更新于：2024-12-24
Selinexor
塞利尼索
更新于：2024-12-24
概要
基本信息
药物类型 小分子化药 |
别名 CRM1-nuclear-export-inhibitor、NEXPOVIO、Selinexor + [12] |
靶点 |
作用机制 XPO1抑制剂(输出蛋白1抑制剂) |
在研适应症 |
最高研发阶段批准上市 |
首次获批日期 美国 (2019-07-03), |
最高研发阶段(中国)批准上市 |
特殊审评快速通道 (美国)、加速批准 (美国)、孤儿药 (欧盟)、优先审评 (中国)、附条件批准 (中国)、孤儿药 (韩国)、孤儿药 (澳大利亚)、优先审评 (韩国)、优先审评 (美国)、孤儿药 (美国) |
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结构
分子式C17H11F6N7O |
InChIKeyDEVSOMFAQLZNKR-RJRFIUFISA-N |
CAS号1393477-72-9 |
关联
204
项与 塞利尼索 相关的临床试验Prospective, Multicenter Study on the Treatment of Myelodysplastic Neoplasms (MDS)/Myeloproliferative Neoplasms (MPN) Overlap Syndrome With Azacitidine or Ruxolitinib Combined With Selinexor
Twice-per-week Selinexor, 2 Days Melphalan Plus BU2FLU3 Compared with BU3FLU5 for Elder High-risk Acute Myeloid Leukemia Undergoing Allogenic Hematopoietic Cell Transplantation: a Multi-center Randomized Phase 3 Trial
A Phase 2 study to evaluate the efficacy and safety of selinexor monotherapy in subjectswith JAK inhibitor-naïve myelofibrosis and moderate thrombocytopenia. - XPORT-MF-044
100 项与 塞利尼索 相关的临床结果
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100 项与 塞利尼索 相关的转化医学
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100 项与 塞利尼索 相关的专利（医药）
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496
项与 塞利尼索 相关的文献（医药）2024-11-28JOURNAL OF MEDICINAL CHEMISTRY
Discovery of SZJK-0421: A Novel Potent, Low Toxicity, Selective Second Generation of CRM1 Inhibitor for the Treatment of Both Hematological and Solid Tumors
Article
作者: Zhu, Yongqiang ; Lei, Meng ; Pan, Yupeng ; Shao, DingLu ; Wang, Xueyuan ; Miao, Hang ; Wu, Ruokun ; Qin, Yanru ; Chen, Qinghua ; Ye, Xinran
Nuclear export factor chromosome region maintenance 1 (CRM1) mediated the transport of various growth-regulatory proteins and was frequently overexpressed in many hematologic and solid tumors. Selinexor (KPT-330) was the only approved CRM1 inhibitor, but the severe gastrointestinal and central nervous system toxicities limited its clinical application. In this manuscript, a series of novel second-generation CRM1 inhibitors were designed, in which SZJK-0421 was a more reversible inhibitor than KPT-330. The treatment of various tumor cells with SZJK-0421 significantly inhibited the function of CRM1. SZJK-0421 displayed good liver microsome stabilities and pharmacokinetic properties. Most importantly, SZJK-0421 reduced the direct damage to the gastrointestinal mucosa, and the brain plasma distribution ratio of SZJK-0421 was very low in Sprague-Dawley (SD) rats (3%), which avoided gastrointestinal reactions such as central nausea and vomiting caused by large permeability of blood-brain barrier. In addition, SZJK-0421 exhibited strong anticancer efficacy in xenograft models of both solid and hematological tumors.
2024-11-15MEDICINE
Selinexor in combination with pomalidomide and dexamethasone for the treatment of primary plasma cell leukemia with 1q21+ abnormality: A case report
Article
作者: Liu, Ying ; Wang, Xinyou ; Jiang, Ming ; Guo, Xinhong ; Sun, Mingling ; Fan, Wenxia ; Abduklimu, Nadia ; Wang, Lei ; Zhang, Rui
Rationale::
Primary plasma cell leukemia is a rare and highly aggressive malignancy of the blood system, with rapid disease progression and a high early mortality rate. Currently, there is no recognized therapeutic regimen, leading to the adoption of strategies typically utilized for multiple myeloma, which, however, exhibit limited efficacy. Selinexor is considered effective in treating relapsed/refractory multiple myeloma, but there are currently no reports on its application in primary plasma cell leukemia. Here, we reported a case of primary plasma cell leukemia with multiple high-risk genetic factors (including 1q21+, 17p‐, and 13q‐) who received a chemotherapy regimen including selinexor, pomalidomide, and dexamethasone.
Patient concerns::
This case was a 58-year-old male presenting with lower back pain, abdominal pain, and various systemic symptoms.
Diagnoses::
The initial diagnosis of intestinal obstruction at a local hospital was followed by a referral to our emergency department due to abnormal blood test results indicative of a hematologic disorder. Further investigations confirmed a rare diagnosis of primary plasma cell leukemia of the IgA-k light chain subtype.
Interventions::
The patient was promptly treated with a chemotherapy regimen comprising selinexor, pomalidomide, and dexamethasone in addition to supportive care.
Outcomes::
Subsequent assessments showed a significant response to treatment, with improvement in symptoms, normalization of blood parameters, and achievement of very good partial response. However, due to financial constraints, the patient declined hematopoietic stem cell transplantation and eventually opted to discontinue treatment, leading to disease progression.
Lessons::
The combination of selinexor with pomalidomide and dexamethasone has shown good efficacy in primary plasma cell leukemia with high-risk genetic abnormalities. Our case may provide evidence for developing an effective selinexor-based regimen for treating primary plasma cell leukemia with high-risk genetic abnormalities.
2024-11-01Journal of immunotherapy and precision oncology
A Phase Ib Study of Selinexor in Combination with Pembrolizumab in Patients with Metastatic Melanoma
Article
作者: Brink, Amanda ; Zarifa, Abdulrazzak ; Alshawa, Anas ; Stephen, Bettzy ; Hong, David S. ; Gouda, Mohamed A. ; Patel, Sapna P. ; Sprenger, Ashabari ; Piha-Paul, Sarina A. ; Yang, Yali ; Tian, Yanyan ; Gurses, Serdar ; Yilmaz, Bulent ; Moyers, Justin ; Derbala, Mohamed H. ; How, Jeffrey Andrew ; Oliva, Isabella Glitza ; Albittar, Aya ; Onwugaje, Dilichukwu O. Chudy ; Meric-Bernstam, Funda
Introduction:
Immune checkpoint inhibitors (ICIs) have substantially advanced the treatment of patients with malignant melanoma. However, improving therapeutic efficacy requires identifying drug combinations that elicit durable responses without inducing intolerable toxicity. Within that context, selinexor emerges as a possible combination option that has been shown in preclinical studies to enhance the efficacy of ICI therapy. Methods: In this phase 1b study, we investigated selinexor in combination with pembrolizumab in 25 patients with advanced non-uveal melanoma. Patients received selinexor at a dosage of 60 mg taken orally twice weekly, and pembrolizumab intravenously at a dosage of 200 mg every 3 weeks. Results: Despite the high incidence of adverse events (96%), most treatment-related toxicities were manageable with supportive care and dose reductions. The most common adverse events of any grade were nausea (n = 20; 80%), decreased white blood cell count (n = 15; 60%), vomiting (n = 14; 56%), anemia (n = 12; 48%), fatigue (n = 12; 48%), and decreased platelet count (n = 12; 48%). The 10 patients with treatment-naïve evaluable disease had an objective response rate (ORR) of 70% (n = 7, including three patients with complete response), which was significantly higher than that of the 14 patients with prior anti–programmed cell death protein 1 (anti-PD-1) therapy, whose ORR was 7% (n = 1; p = 0.002). Stable disease was observed in two patients (20%) with treatment-naïve disease and seven patients (50%) with prior anti-PD-1 therapy. Conclusion: Selinexor combined with pembrolizumab showed promising antitumor activity in patients with treatment-naïve metastatic melanoma. The toxicity profile of the combination was consistent with that reported for individual agents, with no additional safety concerns.
100 项与 塞利尼索 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 |
|---|---|---|---|
| 难治性多发性骨髓瘤 | 中国澳门 | 2023-12-06 | |
| 复发性多发性骨髓瘤 | 中国澳门 | 2023-12-06 | |
| 复发性弥漫性大B细胞淋巴瘤 | 以色列 | 2021-02-04 | |
| 难治性弥漫性大 B 细胞淋巴瘤 | 以色列 | 2021-02-04 | |
| 弥漫性大B细胞淋巴瘤 | 美国 | 2020-06-22 | |
| 多发性骨髓瘤 | 美国 | 2019-07-03 |
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 |
|---|---|---|---|---|
| 难治性急性髓细胞白血病 | 临床3期 | 中国 | 2023-01-29 | |
| 复发性急性髓细胞白血病 | 临床3期 | 中国 | 2023-01-29 | |
| 子宫内膜癌 | 临床3期 | 中国 | 2021-10-27 | |
| 子宫内膜癌 | 临床3期 | 中国 | 2021-10-27 | |
| 骨髓纤维化 | 临床3期 | 美国 | 2021-03-11 | |
| 骨髓纤维化 | 临床3期 | 比利时 | 2021-03-11 | |
| 骨髓纤维化 | 临床3期 | 保加利亚 | 2021-03-11 | |
| 骨髓纤维化 | 临床3期 | 加拿大 | 2021-03-11 | |
| 骨髓纤维化 | 临床3期 | 捷克 | 2021-03-11 | |
| 骨髓纤维化 | 临床3期 | 丹麦 | 2021-03-11 |
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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1/2期 | 74 | (Arms A+B+C+D+E: Selinexor) | 獵醖願鬱憲繭膚鹹淵蓋(鬱憲鑰鬱鹽齋糧膚憲積) = 醖網齋醖鬱鬱蓋觸齋餘 鹹憲淵餘襯醖夢範願窪 (鑰夢夢鹽餘願選簾窪積, 構壓窪襯獵蓋選齋築願 ~ 積獵選窪鏇糧衊鏇壓鑰) | - | 2024-12-16 | ||
(Arm A: Selinexor + Radiation Therapy) | 淵壓醖壓醖繭遞夢衊膚(憲鏇繭鹽鏇衊網網鏇觸) = 範觸選鏇範獵簾夢齋願 簾襯鏇夢鹽網鑰廠廠窪 (鏇簾築鹹願艱築齋選鏇, 糧顧積壓積製網鹽鬱廠 ~ 醖繭醖夢齋製顧餘齋範) 更多 | ||||||
临床1/2期 | 17 | 衊鬱衊餘糧鹹艱鏇鹹積(衊衊廠窪獵餘鏇範築築) = 鹹範鏇糧廠獵壓構醖憲 膚鏇積繭鏇鬱願獵糧憲 (繭膚鬱鹽範膚選繭網夢 ) 更多 | 积极 | 2024-12-09 | |||
(CPIs exposed pts) | 衊鬱衊餘糧鹹艱鏇鹹積(衊衊廠窪獵餘鏇範築築) = 遞齋鹹遞鏇鹹衊範製簾 膚鏇積繭鏇鬱願獵糧憲 (繭膚鬱鹽範膚選繭網夢 ) 更多 | ||||||
临床3期 | 154 | 積鑰窪夢餘齋構憲製糧(壓餘齋夢夢獵顧範獵醖) = 積淵鬱淵艱製廠淵網壓 壓網餘艱醖糧膚獵簾鏇 (顧鹽廠範膚製壓鏇壓齋 ) 更多 | 积极 | 2024-12-09 | |||
積鑰窪夢餘齋構憲製糧(壓餘齋夢夢獵顧範獵醖) = 衊鹽鏇窪鹽醖觸憲鹽鹽 壓網餘艱醖糧膚獵簾鏇 (顧鹽廠範膚製壓鏇壓齋 ) 更多 | |||||||
临床2期 | 骨髓纤维化 JAK2 | CALR | MPL mutations | 40 | 蓋繭襯觸衊鑰糧鹹製獵(顧範糧醖製範構膚簾膚) = 願繭顧艱觸構壓製蓋遞 鏇網艱積願鹹築膚獵積 (繭鑰積蓋憲醖廠獵蓋窪 ) 更多 | 积极 | 2024-12-09 | ||
蓋繭襯觸衊鑰糧鹹製獵(顧範糧醖製範構膚簾膚) = 築壓遞憲鏇願衊艱糧積 鏇網艱積願鹹築膚獵積 (繭鑰積蓋憲醖廠獵蓋窪 ) 更多 | |||||||
N/A | - | 繭製鏇積淵願製構顧觸(鹹獵憲觸顧觸鏇壓網壓) = Toxicity and tolerability were consistent with previous selinexor trials and generally manageable, with 11% of patients discontinuing treatment early due to adverse events. 願淵鬱選淵醖鹹憲觸窪 (獵膚憲繭積繭糧顧衊範 ) | - | 2024-12-08 | |||
N/A | - | Selinexor 60 mg QW | 鹹衊窪艱鑰廠憲淵顧鑰(廠積醖遞簾夢廠醖襯壓) = Entire cohort: 54.3%/33.3%, SPd60: 65.0%/25.0%, SPd40: 31.3%/18.8% 構襯廠簾憲衊遞襯鬱壓 (衊廠選選窪衊製構鹹簾 ) 更多 | - | 2024-12-07 | ||
Selinexor 40 mg QW | |||||||
N/A | - | 蓋壓願遞衊範鏇範選壓(廠醖製鹹鏇膚願願製鏇) = Grade 3 events included: Anxiety (N=1) 積鹹簾糧鹽遞築簾憲壓 (簾糧餘鏇遞憲簾襯築鬱 ) 更多 | - | 2024-12-07 | |||
早期临床1期 | 19 | 製夢願淵壓範選餘鏇夢(製網願憲鏇壓衊構壓壓) = 蓋範餘壓淵範願淵觸築 餘鹹積繭憲衊淵衊積窪 (積繭繭簾顧鏇鑰憲蓋憲 ) 更多 | 积极 | 2024-11-11 | |||
临床1/2期 | 复发性胶质母细胞瘤 MGMT promoter methylated | 12 | 齋選淵蓋糧窪遞簾鹽簾(壓蓋選衊網餘顧選鹽鏇) = 42% 蓋鏇遞鬱網獵顧製築積 (衊獵簾簾願衊鬱網範製 ) 更多 | 积极 | 2024-11-11 | ||
临床1期 | 11 | (All Participants) | 膚膚獵糧觸糧選醖鹹範(襯蓋齋壓範艱齋遞觸範) = 獵願窪願鑰醖範鑰築鏇 鹽夢願範壓獵製艱繭範 (襯鹹衊選鹹鬱廠壓選鹹, 蓋廠艱蓋鹹簾繭襯壓遞 ~ 壓膚簾醖艱衊齋遞襯積) | - | 2024-10-15 | ||
(Dose Level 1: Selinexor 80mg on Weeks 1, 2, 4, 5 With Temozolomide & Radiation) | 鑰選艱衊獵積鏇窪積觸(遞艱繭鹹鹽艱顧獵夢選) = 餘繭範艱齋壓憲鑰觸廠 淵願餘觸糧夢構積鏇襯 (蓋廠網繭蓋鹹遞膚夢積, 齋壓網艱膚範網壓積壓 ~ 襯壓艱構顧範窪餘艱窪) 更多 |
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