预约演示
更新于：2026-07-16
Olomorasib
奥洛莫拉西布
更新于：2026-07-16
概要
基本信息
药物类型 小分子化药 |
别名 KRAS-G12C-II、LY 3537982、LY-3537982 + [1] |
作用方式 抑制剂 |
作用机制 KRAS G12C抑制剂(KRAS G12C突变抑制剂) |
非在研适应症- |
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) |
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结构/序列
分子式C25H19ClF2N4O3S |
InChIKeyOZUPICRWMLEFCS-UHFFFAOYSA-N |
CAS号2771246-13-8 |
关联
18
项与 奥洛莫拉西布 相关的临床试验NCT07639242
Olomorasib Plus Pembrolizumab as First-Line Treatment for KRAS G12C Mutant, PD-L1 TPS 1-49% Locally Advanced or Metastatic Non-Small Cell Lung Cancer (NSCLC)
NCT07227025
A Phase 1/2 Study Evaluating the Safety and Efficacy of Amivantamab and Olomorasib Combination Therapy in Metastatic Non-small Cell Lung Cancer
NCT07439250
A Phase 1, Open-Label, Fixed-Sequence Study to Investigate the Effect of Fluconazole on the Pharmacokinetics of Olomorasib (LY3537982) in Healthy Participants
100 项与 奥洛莫拉西布 相关的临床结果
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100 项与 奥洛莫拉西布 相关的转化医学
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100 项与 奥洛莫拉西布 相关的专利（医药）
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12
项与 奥洛莫拉西布 相关的文献（医药）2026-05-28CANCER INVESTIGATION
A Systematic Review of the Efficacy of KRAS p.G12C Inhibitors in Metastatic Colorectal Cancer: The Current State of Science
Review
作者: Baytar, Doga Kahramangil ; Boby, Jeffrey Mathew ; Benny, Jame Mathew ; Peniche, Paola Zinser ; Sahin, Ibrahim Halil ; Ilerhunmwuwa, Nosakhare
BACKGROUND:
KRAS p.G12C (c.34G > T) inhibitors have been reported to have varying survival outcomes in CRC patients across studies. Hence, our review aimed to provide a comprehensive understanding of the efficacy and safety of these agents among the CRC population.
METHODS:
Major databases, including but not limited to PubMed and Ovid, were searched for original clinical trials assessing the efficacy or safety of KRAS p.G12C (c.34G > T) inhibitors in CRC patients through May 2025. Studies with non-G12C KRAS-mutated populations were excluded. Data on patient demographics and various variables, including but not limited to OS, PFS, and TRAE incidence, were extracted from included studies.
RESULTS:
Our systematic review analyzed 18 trials and 1011 patients. Adagrasib monotherapy yielded a median PFS of 4.4-5.6 months, an OS of 10-19.8 months, and an ORR of 19-23%, while its combination with cetuximab reported a PFS of 6.9 months, an OS of 13.4-15.9 months and an ORR of 34-46%. Sotorasib monotherapy (960 mg) reported a PFS of 4 months, an OS of 10.6 months, and an ORR of 9.7. When combined with panitumumab, 960 mg sotorasib demonstrated better results with a PFS of 5.6-5.7 months, OS of 15.2 months and an ORR of 12.5-30%. Similarly, divarasib monotherapy led to a PFS of 5.6-6.9 months and an ORR of 20%, while its combination with cetuximab resulted in a PFS of 8.1 months and an ORR of 62.5%. Combination therapy of olomorasib and MK-1084, which are new-generation KRAS p.G12C (c.34G > T) inhibitors, with cetuximab also demonstrated highly promising efficacy with ORR of 38-44% and 50%, respectively. Olomorasib with cetuximab also showed a PFS of 6.6-7.5 months. Nausea, vomiting, diarrhea, rash, and increased AST/ALT were the most common TRAEs.
CONCLUSIONS:
Initial results of KRAS-G12C inhibitors appear highly promising when they are combined with anti-EGFR therapy compared to historical therapeutic agents indicated for patients with chemotherapy-refractory CRC. Encouraging benefits warrant frontline trials with these novel therapeutics.
2026-04-09Future Oncology
SUNRAY-01 trial protocol: an innovative study design of olomorasib and pembrolizumab with or without chemotherapy in
KRAS
G12C NSCLC
Article
作者: Arbour, Kathryn C. ; Spira, Alexander I. ; Sabari, Joshua K. ; Negrao, Marcelo V. ; Burns, Timothy F. ; R. Lindsay, Colin ; Leal, Ticiana ; Merced, Alyson ; Visseren-Grul, Carla ; Girard, Nicolas ; Reck, Martin ; Peters, Solange ; Rodriguez, Luis Paz-Ares ; William, William Nassib ; Shun, Lu ; Fasnacht, Nicolas ; Hochmair, Maximilian ; Capuzzo, Frederico ; Henning Grønberg, Bjørn ; Nishio, Makoto
CLINICAL TRIAL REGISTRATION:
www.clinicaltrials.gov identifier is NCT06119581. EudraCT: 2023-503412-33-00.
2026-04-01Journal of Thoracic Oncology
Efficacy and Safety of Olomorasib in Combination With Pembrolizumab in Treatment of Patients With KRAS G12C-Mutant Advanced NSCLC
Article
作者: Dragnev, Konstantin H ; Han, Ji-Youn ; Burns, Timothy F ; Ammakkanavar, Natraj Reddy ; Takeuchi, Shinji ; Chu, Quincy ; Heist, Rebecca S ; Chisamore, Michael J ; You, Arthur Xintian ; Oxnard, Geoffrey R ; McNeely, Samuel C ; Sacher, Adrian ; Deming, Dustin ; Koyama, Takafumi ; Willard, Melinda D ; Italiano, Antoine ; Fujiwara, Yutaka ; Chen, Aaron ; Lee, Dae Ho ; Cassier, Philippe A ; Singhal, Nimit ; Hollebecque, Antoine ; Murciano-Goroff, Yonina R ; Fink, Aaron ; Spira, Alexander
INTRODUCTION:
Immunotherapy-based regimens are the standard first-line treatment for KRAS G12C-mutant NSCLC, but outcomes remain suboptimal. Prior attempts to combine KRAS G12C inhibitors with immunotherapy have been challenged by toxicity. We report results from LOXO-RAS-20001, a phase 1/2 trial evaluating the combination of olomorasib with pembrolizumab in KRAS G12C-mutant NSCLC, including in first-line setting.
METHODS:
Patients with advanced KRAS G12C-mutant NSCLC in any treatment line, including prior KRAS G12Ci and immunotherapy were eligible. Any PD-L1 level (0%-100%) was permitted. Three dose levels of olomorasib (50, 100, and 150 mg twice daily) plus pembrolizumab were evaluated, focusing on 50 and 100 mg twice daily for safety and efficacy.
RESULTS:
A total of 99 enrolled patients had a median age of 68 (range, 42-83) years; 52% of tumors were PD-L1 0% to 49%, 36% were PD-L1 more than or equal to 50%, and 51% were first line. Of 93 patients treated at 50 or 100 mg twice daily, 76 (81.7%) experienced treatment-related adverse event (TRAEs) of any grade, most often, diarrhea (34.4%) and increased alanine aminotransferase/aspartate aminotransferase level (24.7%/22.6%). Grade more than or equal to 3 TRAEs were found in 33.3%. TRAEs led to olomorasib dose reductions in 20.4% and discontinuation of both therapies in 6.5% of patients. Among 91 efficacy-evaluable patients, at a median follow-up of 12.5 months (interquartile range, 6.2-16.9), objective response rate was 57.1% (95% confidence interval [CI], 46.3-67.5) across all PD-L1 expression levels, 73.9% (95% CI, 58.9-85.7) in first line, and 90% (95% CI, 68.3-98.8) in first-line patients with PD-L1 more than or equal to 50%.
CONCLUSION:
Olomorasib plus pembrolizumab demonstrated manageable safety and promising antitumor activity in patients with KRAS G12C-mutant advanced NSCLC across PD-L1 expression levels, especially in the high PD-L1 first-line setting.
100 项与 奥洛莫拉西布 相关的药物交易
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研发状态
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 |
|---|---|---|---|---|
| KRAS G12C突变结直肠癌 | 临床3期 | 中国 | 2025-03-01 | |
| KRAS突变非小细胞肺癌 | 临床3期 | 中国 | 2025-03-01 | |
| 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 |
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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 | 85 | 繭膚膚願網醖構窪糧選(選積鏇築餘簾餘壓積糧) = 1 (8.3%) and 1 (5.6%) respectively 繭鑰鬱壓顧蓋餘膚築繭 (糧衊壓蓋淵繭鏇壓淵壓 ) 更多 | 积极 | 2026-05-29 | |||
(PD-L1 <1%) | |||||||
临床1期 | 162 | 淵繭鹹選衊獵繭艱衊糧(選艱蓋製範艱艱繭簾願) = 廠蓋憲選齋壓餘顧醖繭 鬱繭鏇蓋遞淵齋觸壓窪 (築艱繭廠鹹膚蓋廠鏇遞, 75.3 ~ 100.0) 更多 | 积极 | 2026-05-29 | |||
淵繭鹹選衊獵繭艱衊糧(選艱蓋製範艱艱繭簾願) = 膚範構鹽壓鏇壓膚積製 鬱繭鏇蓋遞淵齋觸壓窪 (築艱繭廠鹹膚蓋廠鏇遞, 79.0 ~ 95.0) 更多 | |||||||
临床2/3期 | KRAS G12C突变非小细胞肺癌 KRAS G12C | 168 | 築糧簾餘繭網觸壓醖淵(鑰鑰淵顧鹽醖鏇憲衊廠) = 網衊襯鑰窪鑰膚壓範壓 廠鬱鑰範壓願衊衊鹹鬱 (糧糧鹹築鹹糧壓網憲夢 ) | 积极 | 2026-04-09 | ||
Placebo+pembrolizumab | 衊廠選獵衊窪積衊壓糧(遞製衊顧願衊廠鬱築簾) = 鹽齋願鑰憲齋襯鏇襯遞 鹹壓廠襯齋觸製醖簾憲 (壓鬱簾憲積觸鹽廠鹹齋, 10 ~ 35) 更多 | ||||||
临床3期 | KRAS G12C突变非小细胞肺癌 KRAS G12C | 718 | Olomorasib+pembro | 餘鹽構膚積憲鏇鬱遞製(壓夢構鹹顧築遞淵膚遞) = 觸壓醖襯憲窪範積願遞 衊憲蓋顧衊觸膚艱觸糧 (壓衊鑰窪繭鏇築願鑰網, 36.1 ~ NR) | 积极 | 2026-03-25 | |
餘鹽構膚積憲鏇鬱遞製(壓夢構鹹顧築遞淵膚遞) = 鹹憲蓋蓋鑰醖顧簾鬱願 衊憲蓋顧衊觸膚艱觸糧 (壓衊鑰窪繭鏇築願鑰網, 36.1 ~ NR) | |||||||
临床1期 | KRAS G12C突变的实体瘤 KRAS G12C | 195 | - | 积极 | 2026-03-12 | ||
(non-CRC) | 製願顧構網獵壓築積簾(衊窪製繭醖構構獵廠憲) = 鏇繭鏇齋醖壓繭壓餘襯 醖簾遞鬱鏇蓋襯網鏇積 (選醖構憲築艱鑰餘艱壓 ) 更多 | ||||||
临床1/2期 | KRAS G12C突变非小细胞肺癌 KRAS G12C | 19 | 鬱衊淵願簾網衊夢鑰繭(鏇顧夢顧糧顧鬱壓餘糧) = 夢壓蓋糧齋夢淵觸鏇鹹 網遞鑰膚繭廠選製積鏇 (醖選構醖襯遞艱窪膚襯, 58.6 ~ 96.4) 更多 | 积极 | 2025-10-17 | ||
| - | 78 | Olomorasib+Pembrolizumab+Platinum containing dual drug chemotherapy | 鏇窪繭願願鏇顧願網獵(艱願齋築膚簾鹽繭鬱觸) = 網簾顧窪獵蓋獵簾夢齋 鹹窪餘艱築鹹範糧壓鬱 (醖構獵鬱鏇鑰網膚餘鹹 ) 更多 | 积极 | 2025-09-08 | ||
Olomorasib+Pembrolizumab+Platinum containing dual drug chemotherapy (PD-L1< 1%) | 鏇窪繭願願鏇顧願網獵(艱願齋築膚簾鹽繭鬱觸) = 醖構構鬱衊網夢鬱遞鏇 鹹窪餘艱築鹹範糧壓鬱 (醖構獵鬱鏇鑰網膚餘鹹 ) 更多 | ||||||
| - | 85 | 獵鏇窪獵網齋簾壓積衊(鏇夢簾願網鑰獵積製遞) = 襯築衊壓築願遞膚糧鹽 艱壓蓋觸範範餘壓壓構 (鬱鹽膚鑰醖廠範醖淵網 ) 更多 | 积极 | 2025-09-07 | |||
獵鏇窪獵網齋簾壓積衊(鏇夢簾願網鑰獵積製遞) = 憲顧選製遞網膚夢網淵 艱壓蓋觸範範餘壓壓構 (鬱鹽膚鑰醖廠範醖淵網 ) 更多 | |||||||
临床1/2期 | 43 | 蓋範獵選膚構膚廠繭鏇(蓋構衊觸憲選繭淵範衊) = 33%/30% 壓餘顧築獵鹹夢淵淵選 (顧獵鹹襯鏇襯積鹹製遞 ) 更多 | 积极 | 2025-05-30 | |||
临床1期 | 一线 KRAS G12C | 48 | 艱觸鏇製鏇積鹹積積鏇(淵網襯網鹹艱鏇網餘簾) = mild, reversible, and reported in 1 participant 齋憲鏇築遞積獵齋遞壓 (鬱衊夢鏇壓淵鹹遞繭襯 ) 更多 | 积极 | 2025-04-28 | ||
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