预约演示
更新于：2026-04-03
Opnurasib
更新于：2026-04-03
概要
基本信息
原研机构 |
非在研机构- |
权益机构- |
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1/2期 |
特殊审评- |
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结构/序列
分子式C29H28ClN7O |
InChIKeyAZUYLZMQTIKGSC-UHFFFAOYSA-N |
CAS号2653994-08-0 |
关联
9
项与 Opnurasib 相关的临床试验NCT07468071
KontRASt-R: An Open-label, Multi-center, Rollover Study for Participants Who Have Been Previously Enrolled Into a Novartis-sponsored Opnurasib (JDQ443) Study and Are Continuing to Benefit From Opnurasib as a Single Agent or in Combination With Other Study Treatments
NCT05999357
A Phase II Study evaluaTing intRacranial effIcacy of JDQ443 in patiEnts With KRAS G12C+ NSCLC and bRain Metastases
NCT05714891
Neoadjuvant Platform Trial in Patients With Surgically Resectable Non-Small Cell Lung Cancer (NSCLC)
100 项与 Opnurasib 相关的临床结果
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100 项与 Opnurasib 相关的转化医学
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100 项与 Opnurasib 相关的专利（医药）
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11
项与 Opnurasib 相关的文献（医药）2025-08-13EXPERT OPINION ON PHARMACOTHERAPY
Profiling opnurasib (JDQ-443) for the treatment of non-small cell lung cancer (NSCLC)
Review
作者: Bazhenova, Lyudmila ; Hilburn, Van ; Herrmann, Amanda ; Azenkot, Tali
INTRODUCTION:
Oncogenic activation of KRAS is a common driver of solid tumor malignancies and has been considered 'undruggable' for several decades. Oral small molecule inhibitors, including sotorasib and adagrasib, have demonstrated moderate efficacy in targeting KRAS G12C in NSCLC. More potent inhibitors are needed, and the landscape is rapidly evolving.
AREAS COVERED:
Opnurasib (JDQ-443) is an irreversible covalent inhibitor of GDP-bound KRAS G12C that has been under investigation in patients with KRAS G12C-mutated solid tumors, including NSCLC. Here, we review its mechanism of action, pharmacologic properties, clinical efficacy, role within the NSCLC landscape prior to its withdrawal from the market, as well as the regulatory and market-driven dynamics that may result in the abandonment of aspiring drugs.
EXPERT OPINION:
JDQ-443's unique binding within the Switch II pocket of KRAS G12C allows for novel interactions and helps define its characteristic profile of anti-tumor activity, tolerability, and resistance. JDQ-443 has demonstrated promising early clinical activity in KRAS G12C-mutated NSCLC. More data is necessary to allow comparison of available agents and combination strategies. In the face of an expanding market, development of JDQ-443 has been halted despite promising safety and efficacy outcomes and ongoing innovative trials, highlighting critical challenges in the drug development process. The existing body of work characterizing JDQ-443 remains extremely informative.
2025-03-01Clinical Lung Cancer
A Phase II Study of Neoadjuvant Opnurasib KRAS G12C Inhibitor in Patients With Surgically Resectable Non-Small Cell Lung Cancer (CCTG IND.242A): A Substudy of the IND.242 Platform Master Protocol
Article
作者: Jensen, K. ; Shieh, B. ; Labbe, C. ; Owen, S. ; Spicer, J ; Tsao, M-S ; Blais, N ; Chu, Q. ; Kidane, B ; Labbe, C ; Spicer, J. ; Tsao, M.-S. ; Juergens, R. ; Cottrell, T.R. ; Cottrell, T R ; Sederias, J ; Blais, N. ; Robinson, A.G. ; Owen, S ; Bradbury, P A ; Shieh, B ; Tu, W ; Jensen, K ; Farago, A F ; Gaudreau, P-O ; Juergens, R ; Sederias, J. ; Farago, A.F. ; Tu, W. ; Kidane, B. ; Bradbury, P.A. ; Robinson, A G ; Brown-Walker, P ; Chu, Q ; Brown-Walker, P. ; Laurie, S ; Gaudreau, P.-O. ; Laurie, S.
Molecularly targeted agents are increasingly being studied in the treatment of early-stage non-small cell lung cancer (NSCLC) to try and improve cure. However, phase 3 data on neoadjuvant therapy have largely been conducted in a biomarker agnostic manner with inconsistent exclusion of EGFR and ALK alterations. Our objective was to develop IND.242 as a large-scale neoadjuvant platform trial to introduce novel agents into the preoperative window for molecularly-defined NSCLC patient populations. Given that KRAS G12C mutations are common in the overall NSCLC patient population, ranging from 9.4% to 13% of cases across different cohorts, and may be associated to worse prognosis, the initial IND.242A Substudy was designed to test neoadjuvant JDQ443 (opnurasib), a selective KRAS G12C inhibitor. This current trial report describes the multicenter, Canadian Cancer Trials Group (CCTG)-led IND.242 neoadjuvant phase 2 platform master protocol and its first Substudy (IND.242A) of neoadjuvant opnurasib KRAS G12C inhibitor for patients with surgically resectable NSCLC (AJCC 8th edition stage IA2 to IIIA). In IND.242A, a maximum of 27 patients will be accrued in participating Canadian sites. The primary objective is the rate of major pathological response (MPR) following neoadjuvant opnurasib. Secondary objectives include safety and tolerability of the treatment regimen, objective response rate (ORR) by RECIST 1.1 for the neoadjuvant treatment period, pathological complete response (pCR) rate, event-free survival (EFS) at 2 years, and surgical outcomes. Exploratory objectives are to explore patient related outcomes (PROs) and identify potential predictive biomarkers of response and mechanisms of resistance on tissue and peripheral blood samples.
2024-10-01CELL
Targeting Ras-, Rho-, and Rab-family GTPases via a conserved cryptic pocket
Article
作者: Guiley, Keelan Z. ; Jenkins, Meredith L. ; Lin, Zhi ; Huang, Benjamin J ; Shokat, Kevan M. ; Peacock, D Matthew ; Zhu, Lawrence ; Stephen, Andrew G ; Burke, John E ; Peacock, D. Matthew ; Evans, John T. ; Bowcut, Victoria ; Morstein, Johannes ; Yang, Yue ; Lightstone, Felice C. ; Taran, Katrine A. ; Evans, John T ; Fernando, Micah ; Taran, Katrine A ; Krahnke, Sophie ; Stephen, Andrew G. ; Jenkins, Meredith L ; Shokat, Kevan M ; Huang, Benjamin J. ; Burke, John E. ; Lightstone, Felice C ; Guiley, Keelan Z
The family of Ras-like GTPases consists of over 150 different members, regulated by an even larger number of guanine exchange factors (GEFs) and GTPase-activating proteins (GAPs) that comprise cellular switch networks that govern cell motility, growth, polarity, protein trafficking, and gene expression. Efforts to develop selective small molecule probes and drugs for these proteins have been hampered by the high affinity of guanosine triphosphate (GTP) and lack of allosteric regulatory sites. This paradigm was recently challenged by the discovery of a cryptic allosteric pocket in the switch II region of K-Ras. Here, we ask whether similar pockets are present in GTPases beyond K-Ras. We systematically surveyed members of the Ras, Rho, and Rab family of GTPases and found that many GTPases exhibit targetable switch II pockets. Notable differences in the composition and conservation of key residues offer potential for the development of optimized inhibitors for many members of this previously undruggable family.
100 项与 Opnurasib 相关的药物交易
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外链
| KEGG | Wiki | ATC | Drug Bank |
|---|---|---|---|
| - | Opnurasib | - | - |
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突变非小细胞肺癌 | 临床3期 | 美国 | 2022-06-15 | |
| KRAS G12C突变非小细胞肺癌 | 临床3期 | 中国 | 2022-06-15 | |
| KRAS G12C突变非小细胞肺癌 | 临床3期 | 阿根廷 | 2022-06-15 | |
| KRAS G12C突变非小细胞肺癌 | 临床3期 | 阿根廷 | 2022-06-15 | |
| KRAS G12C突变非小细胞肺癌 | 临床3期 | 澳大利亚 | 2022-06-15 | |
| KRAS G12C突变非小细胞肺癌 | 临床3期 | 巴西 | 2022-06-15 | |
| KRAS G12C突变非小细胞肺癌 | 临床3期 | 保加利亚 | 2022-06-15 | |
| KRAS G12C突变非小细胞肺癌 | 临床3期 | 保加利亚 | 2022-06-15 | |
| KRAS G12C突变非小细胞肺癌 | 临床3期 | 加拿大 | 2022-06-15 | |
| KRAS G12C突变非小细胞肺癌 | 临床3期 | 智利 | 2022-06-15 |
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临床结果
临床结果
适应症
分期
评价
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临床2期 | 95 | (Cohort A- PD-L1<1%) | 鏇艱膚憲簾選廠膚願築 = 襯窪築蓋願獵艱鹹築糧 齋鑰鹽築壓積艱蓋願鹹 (簾蓋艱繭膚窪蓋鑰觸憲, 艱膚餘餘蓋鹹範積憲獵 ~ 選鹽齋窪願積築窪觸鹽) 更多 | - | 2025-10-09 | ||
(Cohort B- PD-L1≥ 1% and STK11 Mutation) | 願製繭齋選鹹醖製構蓋 = 廠網築廠餘衊淵範襯遞 觸鏇醖獵廠窪繭醖製觸 (築繭繭願遞糧遞構獵遞, 壓簾餘鑰衊鬱顧廠廠範 ~ 製淵網醖夢築膚獵齋積) 更多 | ||||||
临床2期 | KRAS G12C突变的实体瘤 KRAS G12C | 50 | 築繭壓顧構鏇構願壓蓋(糧蓋構顧鹹築壓網窪糧) = 窪積範鏇餘願壓鹹構鑰 選鏇襯糧壓憲襯衊窪壓 (衊構衊淵鬱糧遞鹹壓窪 ) 更多 | 积极 | 2023-09-10 | ||
築鹽艱鹹製繭簾夢醖選(鏇積獵蓋壓艱窪醖構網) = 繭簾網願獵製衊鹹襯遞 窪製衊艱餘糧艱蓋築觸 (襯鑰網衊艱餘壓選齋淵 ) 更多 | |||||||
临床1/2期 | KRAS突变肿瘤 KRAS G12C | 38 | 鏇築膚餘齋範淵餘鬱構(壓醖壓鑰廠製製鏇艱夢) = Among pts treated at 200 mg BID,4 (7.1%). 願糧淵衊顧廠夢鏇鑰淵 (憲鹹衊鹽範衊壓鑰選鬱 ) 更多 | 积极 | 2023-05-26 | ||
临床1/2期 | KRAS G12C突变的实体瘤 KRAS G12C Mutation | 39 | 糧鏇鏇選繭築遞壓蓋淵(範顧簾廠遞鏇獵範製壓) = 衊範積壓襯範網獵簾範 夢築築艱積獵艱選廠廠 (遞顧壓壓艱壓淵憲鹽築 ) 更多 | 积极 | 2022-06-15 |
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