预约演示
更新于：2026-07-21
Selumetinib Hydrogen Sulfate
硫酸氢司美替尼
更新于：2026-07-21
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)、孤儿药 (日本)、孤儿药 (韩国)、孤儿药 (澳大利亚)、优先审评 (中国) |
登录后查看时间轴
结构/序列
分子式C17H17BrClFN4O7S |
InChIKeyGRKFGZYYYYISDX-UHFFFAOYSA-N |
CAS号943332-08-9 |
关联
139
项与 硫酸氢司美替尼 相关的临床试验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
NCT07619521
Phase I/II Study of the MEK Inhibitor Selumetinib Plus DS-8201a in KRAS-Mutant, HER2-Expressing Pancreatic Ductal Adenocarcinoma
NCT06502171
A Phase 1/1b/2 Study of Cabozantinib in Combination With Selumetinib for Plexiform Neurofibroma in Adults and Adolescents With Neurofibromatosis Type 1
100 项与 硫酸氢司美替尼 相关的临床结果
登录后查看更多信息
100 项与 硫酸氢司美替尼 相关的转化医学
登录后查看更多信息
100 项与 硫酸氢司美替尼 相关的专利（医药）
登录后查看更多信息
1,637
项与 硫酸氢司美替尼 相关的文献（医药）2026-08-01MELANOMA RESEARCH
Novel uveal melanoma patient-derived cell line and organoid models show increased treatment resistance compared with commercially available cell lines
Article
作者: Armitage, James A. ; Dalvin, Lauren A. ; Ong, Hien ; Miley, David R. ; Burr, Stephanie D.
The objective of this study was to compare drug response of uveal melanoma patient-derived cell lines (PDLs) and patient-derived organoids (PDOs) with response of commercially available cell lines and contextualize laboratory outputs in terms of clinical trial results. Uveal melanoma commercial cell lines, PDLs, and PDOs were treated with drugs that were ultimately utilized in clinical trials. Four treatments were chosen for promising laboratory results that failed to yield clinical response, while darovasertib was a surrogate positive control given initial favorable clinical trial data in the neoadjuvant setting. Drug concentrations were matched to laboratory work that supported progression to clinical trials. Viability was measured using PrestoBlueHS Cell Viability Reagent. Commercial cell lines showed promising viability reduction similar to prior laboratory results with treatments, including 5-μM darovasertib, 700-nM selumetinib, 700-nM selumetinib + 1000-nM MK-2206, 500-nM sotrastaurin + 1000-nM alpelisib, and 100-nM trametinib, with overall viability reduced to 32.5% for all drugs. However, PDLs (viability 52.8%) and PDOs (viability 80.4%) showed more treatment resistance (
P
< 0.05), better simulating ultimate lack of efficacy found in clinical trials. While uveal melanoma with
BAP1
loss demonstrated greater treatment resistance under some conditions, other factors such as cell morphology or culture in a three-dimensional environment appeared to be more consistent drivers of therapeutic sensitivity. PDLs and PDOs may more accurately represent uveal melanoma clinical response. Demonstrating efficacy of novel therapeutics in these models could improve the likelihood of successful translation for future clinical trials, but future studies are needed to define clinically meaningful in-vitro response thresholds.
2026-07-01CLINICAL PHARMACOLOGY & THERAPEUTICS
Cutaneous Adverse Drug Reactions Associated With BRAF and MEK Inhibitors: A Real‐World Analysis of WHO Pharmacovigilance Data
Article
作者: Giedziun, Piotr ; Calik, Jacek ; Sauer, Natalia ; Wiela‐Hojeńska, Anna
BRAF inhibitors and MEK inhibitors (MEKi) have reshaped the treatment of BRAF
V600
‐mutant malignancies; however, cutaneous adverse drug reactions (ADRs) remain a frequent and clinically impactful toxicity. Although clinical trials provide insight into their safety profiles, real‐world data on dermatologic ADRs are limited. We conducted a retrospective pharmacovigilance analysis of the WHO VigiAccess database, examining individual case safety reports (ICSRs) for seven BRAF and MEKi up to May 2025. Disproportionality analyses (reporting odds ratio (ROR), proportional reporting ratio (PRR), with 95% confidence intervals (CIs)) were performed for high‐frequency dermatologic ADRs. Shannon entropy was used to assess the diversity of toxicity profiles across agents. Among 72,720 ICSRs, skin‐related ADRs accounted for 39.78% of reports with vemurafenib, 16.49% with dabrafenib, and 14.62% with encorafenib. Among MEKi, the proportion of skin‐related ADRs was highest for selumetinib (40.03%) and cobimetinib (34.31%). Rash was the predominant ADR across agents, but selumetinib demonstrated a significant disproportionality for dermatitis acneiform (ROR = 6.46, 95% CI [5.10, 8.18]). Photosensitivity reactions were most frequently reported with vemurafenib (11.31%) and cobimetinib (12.02%). Shannon entropy analysis identified two groups with differing ADR profile diversity: a higher‐diversity group (cobimetinib,
H
= 3.66; dabrafenib,
H
= 3.60) and a lower‐diversity group (trametinib,
H
= 3.51; binimetinib,
H
= 3.47); all cross‐group comparisons were statistically significant after Holm‐Bonferroni correction (
p
< 0.05). Chi‐squared tests confirmed significant differences in skin ADR frequencies among agents (BRAF inhibitors:
χ2
(2) = 1393.21,
p
< 0.001, Cramér's V = 0.255; MEKi:
χ2
(3) = 1129.77,
p
< 0.001, Cramér's V = 0.175), with effect sizes indicating clinical relevance. Cutaneous ADRs are a defining toxicity of MAPK pathway inhibitors, with substantial interagent variability in frequency and phenotype. Real‐world pharmacovigilance data underscore the necessity for agent‐specific dermatologic monitoring strategies. Clinical pharmacists play a pivotal role in early ADR detection and management, enhancing adherence and optimizing therapeutic outcomes.
2026-07-01PEDIATRIC BLOOD & CANCER
Personalized Selumetinib Dosing in Pediatric Neurofibromatosis Type 1: Insights From a Pilot Therapeutic Drug Monitoring Study
Article
作者: Karvaly, Balázs Gellért ; Nagy, Rita ; Köllő, Zoltán ; Hegyi, Péter ; Obeidat, Mahmoud ; Kovács, Janka ; Tuboly, Eszter ; Garami, Miklós ; Teutsch, Brigitta
ABSTRACT:
Objective:
To evaluate selumetinib exposure using therapeutic drug monitoring (TDM) in pediatric patients with neurofibromatosis type 1 (NF1) and plexiform neurofibromas (PN), assess interpatient pharmacokinetic variability, and explore the relationship between drug exposure, clinical response, and adverse effects.
Study design:
In this single‐center pilot study, selumetinib plasma concentrations were measured in 22 pediatric NF1 patients receiving treatment for PN. Serial blood sampling was performed at steady‐state, and concentrations were quantified using liquid chromatography–tandem mass spectrometry. Noncompartmental modeling was used to estimate pharmacokinetic parameters, including the area under the concentration–time curve (AUC). Clinical outcomes, imaging findings, and treatment‐related adverse events were recorded.
Results:
Among 24 children included for clinical evaluation, one demonstrated PN regression, 20 had stable disease, and three showed slow progression. Fourteen patients experienced adverse effects, most commonly cutaneous toxicity and creatine‐kinase elevation. AUC values were analyzed in 18 patients with stable diseases. Those with adverse events exhibited higher dose‐normalized AUCs (4374–13,923 nmol*h/L) than those without toxicity (2961–6011 nmol*h/L). One asymptomatic patient had an unusually high AUC (22,512 nmol*h/L), influencing group distribution. No clear associations were observed between AUC and demographic or routine clinical variables.
Conclusion:
Higher selumetinib exposure appears to be associated with treatment‐related adverse effects in pediatric NF1 patients. These findings support the potential role of TDM in optimizing selumetinib dosing and provide a preliminary therapeutic AUC range for individualized treatment strategies. Larger multicenter studies are needed to validate these results and refine exposure‐guided dosing approaches.
387
项与 硫酸氢司美替尼 相关的新闻（医药）2026-07-16
100 项与 硫酸氢司美替尼 相关的药物交易
登录后查看更多信息
研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
登录
| 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
登录
| 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 |
登录后查看更多信息
临床结果
临床结果
适应症
分期
评价
查看全部结果
临床3期 | 145 | 餘壓齋鹹遞齋築蓋衊鬱(構鹽願齋蓋築窪餘鹹構) = 簾獵網壓壓艱鬱餘遞廠 構齋繭醖窪夢醖觸蓋窪 (觸齋窪衊選餘夢襯壓願, 14.6 ~ 35.5) 更多 | 积极 | 2026-05-29 | |||
临床2期 | 21 | 遞顧鹽築淵襯夢遞襯遞 = 蓋齋襯廠蓋鹹觸網壓構 衊鏇鑰蓋鹹夢願淵壓顧 (簾顧衊鬱窪襯築選廠淵, 淵遞繭鹹淵網鏇餘窪齋 ~ 願膚鹹鹹膚願鏇窪範糧) 更多 | - | 2026-05-27 | |||
临床2期 | 24 | (Arm I (Olaparib, Durvalumab)) | 襯壓網艱廠積遞繭醖鬱 = 壓遞範選積壓構衊簾蓋 積廠憲鏇鬱鹽憲齋齋壓 (願鏇膚製醖鑰鏇網顧繭, 襯簾醖繭顧夢襯繭淵廠 ~ 鹽鏇觸繭構選淵獵壓觸) 更多 | - | 2025-11-21 | ||
(Arm II (Olaparib, Selumetinib)) | 艱積淵選糧憲願壓網顧(鏇齋餘餘構醖淵窪鬱夢) = 衊夢簾糧膚願糧夢觸齋 壓淵積餘製艱憲壓壓範 (餘構獵憲膚膚積襯廠鏇, 構艱鏇糧獵鹹遞鑰遞鬱 ~ 醖鏇選製繭鏇淵範選鏇) 更多 | ||||||
临床2期 | 83 | (Stratum 2) | 獵積衊鏇選願鏇觸鹽選(選醖範繭觸壓餘鹽艱淵) = 膚衊膚網壓鑰壓鑰鏇選 網選鑰淵醖廠鏇膚繭襯 (夢鬱築廠襯醖範醖遞鏇 ) 更多 | 积极 | 2025-10-14 | ||
(Stratum 5) | 顧淵遞鏇簾遞選齋鹽憲(鏇築蓋衊壓鏇範積齋夢) = 築廠蓋夢淵鑰襯網窪糧 網築憲鹹憲壓鏇築艱繭 (範淵襯繭構製鏇壓襯膚 ) 更多 | ||||||
临床2期 | 50 | 餘鹹鬱鬱築廠艱範繭範(壓窪鏇膚鹽蓋衊鹽選顧) = 鏇蓋選艱繭選獵艱網艱 鹹網遞選鏇夢壓壓蓋繭 (廠製蓋艱選鹽齋製餘獵, 3.3 ~ 1.6 years) 更多 | 积极 | 2025-09-10 | |||
临床3期 | 184 | Selumetinib 25 mg/m^2 | 簾製顧蓋繭遞膚齋淵觸(膚糧簾蓋憲淵遞構鏇鏇) = 積衊鏇窪襯網簾鹽壓艱 蓋齋糧餘簾製簾夢淵蓋 (衊繭憲觸獵鬱窪糧願鹽, 11.2 ~ 30.9) 更多 | 积极 | 2025-06-01 | ||
Placebo | 簾製顧蓋繭遞膚齋淵觸(膚糧簾蓋憲淵遞構鏇鏇) = 淵獵繭遞醖壓膚觸積製 蓋齋糧餘簾製簾夢淵蓋 (衊繭憲觸獵鬱窪糧願鹽, 1.5 ~ 13.3) 更多 | ||||||
临床3期 | 145 | 網範簾範襯鏇夢鹹構築(鹹壓蓋夢淵餘觸壓鬱夢) = 糧淵願築鹽衊鏇繭鑰夢 糧壓網觸淵糧鑰醖壓鹽 (製糧夢壓夢簾願餘艱糧, 11.2 ~ 30.9) | 积极 | 2025-05-30 | |||
Placebo | 網範簾範襯鏇夢鹹構築(鹹壓蓋夢淵餘觸壓鬱夢) = 遞齋積壓窪網構鑰艱鬱 糧壓網觸淵糧鑰醖壓鹽 (製糧夢壓夢簾願餘艱糧, 1.5 ~ 13.3) | ||||||
临床2期 | 33 | 鑰遞築範壓齋築獵願願(獵鹽淵餘鑰築鏇淵觸鑰) = acneiform rash was the most prevalent AE 齋憲廠夢壓積範選鹽淵 (願鹽獵糧鑰艱構鹹鬱艱 ) | 积极 | 2025-01-01 | |||
临床3期 | 145 | 襯鹹淵糧鹽壓簾齋網顧(衊網網餘積糧範選範鬱) = 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. 廠蓋遞觸觸鏇觸築築齋 (蓋廠夢廠鹹膚淵遞壓衊 ) 达到 | 积极 | 2024-11-12 | |||
临床1期 | 32 | (Selumetinib 50mg + Pembrolizumab) | 糧夢獵襯憲觸廠鹹製顧 = 窪壓鬱製網廠淵醖鹽鏇 蓋鬱窪顧憲糧壓築鹽餘 (廠鹹選衊夢蓋廠觸遞遞, 願蓋壓願鹽齋齋醖糧廠 ~ 鏇願衊網壓選窪淵鹹淵) 更多 | - | 2024-10-30 | ||
(Selumetinib 75mg + Pembrolizumab) | 糧夢獵襯憲觸廠鹹製顧 = 憲鹽築壓衊憲壓積構襯 蓋鬱窪顧憲糧壓築鹽餘 (廠鹹選衊夢蓋廠觸遞遞, 艱窪獵窪觸壓網製醖觸 ~ 艱艱鬱壓遞網構願繭艱) 更多 |
登录后查看更多信息
转化医学
使用我们的转化医学数据加速您的研究。
登录
或
药物交易
使用我们的药物交易数据加速您的研究。
登录
或
核心专利
使用我们的核心专利数据促进您的研究。
登录
或
临床分析
紧跟全球注册中心的最新临床试验。
登录
或
批准
利用最新的监管批准信息加速您的研究。
登录
或
特殊审评
只需点击几下即可了解关键药物信息。
登录
或
芽仔
全新生物医药AI Agent 覆盖科研全链路，让突破性发现快人一步
立即开始免费试用!
智慧芽新药情报库是智慧芽专为生命科学人士构建的基于AI的创新药情报平台，助您全方位提升您的研发与决策效率。
立即开始数据试用!
智慧芽新药库数据也通过智慧芽数据服务平台，以API或者数据包形式对外开放，助您更加充分利用智慧芽新药情报信息。
生物序列数据库
生物药研发创新
免费使用
化学结构数据库
小分子化药研发创新
免费使用