餘顧網憲廠鏇獵) = 觸鹹築觸願獵醖觸築廠 鑰遞艱製鑰築鬱餘淵鹽 (憲廠膚鏇製壓積憲鬱製 ) 更多 | |||||||
临床1/2期 | 43 | 觸夢糧觸顧夢壓淵鏇淵(積簾範繭顧糧餘製廠衊) = 33%/30% 鹹簾簾襯獵蓋簾鬱齋築 (鏇艱顧願壓選鬱鏇齋齋 ) 更多 | 积极 | 2025-05-30 | |||
临床1期 | 一线 KRAS G12C | 48 | 齋願範鹹範襯簾鹽衊築(憲選淵襯窪齋築淵淵製) = mild, reversible, and reported in 1 participant 蓋鑰糧糧積遞遞選範鏇 (構獵衊糧淵築醖選遞鹹 ) 更多 | 积极 | 2025-04-28 | ||
临床1/2期 | KRAS G12C突变非小细胞肺癌 KRAS G12C | 50 | 艱構積鬱觸遞衊憲鑰壓(範構選網艱夢製網淵窪) = 構網鑰觸鏇築餘鑰艱鹽 衊顧窪網網範網壓壓餘 (鏇糧鏇選憲壓醖選醖願, 78 ~ 99) 更多 | 积极 | 2024-05-24 | ||
(PD-L1 ≥50%) | 壓遞繭醖顧齋鏇選鏇鬱(遞積窪鬱網齋糧鹽廠齋) = 網構醖夢齋鬱獵選壓繭 鬱淵積餘窪獵鑰願醖願 (齋繭壓選壓艱襯蓋廠鹽 ) | ||||||
临床1/2期 | KRAS G12C突变的实体瘤 KRAS G12C | 157 | 範糧選鬱願觸鏇蓋遞齋(觸選廠獵衊壓衊襯膚願) = 觸憲齋製鑰遞蓋襯簾簾 鏇鬱醖蓋齋壓鹹遞顧艱 (憲艱遞選觸範蓋廠繭繭 ) 更多 | 积极 | 2024-05-24 | ||
(CRC) | 範糧選鬱願觸鏇蓋遞齋(觸選廠獵衊壓衊襯膚願) = 齋觸齋艱蓋鏇製窪簾範 鏇鬱醖蓋齋壓鹹遞顧艱 (憲艱遞選觸範蓋廠繭繭 ) 更多 | ||||||
临床1期 | 胃肠道肿瘤 KRAS G12C | 119 | 窪願鑰獵積鹹醖衊觸蓋(餘糧齋壓糧餘網鹹艱醖) = 廠製簾淵淵糧觸簾願壓 憲窪觸夢觸選鏇製遞憲 (壓獵獵鏇獵膚壓窪艱淵 ) 更多 | 积极 | 2024-01-18 | ||
(CRC) | 膚簾網鬱齋鹹艱顧鹹鑰(製獵壓壓簾製廠鬱齋鏇) = 廠構齋繭簾鏇遞蓋鏇襯 積壓夢窪窪簾襯齋夢簾 (積齋獵蓋觸顧襯獵蓋廠 ) 更多 | ||||||
临床1期 | KRAS G12C突变的实体瘤 KRAS G12C Mutation | 56 | (NSCLC (KRAS G12Ci naïve)) | 艱遞築壓鬱積衊艱餘製(艱鹽積壓壓壓製醖觸壓) = No DLTs were observed 觸願襯築鹹構積遞繭廠 (繭鏇襯遞淵鬱壓鹽蓋顧 ) 更多 | 积极 | 2023-04-15 | |
(NSCLC(Prior KRAS G12Ci treated)) |
登录后查看更多信息
转化医学
使用我们的转化医学数据加速您的研究。
登录
或
药物交易
使用我们的药物交易数据加速您的研究。
登录
或
核心专利
使用我们的核心专利数据促进您的研究。
登录
或
临床分析
紧跟全球注册中心的最新临床试验。
登录
或
批准
利用最新的监管批准信息加速您的研究。
登录
或
特殊审评
只需点击几下即可了解关键药物信息。
登录
或
Eureka LS:
全新生物医药AI Agent 覆盖科研全链路，让突破性发现快人一步
立即开始免费试用!
智慧芽新药情报库是智慧芽专为生命科学人士构建的基于AI的创新药情报平台，助您全方位提升您的研发与决策效率。
立即开始数据试用!
智慧芽新药库数据也通过智慧芽数据服务平台，以API或者数据包形式对外开放，助您更加充分利用智慧芽新药情报信息。
生物序列数据库
生物药研发创新
免费使用
化学结构数据库
小分子化药研发创新
免费使用