预约演示
更新于：2025-04-30
Apatinib Mesylate
甲磺酸阿帕替尼
更新于：2025-04-30
概要
基本信息
在研机构 |
最高研发阶段批准上市 |
最高研发阶段(中国)批准上市 |
特殊审评孤儿药 (美国)、孤儿药 (欧盟)、优先审评 (中国)、特殊审批 (中国)、孤儿药 (韩国)、国家科技重大专项 (中国)、突破性疗法 (中国) |
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结构/序列
分子式C25H27N5O4S |
InChIKeyFYJROXRIVQPKRY-UHFFFAOYSA-N |
CAS号1218779-75-9 |
关联
862
项与 甲磺酸阿帕替尼 相关的临床试验NCT06881017
Establishment of Precision Targeted Therapy Strategies for Advanced Gastric Cancer Based on Novel Molecular Subtyping: an Umbrella Phase II Exploratory Clinical Study
ChiCTR2500099852
Adebrelimab combined with apatinib and chemotherapy in NSCLC treated with first-line PD-1 inhibitor therapy:a prospective, single-center, single-arm clinical study
NCT06913777
An Open-Label, Multicenter, Randomized Controlled Phase III Clinical Study of Neoadjuvant Chemotherapy Based on SNF Classification With or Without Precision Medicine Agents for Early-Stage or Locally Advanced HR+/HER2- Breast Cancer
100 项与 甲磺酸阿帕替尼 相关的临床结果
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100 项与 甲磺酸阿帕替尼 相关的转化医学
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100 项与 甲磺酸阿帕替尼 相关的专利（医药）
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2,778
项与 甲磺酸阿帕替尼 相关的文献（医药）2025-12-01Journal of Gastrointestinal Cancer
Third- or Further-Line Treatment in Patients with MSS Type Metastatic Colorectal Cancer
Article
作者: Gou, Miaomiao ; Qian, Niansong ; Dai, Guanghai ; Zhang, Yong ; Wang, Zhikuan
BACKGROUND:
The survival benefit from later-line treatment for patients with metastatic colorectal cancer (mCRC) remains disappointing. Here, in a real-world study, we were aimed to evaluate which choice will affect the survival of mCRC patients after standard treatment in Chinese patients.
METHODS:
A total of 129 patients with refractory mCRC were involved in the study. They received targeted monotherapy or combined with chemo-agents or PD-1 inhibitor before death. Overall survival (OS) and progression-free survival (PFS) were reviewed and evaluated from clinical features and treatment options.
RESULTS:
Among the 129 patients, the median age was 56 years (25-81). The mOS from third-line was 12.5 months. OS of patients who treated with chemo plus targeted therapy group in third-line was shown to be superior to pd-1 inhibitor in combination with antiangiogenic agents or antiangiogenic monotherapy group (15.6 m vs. 10.5 m vs. 8.4 m, p < 0.05). Patients had received triplet-drugs (bevacizumab plus low-dose irinotecan and oxaliplatin) and had prolonged survival compared to those had not (21.3 m vs 10.3 m, p = 0.004). OS between patients who had immunotherapy history or not was not significantly different (p > 0.05). The mPFS was 3.5 months in patients who had administered with antiangiogenic targeted agents plus anti-pd-1 and 4.7 months in chemo plus targeted therapy group and 2.2 months in the other group. In the triplet drugs group, preliminary results showed that ORR was 13.3% and DCR was 80%. The median PFS was 5.1 m, and the median OS was 10.6 m.
CONCLUSIONS:
Triplet drugs resulted in significantly longer overall survival, and immunotherapy may have limited benefit in MSS type CRC patients.
2025-07-01CRITICAL REVIEWS IN ONCOLOGY HEMATOLOGY
Targeting TIME in advanced hepatocellular carcinoma: Mechanisms of drug resistance and treatment strategies
Review
作者: Li, Fangfang ; Fang, Xizhu ; Ye, Xinyi ; Jin, Dan
Hepatocellular carcinoma (HCC) is the predominant form of primary liver cancer. While early-stage HCC can be effectively managed with surgical resection and other interventions, treatment options for advanced HCC are limited. Current systemic treatments for advanced HCC include VEGF-targeted tyrosine kinase inhibitors (Sorafenib, Lenvatinib), and the combination therapy of anti PD-1/PD-L1 and anti VEGF (Atezolizumab plus Bevacizumab, Camrelizumab plus Rivoceranib). However, the lack of response to these drugs and the emergence of acquired drug resistance significantly impairs their efficacy. Numerous studies have demonstrated that the tumor immune microenvironment (TIME) plays a crucial role in modulating the response to these therapies. Various immune cells and their secreted factors within the TIME play a pivotal role in the emergence of secondary drug resistance in HCC. This article reviews the mechanism of TIME promoting drug resistance, discusses the influence of current systemic HCC treatment drugs on TIME, and evaluates how these TIME changes affect the efficacy of treatment. A deeper understanding of the interaction between TIME and systemic treatment drugs may be beneficial to enhance the treatment effect, mitigate drug resistance of advanced HCC, and ultimately improve the prognosis of patients.
2025-07-01CELLULAR SIGNALLING
Apatinib combined with paclitaxel suppresses synergistically TNBC progression through enhancing ferroptosis susceptibility regulated SLC7A11/GPX4/ACSL4 axis
Article
作者: Cao, Di ; Wang, Jing ; Hu, Zhiqiang ; Ma, Xiaoxia ; Ding, Xiaoyun ; Zhang, Yan
Triple-negative breast cancer (TNBC) is highly heterogeneous, often leading to resistance to chemotherapy agents like paclitaxel (PTX) and resulting in suboptimal outcomes. The anti-angiogenic agent apatinib not only enhances chemotherapy sensitivity but also involves in regulating ferroptosis. However, the potential of combining apatinib with PTX to improve treatment efficacy in refractory TNBC by increasing tumor cell susceptibility to ferroptosis remains elusive. This study aims to elucidate whether inducing ferroptosis participates in the beneficial effects of apatinib combined with PTX to synergistically suppress TNBC. Herein, we demonstrated that the coadministration of apatinib and PTX exerted significant inhibitory effects on both primary tumor progression and distant metastases to pulmonary and hepatic tissues in TNBC-bearing murine models. Transcriptomic and proteomic analyses indicated that ferroptosis induction is a key mechanism by which the drug combination suppresses TNBC, as evidenced by a marked downregulation of SLC7A11, GPX4, NRF2, and FTH1, and a significant upregulation of ACSL4. In vitro, the combination of 5 μM apatinib and 8 nM PTX synergistically inhibited tumor cell proliferation, migration, and invasion. Notably, the combination therapy markedly augmented ferroptosis in tumor cells through the regulation of the SLC7A11/GPX4/ACSL4 axis, leading to increased intracellular iron accumulation and lipid peroxide generation, concomitant with a reduction in GSH levels. The effect of apatinib combined with PTX on enhancing ferroptosis susceptibility could be exploited as a combination treatment regimen for future TNBC therapy.
694
项与 甲磺酸阿帕替尼 相关的新闻（医药）2025-04-29
·恒瑞医药
ASCO会议抗体药物偶联物临床结果申请上市临床1期
2025-04-28
·药研网
ASCO会议抗体药物偶联物临床结果临床1期临床3期
2025-04-26
财报上市批准医药出海
100 项与 甲磺酸阿帕替尼 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 |
|---|---|---|---|
| gBRCA突变/HER2阴性乳腺癌 | 中国 | 2024-12-01 | |
| 肝细胞癌 | 中国 | 2021-01-07 | |
| 胃食管交界处腺癌 | 中国 | 2014-10-17 | |
| 胃腺癌 | 中国 | 2014-10-17 |
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 |
|---|---|---|---|---|
| 转移性肝细胞癌 | 申请上市 | 美国 | 2024-10-21 | |
| 不可切除的肝细胞癌 | 申请上市 | 美国 | 2023-05-17 | |
| 胃癌 | 申请上市 | 中国 | 2011-08-09 | |
| 晚期胃食管交界处腺癌 | 临床3期 | 中国 | 2020-09-21 | |
| 晚期非小细胞肺癌 | 临床3期 | 中国 | 2020-09-16 | |
| 晚期三阴性乳腺癌 | 临床3期 | 中国 | 2020-07-06 | |
| 乳腺癌 | 临床3期 | 中国 | 2020-07-03 | |
| 转移性乳腺癌 | 临床3期 | 中国 | 2020-07-03 | |
| PD-L1阳性非小细胞肺癌 | 临床3期 | - | 2020-06-15 | |
| 卵巢癌 | 临床3期 | 中国 | 2020-05-12 |
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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 | 72 | Rivoceranib 700 mg | 壓鏇壓廠積願襯餘鬱餘(簾鏇範壓醖鑰繭鹽觸網) = 廠網構築顧糧簾蓋鬱構 齋鹹獵齋觸夢簾鏇鑰簾 (淵鹹製廠鹽壓鑰築糧觸, 7.9 ~ 25.7) 更多 | 积极 | 2025-04-28 | ||
临床2期 | 36 | 範鹽淵獵蓋鹹構餘鬱製(廠醖積築積網願鏇築築) = 壓鏇網夢艱鬱餘憲糧繭 齋觸餘鏇蓋觸膚醖構鬱 (獵鑰淵鏇簾繭衊廠蓋築, 49.0 ~ 81.4) 达到 更多 | 积极 | 2025-04-18 | |||
临床2期 | 转移性肝细胞癌 二线 | - | Apatinib + HAIC | 鑰築艱醖窪觸餘糧淵廠(醖鹽獵構鹹鬱鏇夢夢選) = 構蓋鑰襯獵簾顧憲窪糧 選獵醖醖鑰鬱齋繭淵積 (糧鹹襯願鏇醖繭選網襯 ) 更多 | 积极 | 2025-03-03 | |
临床1期 | 广泛期小细胞肺癌 一线 | 40 | 2 cycles of etoposide and carboplatin (EC) as induction treatment followed by 2-4 cycles of camrelizumab, apatinib plus EC, then maintenance camrelizumab plus apatinib. | 齋衊範膚鑰觸糧鹹願鏇(餘蓋觸鏇鹽廠顧窪鹹壓) = 積壓積觸鬱鏇鑰淵鬱憲 鹹繭顧夢鹹製積繭獵鏇 (製膚淵構網鑰膚獵築淵, 73.9 ~ 96.9) 更多 | 积极 | 2025-02-18 | |
ASCO_GU2025 人工标引  | 临床2期 | 23 | 餘餘範網網廠廠鏇夢願(範淵鹽簾範衊窪餘蓋獵) = 顧齋顧積淵糧餘製鑰齋 艱簾鏇憲構鑰顧淵簾獵 (衊鏇膚廠鹹顧網襯膚齋, 10 ~ 42) 更多 | 不佳 | 2025-02-13 | ||
临床2期 | 34 | 糧窪艱製觸鏇築遞憲製(鏇製壓構顧衊鏇簾廠餘) = 壓膚齋鬱窪鹹衊艱範夢 襯顧糧遞觸觸淵選淵網 (艱襯衊鏇壓簾齋糧選鏇, 53.0 ~ 85.3) 更多 | 积极 | 2025-02-07 | |||
临床2期 | 200 | 鏇蓋窪醖製鏇襯窪積築(願網鹹網夢壓餘憲夢鹹) = 鏇醖艱築夢遞積網簾網 鏇憲齋壓膚壓鏇積鹹獵 (鹽鑰構淵簾構蓋糧製構, 8.8 ~ 13.8) 更多 | 积极 | 2025-01-23 | |||
TACE | 鏇蓋窪醖製鏇襯窪積築(願網鹹網夢壓餘憲夢鹹) = 鏇齋齋構蓋遞襯醖繭積 鏇憲齋壓膚壓鏇積鹹獵 (鹽鑰構淵簾構蓋糧製構, 2.0 ~ 4.1) 更多 | ||||||
ESMO_IO2024 人工标引 | N/A | 33 | Regorafenib+PD-1 inhibitor | 鏇壓襯鏇鏇窪積遞鏇淵(鏇築膚艱膚夢遞鏇範鹽) = 衊艱願繭糧艱網蓋簾遞 夢醖範遞觸憲簾餘鏇淵 (鹽簾範繭夢醖廠顧遞遞 ) 更多 | 积极 | 2024-12-12 | |
Apatinib+PD-1 inhibitor | 鏇壓襯鏇鏇窪積遞鏇淵(鏇築膚艱膚夢遞鏇範鹽) = 製襯糧壓觸積鑰築簾窪 夢醖範遞觸憲簾餘鏇淵 (鹽簾範繭夢醖廠顧遞遞 ) 更多 | ||||||
临床2期 | 35 | 願醖廠鹹顧製壓顧繭壓(築鏇遞鹹蓋選憲網廠積) = 鏇艱餘衊鏇選壓選蓋願 壓範醖網簾糧選鑰淵醖 (構憲餘餘願築夢膚鑰餘 ) 更多 | 积极 | 2024-12-07 | |||
(PVTT-Vp0) | 願醖廠鹹顧製壓顧繭壓(築鏇遞鹹蓋選憲網廠積) = 鹹鏇窪獵夢獵蓋構膚簾 壓範醖網簾糧選鑰淵醖 (構憲餘餘願築夢膚鑰餘 ) 更多 | ||||||
临床3期 | 243 | DEB-TACE + Apatinib | 醖鏇網廠構鏇廠鑰遞夢(淵願顧鬱艱觸憲網鏇憲) = 淵選顧鹽齋醖簾繭壓鬱 鑰選遞淵襯積齋積網製 (壓獵衊鬱壓廠鬱選顧鬱, 6.6 ~ 8.3) 更多 | 积极 | 2024-11-13 | ||
DEB-TACE | 醖鏇網廠構鏇廠鑰遞夢(淵願顧鬱艱觸憲網鏇憲) = 遞餘網餘憲壓顧獵積糧 鑰選遞淵襯積齋積網製 (壓獵衊鬱壓廠鬱選顧鬱, 5.0 ~ 5.9) 更多 |
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