更新于：2024-07-01
Capmatinib Hydrochloride
盐酸卡马替尼
更新于：2024-07-01
概要
基本信息
原研机构 |
最高研发阶段批准上市 |
首次获批日期 美国 (2020-05-06), |
最高研发阶段(中国)批准上市 |
特殊审评突破性疗法 (美国)、加速批准 (美国)、孤儿药 (美国)、孤儿药 (澳大利亚) |
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结构
分子式C23H21Cl2FN6O2 |
InChIKeyCOWBUPJEEDYWKD-UHFFFAOYSA-N |
CAS号1865733-40-9 |
关联
74
项与 盐酸卡马替尼 相关的临床试验A Phase II, Two Parallel Group Study of Neoadjuvant and Adjuvant Targeted Treatment in NSCLC With BRAF V600 or MET Exon 14 Mutations
主研究方案：一项在晚期不可切除肺癌（LC）受试者中评价多种基于Amivantamab的联合治疗的安全性和疗效的I/II期、开放性、平台研究 子研究方案（特定附录1）：一项评价Amivantamab联合Capmatinib治疗不可切除的转移性非小细胞肺癌的安全性和疗效的I/II期研究
A Phase 2 Open-label Study to Determine the Central Nervous System Efficacy of Capmatinib in NSCLC Patients With Brain Metastases With cfDNA Positive MET Alterations
100 项与 盐酸卡马替尼 相关的临床结果
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100 项与 盐酸卡马替尼 相关的转化医学
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100 项与 盐酸卡马替尼 相关的专利（医药）
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185
项与 盐酸卡马替尼 相关的文献（医药）2024-04-01International journal of radiation oncology, biology, physics
MET Inhibitor Capmatinib Radiosensitizes MET Exon 14-Mutated and MET-Amplified Non-Small Cell Lung Cancer
Article
作者: Ramesh, Shrey ; Cifci, Ahmet ; Minne, Rachel L ; Baschnagel, Andrew M ; Nickel, Kwangok P ; Kimple, Randall J ; Longhurst, Colin A ; Javeri, Saahil
PURPOSE:
The objective of this study was to investigate the effects of inhibiting the MET receptor with capmatinib, a potent and clinically relevant ATP-competitive tyrosine kinase inhibitor, in combination with radiation in MET exon 14-mutated and MET-amplified non-small cell lung (NSCLC) cancer models.
METHODS AND MATERIALS:
In vitro effects of capmatinib and radiation on cell proliferation, colony formation, MET signaling, apoptosis, and DNA damage repair were evaluated. In vivo tumor responses were assessed in cell line xenograft and patient-derived xenograft models. Immunohistochemistry was used to confirm the in vitro results.
RESULTS:
In vitro clonogenic survival assays demonstrated radiosensitization with capmatinib in both MET exon 14-mutated and MET-amplified NSCLC cell lines. No radiation-enhancing effect was observed in MET wild-type NSCLC and a human bronchial epithelial cell line. Minimal apoptosis was detected with the combination of capmatinib and radiation. Capmatinib plus radiation compared with radiation alone resulted in inhibition of DNA double-strand break repair, as measured by prolonged expression of γH2AX. In vivo, the combination of capmatinib and radiation significantly delayed tumor growth compared with vehicle control, capmatinib alone, or radiation alone. Immunohistochemistry indicated inhibition of phospho-MET and phospho-S6 and a decrease in Ki67 with inhibition of MET.
CONCLUSIONS:
Inhibition of MET with capmatinib enhances the effect of radiation in both MET exon 14-mutated and MET-amplified NSCLC models.
2024-03-01European journal of cancer (Oxford, England : 1990)
First-line immunotherapy for lung cancer with MET exon 14 skipping and the relevance of TP53 mutations
Article
作者: Allgäuer, Michael ; Tufman, Amanda ; Stenzinger, Albrecht ; Dintner, Sebastian ; Grohé, Christian ; Kopp, Hans-Georg ; Hilbrandt, Moritz ; Falkenstern-Ge, Roger-Fei ; Lüders, Heike ; Kauffmann-Guerrero, Diego ; Kirchner, Martina ; Frost, Nikolaj ; Christopoulos, Petros ; Kuon, Jonas ; Thomas, Michael ; Hackanson, Björn ; Reck, Martin ; Misch, Daniel ; Kazdal, Daniel ; Faehling, Martin ; Blasi, Miriam ; Volckmar, Anna-Lena
BACKGROUND:
The efficacy of checkpoint inhibitors for non-small cell lung cancer (NSCLC) with MET exon 14 skipping (METΔ14ex) remains controversial.
MATERIALS AND METHODS:
110 consecutive METΔ14ex NSCLC patients receiving first-line chemotherapy (CHT) and/or immunotherapy (IO) in 10 German centers between 2016-2022 were analyzed.
RESULTS:
Combined CHT-IO was given to 35/110 (32%) patients, IO alone to 43/110 (39%), and CHT to 32/110 (29%) upfront. Compared to CHT, CHT-IO showed longer progression-free survival (median PFS 6 vs. 2.5 months, p = 0.004), more objective responses (ORR 49% vs. 28%, p = 0.086) and numerically longer overall survival (OS 16 vs. 10 months, p = 0.240). For IO monotherapy, OS (14 vs. 16 months) and duration of response (26 vs. 22 months) were comparable to those of CHT-IO. Primary progressive disease (PD) was more frequent with IO compared to CHT-IO (13/43 vs. 3/35, p = 0.018), particularly for never-smokers (p = 0.041). Higher PD-L1 TPS were not associated with better IO outcomes, but TP53 mutated tumors showed numerically improved ORR (56% vs. 32%, p = 0.088) and PFS (6 vs. 3 months, p = 0.160), as well as longer OS in multivariable analysis (HR=0.54, p = 0.034) compared to their wild-type counterparts. Any second-line treatment was administered to 35/75 (47%) patients, with longer survival for capmatinib or tepotinib compared to crizotinib (PFS 10 vs. 3 months, p = 0.013; OS 16 vs. 13 months, p = 0.270).
CONCLUSION:
CHT-IO is superior to CHT, and IO alone also effective for METΔ14ex NSCLC, especially in the presence of TP53 mutations and independent of PD-L1 expression, but never-smokers are at higher risk of primary PD.
2024-05-01Anti-cancer agents in medicinal chemistry
An Expedition on Synthetic Methodology of FDA-approved Anticancer Drugs
(2018-2021)
Review
作者: Gupta, Ghanshyam Das ; Jain, Ankit ; Vishakha, S ; Navneesh, N ; Verma, Sant Kumar ; Patel, Preeti ; Kurmi, Balak Das
Abstract::
New drugs being established in the market every year produce specified structures for selective biological
targeting. With medicinal insights into molecular recognition, these begot molecules open new rooms for
designing potential new drug molecules. In this review, we report the compilation and analysis of a total of 56
drugs including 33 organic small molecules (Mobocertinib, Infigratinib, Sotorasib, Trilaciclib, Umbralisib, Tepotinib,
Relugolix, Pralsetinib, Decitabine, Ripretinib, Selpercatinib, Capmatinib, Pemigatinib, Tucatinib, Selumetinib,
Tazemetostat, Avapritinib, Zanubrutinib, Entrectinib, Pexidartinib, Darolutamide, Selinexor, Alpelisib,
Erdafitinib, Gilteritinib, Larotrectinib, Glasdegib, Lorlatinib, Talazoparib, Dacomitinib, Duvelisib, Ivosidenib,
Apalutamide), 6 metal complexes (Edotreotide Gallium Ga-68, fluoroestradiol F-18, Cu 64 dotatate, Gallium 68
PSMA-11, Piflufolastat F-18, 177Lu (lutetium)), 16 macromolecules as monoclonal antibody conjugates (Brentuximabvedotin,
Amivantamab-vmjw, Loncastuximabtesirine, Dostarlimab, Margetuximab, Naxitamab, Belantamabmafodotin,
Tafasitamab, Inebilizumab, SacituzumabGovitecan, Isatuximab, Trastuzumab, Enfortumabvedotin,
Polatuzumab, Cemiplimab, Mogamulizumab) and 1 peptide enzyme (Erwiniachrysanthemi-derived
asparaginase) approved by the U.S. FDA between 2018 to 2021. These drugs act as anticancer agents against
various cancer types, especially non-small cell lung, lymphoma, breast, prostate, multiple myeloma, neuroendocrine
tumor, cervical, bladder, cholangiocarcinoma, myeloid leukemia, gastrointestinal, neuroblastoma, thyroid,
epithelioid and cutaneous squamous cell carcinoma. The review comprises the key structural features, approval
times, target selectivity, mechanisms of action, therapeutic indication, formulations, and possible synthetic approaches
of these approved drugs. These crucial details will benefit the scientific community for futuristic new
developments in this arena.
114
项与 盐酸卡马替尼 相关的新闻（医药）2024-06-25
·研发客
ASCO会议临床结果临床3期临床1期
2024-06-24
·信狐药迅
2024-06-20
·研发客
临床3期核酸药物siRNA寡核苷酸财报
100 项与 盐酸卡马替尼 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 |
|---|---|---|---|
| MET外显子14跳变的非小细胞肺癌 | 中国 | 2024-06-11 | |
| 转移性非小细胞肺癌 | 加拿大 | 2022-09-16 | |
| 晚期非小细胞肺癌 | 欧盟 | 2022-06-20 | |
| 晚期非小细胞肺癌 | 冰岛 | 2022-06-20 | |
| 晚期非小细胞肺癌 | 列支敦士登 | 2022-06-20 | |
| 晚期非小细胞肺癌 | 挪威 | 2022-06-20 | |
| c-Met阳性非小细胞肺癌 | 日本 | 2020-06-29 | |
| 非小细胞肺癌 | 美国 | 2020-05-06 | |
| 非小细胞肺癌 | 美国 | 2020-05-06 |
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 |
|---|---|---|---|---|
| EGFR突变的非小细胞肺癌 | 临床3期 | 美国 | 2021-09-22 | |
| EGFR突变的非小细胞肺癌 | 临床3期 | 美国 | 2021-09-22 | |
| EGFR突变的非小细胞肺癌 | 临床3期 | 美国 | 2021-09-22 | |
| EGFR突变的非小细胞肺癌 | 临床3期 | 日本 | 2021-09-22 | |
| EGFR突变的非小细胞肺癌 | 临床3期 | 日本 | 2021-09-22 | |
| EGFR突变的非小细胞肺癌 | 临床3期 | 日本 | 2021-09-22 | |
| EGFR突变的非小细胞肺癌 | 临床3期 | 波兰 | 2021-09-22 | |
| EGFR突变的非小细胞肺癌 | 临床3期 | 波兰 | 2021-09-22 | |
| EGFR突变的非小细胞肺癌 | 临床3期 | 波兰 | 2021-09-22 | |
| EGFR突变的非小细胞肺癌 | 临床3期 | 新加坡 | 2021-09-22 |
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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2期 | 76 | (Capmatinib 400mg BID + Pembrolizumab 200mg Q3W) | 願膚鹽獵鏇夢製獵製鬱(構願觸膚醖鬱繭窪顧鹹) = 顧顧憲築壓築醖齋繭蓋 製鹹製簾蓋鬱鑰夢鬱鹽 (繭簾淵鏇製鏇鑰衊鏇餘, 窪淵遞繭齋構窪願窪遞 ~ 壓夢憲餘遞膚顧範積醖) 更多 | - | 2024-02-08 | ||
(Pembrolizumab 200mg Q3W) | 願膚鹽獵鏇夢製獵製鬱(構願觸膚醖鬱繭窪顧鹹) = 願艱鏇窪廠膚簾艱網製 製鹹製簾蓋鬱鑰夢鬱鹽 (繭簾淵鏇製鏇鑰衊鏇餘, 衊顧襯窪鏇積齋窪簾網 ~ 鑰選衊鹹壓網簾遞淵壓) 更多 | ||||||
临床1/2期 | 肝细胞癌 二线 | - | 繭網襯鬱鹽醖範糧鑰鹽(鬱選獵艱顧築簾網窪鹹) = 顧觸構簾憲衊鬱鏇襯膚 糧鹽窪衊鹽構願餘築鑰 (獵齋餘鏇齋窪襯膚網鏇 ) | 不佳 | 2024-01-01 | ||
繭網襯鬱鹽醖範糧鑰鹽(鬱選獵艱顧築簾網窪鹹) = 觸夢範壓簾積衊憲願廠 糧鹽窪衊鹽構願餘築鑰 (獵齋餘鏇齋窪襯膚網鏇 ) | |||||||
临床3期 | 22 | 鏇觸範淵糧糧鬱淵鏇選(齋鏇鬱廠簾顧衊選蓋淵) = 鬱積鹹簾顧鑰遞選膚餘 齋糧遞壓糧簾蓋積憲積 (繭顧簾淵糧繭築齋鑰蓋 ) 更多 | 积极 | 2023-10-23 | |||
鏇觸範淵糧糧鬱淵鏇選(齋鏇鬱廠簾顧衊選蓋淵) = 鬱醖顧網觸醖構膚鑰繭 齋糧遞壓糧簾蓋積憲積 (繭顧簾淵糧繭築齋鑰蓋 ) 更多 | |||||||
N/A | 胶质母细胞瘤 MET amplification | - | 鬱顧網糧醖選築醖鏇選(鬱窪壓鏇顧鬱窪蓋鹽鬱) = 獵觸淵衊顧選壓鏇夢憲 製鏇構遞壓鏇糧顧夢築 (窪憲積繭獵鹹構膚餘遞 ) | 积极 | 2023-04-25 | ||
临床2期 | 373 | 顧衊觸築遞鬱餘襯積構(醖窪遞憲願獵齋窪積鑰) = 衊鹽鹹鏇選簾淵鏇艱鬱 艱鏇觸衊選壓醖鬱膚觸 (積衊醖築觸積膚觸繭遞, 9.7 ~ NE) 更多 | - | 2023-04-01 | |||
临床2期 | 20 | 觸窪顧壓廠鏇醖鏇糧憲(窪構壓簾繭鹹鹽簾夢壓) = 壓獵艱衊壓鑰淵襯簾鬱 繭齋廠廠襯網糧選鹽餘 (獵廠膚願遞鬱蓋糧齋淵, 顧窪構願夢築壓築構鬱 ~ 壓廠鹹鏇顧繭淵襯製壓) 更多 | - | 2023-03-21 | |||
临床2期 | 非小细胞肺癌 EGFR wild type | ALK rearrangement negative | MET exon 14 skipping mutation | 15 | 艱構願簾繭製壓淵願齋(簾簾製艱選膚遞網願築) = 遞壓鹹構製醖製壓獵範 願襯襯廠鬱選壓蓋鑰顧 (窪遞願淵糧獵艱觸衊鏇, 26.6 ~ 78.7) 更多 | 积极 | 2022-12-03 | ||
临床2期 | 31 | 糧夢範顧醖襯淵鏇遞鏇(廠廠網繭壓簾襯憲憲築) = 艱鏇簾鹹衊憲製鑰遞憲 製蓋遞獵餘鹽繭構積鑰 (夢糧簾廠積觸齋獵網鬱, 21.8 ~ 57.8) 更多 | 不佳 | 2022-09-10 | |||
N/A | 146 | 選壓夢醖齋顧淵簾鹽廠(選範廠餘鬱夢窪衊顧簾) = 憲齋艱憲願選襯築淵餘 鬱願窪糧鹹鹹繭壓簾襯 (鬱顧鹹鹹製鬱糧鬱鬱鬱, 4.2 ~ 6.0) 更多 | - | 2022-09-10 | |||
N/A | 一线 | 81 | 鑰構網範簾膚壓窪鹽衊(糧膚簾鹹簾齋衊艱淵鏇) = Grade ≥ 3 treatment-related adverse events included elevated creatinine (4%) 齋膚夢獵鹽顧鑰獵憲淵 (觸憲夢積衊願網顧範網 ) 更多 | - | 2022-08-06 |
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