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更新于：2025-09-10
RMC-4630
更新于：2025-09-10
概要
基本信息
非在研机构 |
最高研发阶段临床2期 |
首次获批日期- |
最高研发阶段(中国)- |
特殊审评- |
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结构/序列
分子式C20H27ClN6O2S |
InChIKeyHISJAYUQVHMWTA-BLLLJJGKSA-N |
CAS号2172652-48-9 |
关联
7
项与 RMC-4630 相关的临床试验NCT04916236
Phase I/Ib Study With the Combination of RMC-4630 (SHP2 Inhibitor) and LY3214996 (ERK Inhibitor) in Metastatic KRAS Mutant CRC, PDAC and NSCLC
NL-OMON52379
Phase I/Ib study with the combination of RMC-4630 and LY3214996 in metastatic KRAS mutant CRC, PDAC and NSCLC - The SHERPA-trial - Phase I/Ib study with the combination of RMC-4630 and LY3214996
NCT05054725
A Phase 2, Open-Label, Multicenter Study of the Combination of RMC-4630 and Sotorasib for Non-Small Cell Lung Cancer Subjects With KRASG12C Mutation After Failure of Prior Standard Therapies
100 项与 RMC-4630 相关的临床结果
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100 项与 RMC-4630 相关的转化医学
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100 项与 RMC-4630 相关的专利（医药）
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2
项与 RMC-4630 相关的文献（医药）2025-06-01SLAS Discovery
Combinatorial screen with apoptosis pathway targeted agents alrizomadlin, pelcitoclax, and dasminapant in multi-cell type tumor spheroids
Article
作者: Coussens, Nathan P ; Doroshow, James H ; Silvers, Thomas ; Takebe, Naoko ; Sanchez, Phillip R ; Dexheimer, Thomas S ; Hollingshead, Melinda G ; Teicher, Beverly A ; Chen, Li
Apoptosis, or programmed cell death, plays a critical role in maintaining tissue homeostasis by eliminating damaged or abnormal cells. Dysregulation of apoptosis pathways is a hallmark of cancer, allowing malignant cells to evade cell death and proliferate uncontrollably. Targeting apoptosis pathways has emerged as a promising therapeutic strategy in cancer treatment, aiming to restore the balance between cell survival and death. The MDM2 inhibitor alrizomadlin, the Bcl-2/Bcl-xL inhibitor pelcitoclax, and the IAP family inhibitor dasminapant were evaluated both individually and in combinations with standard of care and investigational anticancer small molecules in a spheroid model of solid tumors. The multi-cell type tumor spheroids were grown from human endothelial cells and mesenchymal stem cells combined with human malignant cells that were either established or patient-derived cell lines from the NCI Patient-Derived Models Repository. The malignant cell lines were derived from a range of solid tumors including uterine carcinosarcoma, synovial sarcoma, rhabdomyosarcoma, soft tissue sarcoma, malignant fibrous histiocytoma, malignant peripheral nerve sheath tumor (MPNST), pancreas, ovary, colon, breast, and small cell lung cancer. Interactions were observed from combinations of the apoptosis pathway targeted agents. Additionally, interactions were observed from combinations of the apoptosis pathway targeted agents with other agents, including PARP inhibitors, the XPO1 inhibitor eltanexor, and the PI3K inhibitor copanlisib. Enhanced activity was also observed from combinations of the apoptosis pathway targeted agents with MAPK pathway targeted agents, including the MEK inhibitor cobimetinib as well as adagrasib and MRTX1133, which specifically target the KRAS G12C and G12D variants, respectively.
2021-06-24The New England journal of medicine1区 · 医学
Sotorasib for Lung Cancers with
KRAS
p.G12C Mutation
1区 · 医学
Article
作者: Ramalingam, Suresh S ; Henary, Haby ; Tran, Qui ; Ngarmchamnanrith, Gataree ; Velcheti, Vamsidhar ; Skoulidis, Ferdinandos ; Borghaei, Hossein ; Kato, Terufumi ; Li, Bob T ; Besse, Benjamin ; Ang, Agnes ; Mather, Omar ; Falchook, Gerald S ; Sacher, Adrian ; Schuler, Martin ; Curioni-Fontecedro, Alessandra ; Price, Timothy J ; Italiano, Antoine ; Takahashi, Toshiaki ; Dy, Grace K ; Anderson, Abraham ; Govindan, Ramaswamy ; Friberg, Gregory ; Barlesi, Fabrice ; Spira, Alexander ; Wolf, Jürgen
BACKGROUND:
Sotorasib showed anticancer activity in patients with KRAS p.G12C-mutated advanced solid tumors in a phase 1 study, and particularly promising anticancer activity was observed in a subgroup of patients with non-small-cell lung cancer (NSCLC).
METHODS:
In a single-group, phase 2 trial, we investigated the activity of sotorasib, administered orally at a dose of 960 mg once daily, in patients with KRAS p.G12C-mutated advanced NSCLC previously treated with standard therapies. The primary end point was objective response (complete or partial response) according to independent central review. Key secondary end points included duration of response, disease control (defined as complete response, partial response, or stable disease), progression-free survival, overall survival, and safety. Exploratory biomarkers were evaluated for their association with response to sotorasib therapy.
RESULTS:
Among the 126 enrolled patients, the majority (81.0%) had previously received both platinum-based chemotherapy and inhibitors of programmed death 1 (PD-1) or programmed death ligand 1 (PD-L1). According to central review, 124 patients had measurable disease at baseline and were evaluated for response. An objective response was observed in 46 patients (37.1%; 95% confidence interval [CI], 28.6 to 46.2), including in 4 (3.2%) who had a complete response and in 42 (33.9%) who had a partial response. The median duration of response was 11.1 months (95% CI, 6.9 to could not be evaluated). Disease control occurred in 100 patients (80.6%; 95% CI, 72.6 to 87.2). The median progression-free survival was 6.8 months (95% CI, 5.1 to 8.2), and the median overall survival was 12.5 months (95% CI, 10.0 to could not be evaluated). Treatment-related adverse events occurred in 88 of 126 patients (69.8%), including grade 3 events in 25 patients (19.8%) and a grade 4 event in 1 (0.8%). Responses were observed in subgroups defined according to PD-L1 expression, tumor mutational burden, and co-occurring mutations in STK11, KEAP1, or TP53.
CONCLUSIONS:
In this phase 2 trial, sotorasib therapy led to a durable clinical benefit without new safety signals in patients with previously treated KRAS p.G12C-mutated NSCLC. (Funded by Amgen and the National Institutes of Health; CodeBreaK100 ClinicalTrials.gov number, NCT03600883.).
100 项与 RMC-4630 相关的药物交易
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研发状态
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 非小细胞肺癌 | 临床2期 | 美国 | 2021-12-30 | |
| 非小细胞肺癌 | 临床2期 | 澳大利亚 | 2021-12-30 | |
| 非小细胞肺癌 | 临床2期 | 加拿大 | 2021-12-30 | |
| 非小细胞肺癌 | 临床2期 | 法国 | 2021-12-30 | |
| 非小细胞肺癌 | 临床2期 | 德国 | 2021-12-30 | |
| 非小细胞肺癌 | 临床2期 | 意大利 | 2021-12-30 | |
| 非小细胞肺癌 | 临床2期 | 西班牙 | 2021-12-30 | |
| 非小细胞肺癌 | 临床2期 | 中国台湾 | 2021-12-30 | |
| 非小细胞肺癌 | 临床2期 | 英国 | 2021-12-30 | |
| 转移性肿瘤 | 临床2期 | 美国 | 2020-06-09 |
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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1/2期 | 65 | (Part 1- SAR442720 200mg BIW + Pembrolizumab) | 襯鹹憲醖積顧衊築艱鬱 = 壓遞夢齋廠蓋夢夢製憲 獵淵糧憲選窪憲廠構築 (蓋簾網簾鹽網艱壓範窪, 積衊齋網鹹鹽憲衊夢選 ~ 醖選鹹窪夢糧廠獵蓋蓋) 更多 | - | 2025-04-20 | ||
(Part 3A- SAR442720 100mg BIW + Adagrasib) | 簾獵夢築願範夢積淵觸 = 積衊廠糧構憲鬱艱艱築 網餘繭鑰選膚襯夢顧製 (網繭鏇廠窪窪鏇憲艱鬱, 選醖齋製衊獵獵醖膚繭 ~ 遞醖壓鬱壓鹽憲觸獵鹽) 更多 | ||||||
临床1/2期 | 113 | (Intermittent RMC-4630 80mg (D1D4) + Cobimetinib 20mg QD (21/7)) | 鹹觸艱襯壓夢蓋鑰壓願 = 鹹夢襯鏇遞遞鑰鬱網選 膚壓選觸糧簾餘觸構積 (蓋獵鑰鹽鑰鏇範淵壓築, 繭憲夢艱艱願壓鑰願鹹 ~ 積壓積構醖淵餘網構膚) 更多 | - | 2023-06-26 | ||
(Intermittent RMC-4630 80mg (D1D4) + Cobimetinib 40mg QD (21/7)) | 鹹觸艱襯壓夢蓋鑰壓願 = 襯繭窪鬱廠積蓋廠齋衊 膚壓選觸糧簾餘觸構積 (蓋獵鑰鹽鑰鏇範淵壓築, 築窪淵範範鹹襯鹽壓鬱 ~ 廠壓觸觸齋觸築壓醖繭) 更多 | ||||||
临床1期 | 实体瘤 KRAS Mutation | 104 | overall | 鬱選顧觸窪醖鑰積膚網(糧鏇顧網顧襯憲憲醖構) = 200 mg D1D2, delivering a 400 mg weekly dose intensity 選顧壓構鬱壓鹽獵積構 (蓋製糧壓憲鬱膚夢築鬱 ) 更多 | 积极 | 2021-04-10 | |
(KRAS MUT NSCLC) |
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