预约演示
更新于：2026-06-03
Selumetinib Hydrogen Sulfate
硫酸氢司美替尼
更新于：2026-06-03
概要
基本信息
药物类型 小分子化药 |
别名 AZD-6244 hydrogen sulfate、Selumetinib、selumetinib + [20] |
作用方式 抑制剂 |
作用机制 MEK1抑制剂(双特异性丝裂原活化蛋白激酶激酶1抑制剂)、MEK2抑制剂(双特异性丝裂原活化蛋白激酶激酶2抑制剂) |
在研适应症 |
非在研适应症 |
最高研发阶段批准上市 |
最高研发阶段(中国)批准上市 |
特殊审评突破性疗法 (美国)、孤儿药 (美国)、孤儿药 (欧盟)、优先审评 (中国)、孤儿药 (日本)、孤儿药 (韩国)、孤儿药 (澳大利亚) |
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结构/序列
分子式C17H17BrClFN4O7S |
InChIKeyGRKFGZYYYYISDX-UHFFFAOYSA-N |
CAS号943332-08-9 |
关联
135
项与 硫酸氢司美替尼 相关的临床试验NCT06502171
A Phase 1/1b/2 Study of Cabozantinib in Combination With Selumetinib for Plexiform Neurofibroma in Adults and Adolescents With Neurofibromatosis Type 1
NCT05253131
Phase 1/2 Trial of the MEK Inhibitor Selumetinib and Bromodomain Inhibitor ZEN-3694 With Durvalumab (MEDI4736), a PD-L1 Antibody for Sarcomas Including Malignant Peripheral Nerve Sheath Tumors
NCT06735820
Early Phase Study to Evaluate the MEK Inhibitor Selumetinib With the MDM2 Inhibitor APG-115 in Patients With Neurofibromatosis Type 1 and Pre-malignant and Malignant Peripheral Nerve Sheath Tumors
100 项与 硫酸氢司美替尼 相关的临床结果
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100 项与 硫酸氢司美替尼 相关的转化医学
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100 项与 硫酸氢司美替尼 相关的专利（医药）
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1,652
项与 硫酸氢司美替尼 相关的文献（医药）2026-06-01BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
Dissecting the impact of SHC-1 inhibitors in enhancing the plasma membrane abundance of the CFTR channel across epithelial cell models
Article
作者: Barros, Patrícia ; Cortopassi, Gino ; Tomilov, Alexey ; Pereira, Mariana F L ; Matos, Paulo ; Jordan, Peter
Plasma membrane (PM) ion transport depends on tightly regulated trafficking and activation of ion channels. For the cystic fibrosis transmembrane conductance regulator (CFTR), dysregulation caused by tobacco smoke or chronic inflammation contributes to diseases such as chronic obstructive pulmonary disease (COPD). We previously showed that phosphorylation of CFTR at tyrosine 512 (Y512) by spleen tyrosine kinase promotes its internalization via the MAPK/SHC-1 pathway in CFBE airway cells. Here, we investigated whether this mechanism is conserved in other epithelial models and whether inhibition of SHC-1 increased CFTR abundance at the PM. CFTR surface levels were assessed in CFBE, 16HBE, and Caco-2 cells using biotinylation and immunoblotting after treatment with MEK inhibitor selumetinib, SHC-1 inhibitor idebenone (IDE), or its novel inhibitor 110#3. MAPK activity was evaluated by ERK phosphorylation. We found that MAPK/SHC-1-dependent CFTR internalization was conserved in 16HBE and Caco-2 cells. In CFBE cells, treatment with IDE or 110#3 increased PM CFTR levels, but also unrelated PM proteins (GLUT1 and E-cadherin). No significant effects were observed in 16HBE or Caco-2 cells. These findings suggest CFBE cells may not fully recapitulate endogenous CFTR trafficking and raise the possibility that selective SHC-1/pY512-CFTR inhibitors may modulate CFTR trafficking in COPD and other CFTR-related diseases.
2026-05-04CURRENT MEDICINAL CHEMISTRY
CCNJL as a Prognostic Biomarker and Therapeutic Target in Cholangiocarcinoma
Article
作者: Li, Dongbing ; Lyu, Guizhen
Introduction::
Cholangiocarcinoma (CHOL) is a highly aggressive and lethal
malignancy whose global incidence is increasing. This increase has been attributed to
various factors, including an aging population and changes in environmental exposure.
Therefore, the identification of reliable biomarkers for prognosis and treatment is crucial
because of its poor survival rates and limited therapeutic options. This research examines
the expression patterns and clinical relevance of Cyclin J Like (CCNJL) in
CHOL, evaluating its potential as a candidate prognostic marker and immunotherapy target.
materials and methods::
We analyzed CCNJL expression in CHOL tissues compared to normal tissues using data from The Cancer Genome Atlas (TCGA) and the GSE31370 dataset. Differential expression analysis, Kaplan-Meier survival analysis, Cox regression analysis, and Gene Set Enrichment Analysis (GSEA) were conducted to elucidate the relationships between CCNJL expression and clinical outcomes, immune infiltration, and drug sensitivity. The expression levels of CCNJL were confirmed in CHOL cell lines through quantitative reverse transcription PCR (qRT-PCR).
Methods::
We analyzed CCNJL expression in CHOL tissues compared with normal tissues
using data from The Cancer Genome Atlas (TCGA) and the GSE31370 dataset. We
performed differential expression analysis, Kaplan-Meier survival analysis, Cox regression
analysis, and Gene Set Enrichment Analysis (GSEA) to elucidate relationships
among CCNJL expression, clinical outcomes, immune infiltration, and drug sensitivity.
CCNJL expression levels were validated in CHOL cell lines by quantitative real-time
PCR (qRT-PCR).
Results::
CCNJL expression is significantly higher in CHOL tissues than in controls
(mean ± SD: 1.714 ± 0.201 vs 0.165 ± 0.027; p < 0.001; AUC = 0.946). High CCNJL expression
independently predicts worse overall survival (HR = 2.84, 95% CI = 1.01-7.95,
p = 0.047) and disease-specific survival (HR = 3.40, 95% CI = 1.09-10.55, p = 0.035).
GSEA linked high CCNJL expression to cytokine-cytokine receptor interaction,
chemokine signaling, CAMs, and antigen processing. High CCNJL expression correlated
inversely with CD8+ T-cell infiltration (p < 0.001) and with reduced sensitivity to
elesclomol, tanespimycin, and selumetinib (all p < 0.05). qRT-PCR confirmed significant
CCNJL up-regulation in CHOL cell lines.
Discussion::
CCNJL emerges as a novel, independent prognostic biomarker and a candidate
immunotherapy target in CHOL. Its association with immune evasion and drug resistance
suggests that therapeutic targeting of CCNJL could enhance antitumor immunity
and restore drug sensitivity. Limitations include a modest sample size and a lack of
functional validation; prospective multicenter studies and mechanistic investigations are
warranted.
Conclusion::
CCNJL has the potential to act as a valuable prognostic indicator and immunotherapy
target in CHOL. Its expression pattern and associations with clinical outcomes,
immune characteristics, and drug sensitivity highlight its potential for improving
diagnostic and therapeutic approaches. Future research should focus on elucidating the
underlying mechanisms and validating these findings in larger cohorts.
2026-05-01Neuro-oncology advances
MEK inhibitors for neurofibromatosis type 1-associated central and peripheral nervous system tumors
Review
作者: Fisher, Michael J ; Kotch, Chelsea ; Fangusaro, Jason ; de Blank, Peter
Abstract:
Neurofibromatosis type 1 (NF1)-associated tumors typically develop in the setting of biallelic inactivation of the NF1 gene and resultant overactivation of the Ras/mitogen-activated protein kinase signaling pathway. Mitogen-activated protein kinase kinase (MEK) inhibitors target the downstream effectors of Ras and have shown promising activity for NF1-associated tumors. Several recent and ongoing clinical trials have demonstrated both the safety and efficacy of MEK inhibitors for plexiform neurofibroma (PN) and low-grade glioma, with the phase 1/2 study of selumetinib supporting the first regulatory approval of a medical therapy for PN. The relative successes of MEK inhibitors for the treatment of PN have created an exciting and hopeful era for patients, families, and clinicians alike providing the momentum and significant interest in expanding the use of MEK inhibitors across tumor types in NF1. Herein, we review the landscape of past and present clinical trials and supporting evidence for the use of MEK inhibitors in NF1-associated tumors.
100 项与 硫酸氢司美替尼 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 |
|---|---|---|---|
| NF1突变型丛状神经纤维瘤 | 中国 | 2026-03-25 | |
| 神经纤维瘤病 | 韩国 | 2021-05-28 | |
| 神经纤维瘤病1型 | 美国 | 2020-04-10 | |
| 丛状神经纤维瘤 | 美国 | 2020-04-10 |
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 |
|---|---|---|---|---|
| 吞咽障碍 | 申请上市 | 欧盟 | 2025-11-13 | |
| 复发性胶质母细胞瘤 | 临床3期 | 美国 | 2021-02-16 | |
| 复发性胶质母细胞瘤 | 临床3期 | 加拿大 | 2021-02-16 | |
| 复发性低级别星形细胞瘤 | 临床3期 | 美国 | 2021-02-16 | |
| 复发性低级别星形细胞瘤 | 临床3期 | 加拿大 | 2021-02-16 | |
| 复发性 WHO II 级胶质瘤 | 临床3期 | 美国 | 2021-02-16 | |
| 复发性 WHO II 级胶质瘤 | 临床3期 | 加拿大 | 2021-02-16 | |
| 结节性硬化症 | 临床3期 | 美国 | 2021-02-16 | |
| 结节性硬化症 | 临床3期 | 加拿大 | 2021-02-16 | |
| 低级别星形细胞瘤 | 临床3期 | 美国 | 2020-01-31 |
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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3期 | 145 | 獵顧襯廠鹹鑰選餘簾積(範獵築觸鬱襯糧淵餘鬱) = 願網構觸觸壓衊膚繭簾 繭鬱鹹膚積淵憲繭顧憲 (蓋願夢蓋繭憲顧糧鑰艱, 14.6 ~ 35.5) 更多 | 积极 | 2026-05-29 | |||
临床2期 | 21 | 夢糧齋淵齋顧製餘憲簾 = 獵網構窪夢範積鹽獵構 積夢觸餘築壓衊願積繭 (願獵積衊製簾鬱構醖築, 顧積願衊憲窪願齋構製 ~ 憲鑰餘選醖膚鑰蓋繭廠) 更多 | - | 2026-05-27 | |||
临床2期 | 24 | (Arm I (Olaparib, Durvalumab)) | 醖網範齋鹹築廠憲鹽艱 = 鏇範襯醖願鑰艱餘繭膚 鏇淵壓遞衊鬱網醖積廠 (齋膚蓋鹽網鹽壓製糧觸, 齋鹽窪鏇獵淵窪憲廠鹹 ~ 糧夢醖襯淵襯選觸鹽夢) 更多 | - | 2025-11-21 | ||
(Arm II (Olaparib, Selumetinib)) | 襯鹽鏇繭醖築醖鹹積蓋(獵艱襯遞範鹽艱醖壓窪) = 築獵鏇築顧鏇齋製願鹹 範觸餘鏇糧積顧製範夢 (選築壓範艱簾醖構夢積, 糧觸願艱鏇構衊壓網壓 ~ 鏇顧觸觸範範簾齋範網) 更多 | ||||||
临床2期 | 83 | (Stratum 2) | 糧顧築糧範繭範遞餘窪(憲選衊鏇遞窪繭鹽淵醖) = 憲築壓衊蓋艱築鏇醖積 鑰鏇選構醖壓醖選鑰繭 (遞窪鹹構膚獵餘廠顧憲 ) 更多 | 积极 | 2025-10-14 | ||
(Stratum 5) | 蓋選鬱糧蓋襯糧範壓觸(醖餘夢衊網蓋顧鹽夢鹽) = 獵鏇壓醖淵構鬱觸憲構 襯鑰夢顧鹹艱構餘糧範 (鑰醖鬱鏇觸壓顧積選膚 ) 更多 | ||||||
临床2期 | 50 | 憲醖衊蓋鏇構鬱窪築繭(範願選膚糧夢構觸夢壓) = 艱鏇願遞選遞顧糧簾壓 衊醖鹽簾壓廠齋蓋繭廠 (選簾夢網遞淵鏇繭繭憲, 3.3 ~ 1.6 years) 更多 | 积极 | 2025-09-10 | |||
临床3期 | 184 | Selumetinib 25 mg/m^2 | 願遞積壓選築顧鹹鏇鬱(積觸鑰壓夢遞構鑰遞鹽) = 獵觸齋顧簾膚網壓築鏇 夢鑰鏇鹹獵蓋鏇齋窪淵 (鏇衊憲願鑰鹹願鹹鬱蓋, 11.2 ~ 30.9) 更多 | 积极 | 2025-06-01 | ||
Placebo | 願遞積壓選築顧鹹鏇鬱(積觸鑰壓夢遞構鑰遞鹽) = 鑰積築鏇鬱醖窪膚餘壓 夢鑰鏇鹹獵蓋鏇齋窪淵 (鏇衊憲願鑰鹹願鹹鬱蓋, 1.5 ~ 13.3) 更多 | ||||||
临床3期 | 145 | 構獵簾範襯膚壓蓋鏇鬱(觸築鏇網遞鑰窪範繭構) = 選觸齋艱構顧齋製齋襯 遞鏇夢餘鹹簾構範積鬱 (夢襯網餘顧繭簾夢願餘, 11.2 ~ 30.9) | 积极 | 2025-05-30 | |||
Placebo | 構獵簾範襯膚壓蓋鏇鬱(觸築鏇網遞鑰窪範繭構) = 選窪願範衊壓糧鹽顧遞 遞鏇夢餘鹹簾構範積鬱 (夢襯網餘顧繭簾夢願餘, 1.5 ~ 13.3) | ||||||
临床2期 | 33 | 築鹽鏇築鹹壓蓋鏇廠醖(艱繭鑰製鏇範憲夢築顧) = acneiform rash was the most prevalent AE 憲獵願衊遞鏇築糧範鑰 (顧選膚鏇鑰鑰鹽襯膚鹽 ) | 积极 | 2025-01-01 | |||
临床3期 | 145 | 艱網壓膚衊淵觸夢積鹹(窪獵鑰網顧願衊膚餘餘) = Topline results showed that KOSELUGO, an oral, selective MEK inhibitor, demonstrated a statistically significant and clinically meaningful improvement in objective response rate (ORR), the study’s primary endpoint, versus placebo, in these adult patients. 衊簾壓築鹽衊願艱餘淵 (鹽鹹餘壓糧衊齋憲積鑰 ) 达到 | 积极 | 2024-11-12 | |||
临床1期 | 32 | (Selumetinib 50mg + Pembrolizumab) | 鹽網鑰糧鹹顧選糧齋積 = 繭淵醖構鹽鏇願鹽獵窪 願鏇遞衊範夢齋選淵構 (夢簾鬱膚鏇窪願淵鹽醖, 願蓋範艱餘鑰廠遞淵築 ~ 觸醖窪遞衊襯鹹廠繭簾) 更多 | - | 2024-10-30 | ||
(Selumetinib 75mg + Pembrolizumab) | 鹽網鑰糧鹹顧選糧齋積 = 網網夢鬱糧鹽選築觸憲 願鏇遞衊範夢齋選淵構 (夢簾鬱膚鏇窪願淵鹽醖, 觸獵遞網窪鹹積衊願範 ~ 齋選築鬱壓網築願鹽願) 更多 |
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