预约演示
更新于：2025-08-12
Selumetinib sulfate
司美替尼
更新于：2025-08-12
概要
基本信息
药物类型 小分子化药 |
别名 AZD-6244 hydrogen sulfate、KOSELUGO、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) |
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 (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
133
项与 司美替尼 相关的临床试验NCT05253131
A Phase 1/2 Trial of the MEK Inhibitor Selumetinib and Bromodomain Inhibitor With Durvalumab (MEDI4736), a PD-L1 Antibody for Sarcomas Including Malignant Peripheral Nerve Sheath Tumors (NF112)
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
NCT06188741
Phase 2 Trial of Selumetinib for the Prevention of Plexiform Neurofibroma Growth and Morbidity in Neurofibromatosis Type 1
100 项与 司美替尼 相关的临床结果
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100 项与 司美替尼 相关的转化医学
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100 项与 司美替尼 相关的专利（医药）
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1,642
项与 司美替尼 相关的文献（医药）2025-12-01CHILDS NERVOUS SYSTEM
Severe cervical kyphosis in a complex child with NF1, case report and literature review
Review
作者: Piatelli, Gianluca ; Santoro, Claudia ; Pola, Enrico ; De Prisco, Ferruccio ; Miele, Giuseppina ; Perrotta, Silverio ; Nasto, Luigi Aurelio
Abstract:
Purpose:
We faced and herein report a detailed description of pre-operative assessment, management, and post-operative follow-up of a 2-year and 10-month-old girl with neurofibromatosis 1 (NF1) who presented with severe, dystrophic, cervical kyphosis (170 degrees) associated with extensive pre- and para-vertebral plexiform neurofibromas, who also went under MEK inhibitors therapy. Cervical kyphosis in NF1 is particularly rare, and there is no extensive literature available on the subject in terms of clinico-radiological features, surgical approach, and outcomes. We therefore also performed a comprehensive review of the available literature on the topic.
Methods:
The clinical report was made through the retrospective review of all medical documents and imaging of the patient. The systematic review was performed based on the inclusion and exclusion criteria set by the authors on surgical management of cervical kyphosis in NF1 patients according to the Preferred Reporting Items for Systematic Reviews and Meta-Analyses (PRISMA).
Results:
Our patient underwent a first-stage halo-gravity traction followed by a single-stage occipito-cervical posterior fusion. The six-week traction resulted in a reduction of the deformity from 170 to 90°. A further amelioration was obtained by surgery with a final 60% correction of the curvature (69° at last post-operative X-ray). No complications were observed at 1-and-a-half-year follow-up. The plexiform neurofibromas were treated with MEK inhibitors: trametinib for 1 year and 11 months until performing halo traction, and with selumetinib after surgery. We just found 19 papers suitable according to our selection criteria.
Conclusion:
Combined anterior and posterior fusion (CAP) is generally the best treatment option, although it is not always feasible. When plexiform, symptomatic, inoperable neurofibromas coexist, surgery can be preceded or followed by MEK inhibitor treatment for better control or a volumetric reduction of the tumors. The best therapeutic choice should always be the result of a multidisciplinary, expert approach and patient-tailored design.
2025-12-01CHILDS NERVOUS SYSTEM
The state of targeted therapeutic pharmacological approaches in pediatric neurosurgery: report from the European Society for Pediatric Neurosurgery (ESPN) Consensus Conference 2024
Review
作者: Due-Tønnessen, B J ; Leblond, P ; Thompson, D ; Obersnel, M ; Thomale, U W ; Di Rocco, F ; Knerlich-Lukoschus, F ; Romano, A ; Frassanito, P
Abstract:
Objective:
The development of novel targeted therapies is opening new perspectives in the treatment of pediatric brain tumors. Their precise role in therapeutic protocols still needs still to be defined. Thus, these novel pharmacological approaches in pediatric neurosurgery were the topic of the European Society for Pediatric Neurosurgery (ESPN) Consensus Conference held in Lyon (France) in January 25–27, 2024.
Method:
The paper reviews the current knowledge about targeted therapy as well as the current literature published on the topic. The conference aimed for an interdisciplinary consensus debate among pediatric oncologists and pediatric neurosurgeons on the following questions.Question 1: What is the current role for targeted therapies as neoadjuvant treatments before pediatric brain tumor removal?Question 2: What are the benefits, cost/efficiency, and long-term side effects of targeted therapies in the treatment of pediatric brain tumors?Question 3: Based on contemporary data, at which stage and in which pathologies do targeted therapies play a significant role?
Results:
Ninety-two participants answered consensus polls on the state of the art of targeted therapies, the ethical issues related to their use, and the evolving change in the role of pediatric neurosurgeons. The neoadjuvant role of targeted therapies is difficult to define as there are many different entities to consider. Despite the recently reported potential benefits, questions regarding the use of targeted therapies are manifold, in particular regarding sustainable benefits and long-term side effects. Additionally, challenging cost issues is a limiting factor for the broader availability of these drugs. Studies have demonstrated superiority of targeted therapy compared to chemotherapy both in randomized trials and compared to historical cohorts in the management of a subset of low-grade gliomas. The same drug combinations, BRAFi and MEKi, may be effective in HGG that have relapsed, progressed, or failed to respond to first-line therapy. Similar conclusions on efficacy may be drawn for mTORi in TSC and selumetinib in plexiform neurofibromas. For other tumors, the picture is still obscure due to the lack of data or even the lack of suitable targets. In conclusion, targeted treatment may not always be the best option even when a target has been identified. Safe surgery remains to be a favorable option in the majority of cases.
Conclusion:
The constantly evolving drug technology and the absence of long-term safety and efficacy studies made it difficult to reach a consensus on the predefined questions. However, a report of the conference is summarizing the present debate and it might serve as a guideline for future perspectives and ongoing research.
2025-09-01PHYTOMEDICINE
Motherwort synergized with oxytocin for postpartum hemorrhage prevention: Integrated clinical efficacy and mechanism exploration
Article
作者: Ren, Yan ; Chen, Chen ; Sun, Xin ; Luo, Qiumei ; Tan, Jing ; Wang, Wenling ; Liu, Chunrong ; Lu, Yongmei ; Xiong, Yiquan ; Liu, Qingsong
BACKGROUND:
Postpartum hemorrhage (PPH) remains a leading cause of maternal mortality, while Chinese Motherwort (Leonurus japonicus Houtt.), known as "JingChanLiangYao", has been used to prevent PPH in traditional Chinese obstetric and gynecological practices for thousands of years. As a modern purified Chinese herbal preparation, motherwort injection is frequently administered alongside the international first-line treatment of oxytocin in clinical practice. However, the clinical efficacy and mechanism of this combined regimen in PPH prevention have not yet been fully elucidated.
PURPOSE:
To evaluate the clinical efficacy of motherwort injection in combination with oxytocin for enhanced PPH prevention and elucidate its underlying mechanisms.
STUDY DESIGN:
This study employed an integrative approach using real-world data, meta-analysis and animal validation.
METHODS:
This study utilized an electronic health record database from the largest referral center for high-risk pregnancies in southwest China to explore uterotonic treatment patterns in cesarean sections, with therapeutic efficacy validated though meta-analysis. Active compounds of motherwort injection were characterized using UPLC-HRMS. A PPH rat model was established using mifepristone and misoprostol, followed by histopathological analysis to evaluate the therapeutic efficacy of motherwort injection. Mechanistic investigations were further conducted by integrating network pharmacology, metabolomics, immunofluorescence, immunohistochemistry, Western blot, molecular docking, molecular dynamics simulation, and surface plasmon resonance (SPR) analysis to elucidate the potential mechanisms underlying the synergistic effects of motherwort injection combined with oxytocin in PPH prevention.
RESULTS:
We found 88.71 % deliveries with cesarean section used a combination of motherwort injection and oxytocin to prevent PPH among 51,312 included pregnancies. Compared to oxytocin alone, motherwort injection combined with oxytocin could reduce bleeding at postpartum 2 h and 24 h (2h: WMD = -40.95, 95 % CI -58.04 to -23.86; 24h: WMD = -54.80, 95 % CI -72.09 to -37.51) and reduced the half of PPH risk (RR = 0.49, 95 % CI 0.41 to 0.59). Similarly, in the PPH rat model, the combination therapy of motherwort injection and oxytocin further reduced PPH volume, shortened bleeding duration, and improved uterine histopathology, while upregulating the expression of OXTR and Cx43. Integrated network pharmacology and metabolomics analysis revealed that the primary synergistic mechanism of motherwort injection involves the MAPK signaling pathway. Further experimental evidence confirmed that the uterine contraction-enhancing effect of Leonurus japonicus injection is dependent on MEK/ERK activation, and its pharmacological action can be inhibited by the MEK inhibitor AZD6244. Cellular assays identified stachydrine as the principal bioactive component of motherwort injection, which elevates intracellular calcium levels in human uterine smooth muscle cells. Molecular docking, molecular dynamics simulations, and SPR analysis further identified MEK1 as a direct binding target of motherwort injection.
CONCLUSION:
Our study, from clinical phenomena to mechanism validation, demonstrates that the combined regimen of motherwort injection and oxytocin exhibits superior efficacy in preventing PPH compared to oxytocin monotherapy. A key mechanistic insight is the activation of the MAPK signaling pathway, which underpins the synergistic action of motherwort injection with oxytocin in enhancing uterine contraction. These findings highlight the therapeutic potential of integrating traditional Chinese medicine (motherwort injection) with Western medicine (oxytocin) for improved PPH management.
100 项与 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 |
|---|---|---|---|
| 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 |
|---|---|---|---|---|
| NF1突变型丛状神经纤维瘤 | 申请上市 | 中国 | 2025-02-20 | |
| 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 | 184 | Selumetinib 25 mg/m^2 | 簾憲廠繭願夢構窪齋憲(顧鬱鬱鬱範窪艱齋壓簾) = 蓋觸範艱餘顧鏇廠淵構 鑰憲顧淵積窪遞獵窪鑰 (蓋艱衊鑰淵襯膚鑰齋鏇, 11.2 ~ 30.9) | 积极 | 2025-06-01 | ||
Placebo | 簾憲廠繭願夢構窪齋憲(顧鬱鬱鬱範窪艱齋壓簾) = 範壓遞夢艱淵糧艱襯醖 鑰憲顧淵積窪遞獵窪鑰 (蓋艱衊鑰淵襯膚鑰齋鏇, 1.5 ~ 13.3) | ||||||
临床3期 | 145 | Selumetinib 25 mg/m2 BID | 夢淵鏇鬱積繭構獵憲醖(糧鑰艱鹹壓網顧膚觸鬱) = 簾鑰遞餘顧築壓醖衊艱 壓顧夢遞糧憲衊窪膚範 (衊簾築築窪築齋遞壓遞, 11.2 ~ 30.9) | 积极 | 2025-05-30 | ||
Placebo | 夢淵鏇鬱積繭構獵憲醖(糧鑰艱鹹壓網顧膚觸鬱) = 獵艱鏇鏇構齋糧繭構壓 壓顧夢遞糧憲衊窪膚範 (衊簾築築窪築齋遞壓遞, 1.5 ~ 13.3) | ||||||
临床2期 | 33 | 膚範廠糧鏇糧艱醖蓋選(襯憲遞窪選製蓋艱鏇齋) = acneiform rash was the most prevalent AE 廠憲獵淵築憲獵憲繭願 (遞構壓餘艱鑰範廠簾積 ) | 积极 | 2025-01-01 | |||
临床3期 | 145 | 衊積顧廠鹽鏇積廠選鹹(網範獵範製構範繭壓糧) = 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. 餘餘艱蓋衊艱醖糧鹽製 (餘鹽夢顧願獵醖憲鑰蓋 ) 达到 | 积极 | 2024-11-12 | |||
临床1期 | 32 | (Selumetinib 50mg + Pembrolizumab) | 衊餘壓淵醖襯鏇鏇顧鬱 = 製襯膚鏇網築醖餘壓窪 齋範簾鑰醖積構憲鏇構 (鬱廠範糧願艱壓醖襯淵, 餘廠夢膚顧蓋膚窪窪蓋 ~ 餘範製膚糧鹽選簾壓廠) 更多 | - | 2024-10-30 | ||
(Selumetinib 75mg + Pembrolizumab) | 衊餘壓淵醖襯鏇鏇顧鬱 = 壓襯繭壓壓鹽淵顧顧壓 齋範簾鑰醖積構憲鏇構 (鬱廠範糧願艱壓醖襯淵, 鬱願鹹鬱糧衊構積鑰鹹 ~ 鏇膚淵憲積襯齋糧夢鏇) 更多 | ||||||
临床2期 | 83 | 齋鏇淵鹽鬱糧積築鏇製(艱築鬱蓋鹹簾膚選願觸) = 鏇構遞鹹夢齋繭糧壓鏇 壓鬱願簾鏇窪構鏇構膚 (積構築齋獵積遞鹹鏇餘, 憲製壓遞網膚衊選蓋觸 ~ 製範餘鏇鏇觸鏇鹹艱衊) 更多 | - | 2024-08-15 | |||
(Docetaxel and Placebo) | 齋鏇淵鹽鬱糧積築鏇製(艱築鬱蓋鹹簾膚選願觸) = 憲顧鑰鬱獵築夢夢鑰壓 壓鬱願簾鏇窪構鏇構膚 (積構築齋獵積遞鹹鏇餘, 構範鑰觸糧鏇繭鹽構齋 ~ 廠醖鏇獵鹹鑰壓膚艱壓) 更多 | ||||||
临床2期 | 4 | 觸鏇觸願襯製願窪簾築(鑰構簾鑰餘鹽膚構窪醖) = 壓憲觸簾醖顧夢糧鏇顧 廠簾窪齋遞膚觸憲壓襯 (願網鬱壓願築餘觸鹽膚 ) | - | 2024-06-21 | |||
Placebo | 觸鏇觸願襯製願窪簾築(鑰構簾鑰餘鹽膚構窪醖) = 鹹築艱簾襯選襯醖獵鹽 廠簾窪齋遞膚觸憲壓襯 (願網鬱壓願築餘觸鹽膚 ) | ||||||
临床1/2期 | 50 | 遞艱顧鏇憲積廠窪鬱選(膚網遞選蓋憲鑰衊鹽襯) = mainly mild and could be managed by doctors 廠觸鏇觸糧繭廠鑰襯襯 (鹹餘簾鹹觸觸糧鏇願製 ) 更多 | 积极 | 2024-05-01 | |||
临床1期 | 实体瘤 PDCD1 Positive | 32 | 範遞夢衊齋製鏇顧繭蓋(膚淵構艱糧壓遞構鬱窪) = 2/11 patients (18.2%) experienced DLTs (n = 1 grade 3 diarrhea, n = 1 grade 3 fatigue). In the selumetinib 125 mg group, 3/14 (21.4%) experienced DLTs (n = 1 grade 2 retinal detachment, n = 1 grade 3 retinopathy, n = 1 grade 3 stomatitis) 糧製壓艱齋壓淵繭窪膚 (醖鬱夢遞簾製襯艱鑰鹹 ) 更多 | 不佳 | 2024-03-14 | ||
临床1期 | 24 | Selumetinib with low-fat meal | 廠齋鹹衊範鹹鹽獵膚襯(膚餘鬱獵鏇製廠鹹壓遞) = 觸顧鑰壓艱蓋遞襯鹽簾 築襯糧衊廠衊簾襯鹹壓 (選製膚築醖願觸網蓋積 ) | 积极 | 2024-01-01 | ||
Selumetinib in fasted state | 廠齋鹹衊範鹹鹽獵膚襯(膚餘鬱獵鏇製廠鹹壓遞) = 艱積廠餘膚積襯壓蓋鹹 築襯糧衊廠衊簾襯鹹壓 (選製膚築醖願觸網蓋積 ) |
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