预约演示
更新于：2026-08-04
Elenestinib
更新于：2026-08-04
概要
基本信息
药物类型 小分子化药 |
别名 BLU 263、BLU-263 |
靶点 |
作用方式 抑制剂 |
作用机制 c-Kit抑制剂(干细胞生长因子受体抑制剂) |
在研适应症 |
非在研适应症 |
非在研机构- |
最高研发阶段临床2/3期 |
首次获批日期- |
最高研发阶段(中国)- |
特殊审评- |
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结构/序列
分子式C27H29FN10O |
InChIKeyIPMARPMXSFFZFG-MHZLTWQESA-N |
CAS号2505078-08-8 |
关联
3
项与 Elenestinib 相关的临床试验NCT07388511
A Phase 1, Open-Label Study to Evaluate the Effect of Elenestinib on the Pharmacokinetics of Midazolam and Combined Oral Contraceptives, Levonorgestrel/Ethinyl Estradiol, in Healthy Adult Female Participants
NCT05609942
A Phase 1/2, Open-label, 2-arm Study Evaluating BLU-263 as Monotherapy and in Combination With Azacitidine, in Patients With KIT Altered Hematologic Malignancies
NCT04910685
A Randomized, Double-Blind, Placebo-Controlled Phase 2/3 Study of BLU-263 in Indolent Systemic Mastocytosis
100 项与 Elenestinib 相关的临床结果
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100 项与 Elenestinib 相关的转化医学
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100 项与 Elenestinib 相关的专利（医药）
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3
项与 Elenestinib 相关的文献（医药）2023-07-03Expert opinion on emerging drugs
Systemic mastocytosis: 2023 update on diagnosis and management in adults
Review
作者: Claudia Ielo ; Ida Carmosino ; Chiara Masucci ; Massimo Breccia ; Maurizio Martelli ; Mauro Passucci ; Alessandro Costa ; Marcello Capriata ; Emilia Scalzulli
INTRODUCTION:
Systemic mastocytosis (SM) is a complex and heterogeneous disease, characterized by the clonal accumulation of mast cells in one or more organs. In 2022 both the World Health Organization (WHO) and the International Consensus Classification (ICC) modified the diagnostic and classification criteria of SM. Moreover, the identification of new clinical and molecular variables has improved prognostic tools and led to increasingly individualized therapeutic strategies.
AREAS COVERED:
The aim of this review is to present the updates introduced by the International Consensus Classification in diagnostic criteria of SM. In addition, we report the latest data available from the most important clinical trials in patients both with non-advanced and advanced disease, including elenestinib and bezuclastinib.
EXPERT OPINION:
Diagnosis and classification of SM has evolved over years. The most recent WHO and ICC classification improved SM diagnostic work-up, providing clinicians with a clear and simplified diagnostic scheme. New approved targeted therapies such as midostaurin and avapritinib modified the treatment paradigm in patients in advanced stage, and next-generation inhibitors actually investigated in clinical trials are expected in the next future.
2022-12-09Hematology. American Society of Hematology. Education Program
Available and emerging therapies for bona fide advanced systemic mastocytosis and primary eosinophilic neoplasms
Review
作者: Gotlib, Jason
Abstract:
The historically poor prognosis of patients with advanced systemic mastocytosis (AdvSM) and primary eosinophilic neoplasms has shifted to increasingly favorable outcomes with the discovery of druggable targets. The multikinase/KIT inhibitor midostaurin and the highly selective KIT D816V inhibitor avapritinib can elicit marked improvements in measures of mast cell (MC) burden as well as reversion of MC-mediated organ damage (C-findings) and disease symptoms. With avapritinib, the achievement of molecular remission of KIT D816V and improved survival compared with historical therapy suggests a potential to affect disease natural history. BLU-263 and bezuclastinib are KIT D816V inhibitors currently being tested in trials of AdvSM. In the new World Health Organization and International Consensus Classifications, the category of “myeloid/lymphoid neoplasms with eosinophilia and tyrosine kinase (TK) gene fusions” is inclusive of rearrangements involving PDGFRA, PDGFRB, FGFR1, JAK2, FLT3, and ETV6::ABL1. While the successful outcomes with imatinib in FIP1L1::PDGFRA-positive cases and PDGFRB-rearranged neoplasms have become the “poster children” of these disorders, the responses of the other TK-driven neoplasms to small-molecule inhibitors are more variable. The selective FGFR inhibitor pemigatinib, approved in August 2022, is a promising therapy in aggressive FGFR1-driven diseases and highlights the role of such agents in bridging patients to allogeneic transplantation. This review summarizes the data for these approved and investigational agents and discusses open questions and future priorities regarding the management of these rare diseases.
Journal of Blood Medicine
Management of Advanced Systemic Mastocytosis: Clinical Challenges
Review
作者: Mascarenhas, John ; Wagner, Nicole ; Tremblay, Douglas ; Wagner, Nicole E
Advanced systemic mastocytosis (AdvSM) is a rare hematologic malignancy with organ damage and compromised life expectancy arising from organ accumulation of neoplastic mast cells. Identification of the gain-of-function KITD816V in the majority of cases has accelerated pharmaceutical development culminating with the development of selective KIT inhibitors such as avapritinib. While the advent of these therapies has improved the quality and quantity of life in patients with AdvSM, current challenges remain in the management of this disease. In this review, we summarize the present and future therapeutics landscape of AdvSM, highlighting the development of novel KIT inhibitors including elenestinib and bezuclastinib. We also explore the continued role of additional treatment modalities including allogeneic stem cell transplantation before discussing unresolved clinical challenges in the management of AdvSM.
100 项与 Elenestinib 相关的药物交易
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研发状态
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 髓性系统性肥大细胞增多症 | 临床3期 | 美国 | 2021-11-30 | |
| 髓性系统性肥大细胞增多症 | 临床3期 | 阿根廷 | 2021-11-30 | |
| 髓性系统性肥大细胞增多症 | 临床3期 | 澳大利亚 | 2021-11-30 | |
| 髓性系统性肥大细胞增多症 | 临床3期 | 奥地利 | 2021-11-30 | |
| 髓性系统性肥大细胞增多症 | 临床3期 | 比利时 | 2021-11-30 | |
| 髓性系统性肥大细胞增多症 | 临床3期 | 巴西 | 2021-11-30 | |
| 髓性系统性肥大细胞增多症 | 临床3期 | 哥伦比亚 | 2021-11-30 | |
| 髓性系统性肥大细胞增多症 | 临床3期 | 捷克 | 2021-11-30 | |
| 髓性系统性肥大细胞增多症 | 临床3期 | 法国 | 2021-11-30 | |
| 髓性系统性肥大细胞增多症 | 临床3期 | 德国 | 2021-11-30 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
临床2/3期 | 髓性系统性肥大细胞增多症 KIT D816V mutation | 350 | Elenestinib 75 mg QD + SDT | 憲襯鏇選選廠鬱願顧襯(鑰鹽鹽淵餘構淵簾廠餘) = 齋積顧簾鹹顧憲艱糧簾 顧構顧築鹹積廠糧繭鏇 (鹽鏇鹽鬱鹹顧蓋獵顧願 ) 更多 | 积极 | 2026-05-12 | |
N/A | - | 壓網襯衊壓襯顧淵範鏇(範餘窪簾繭鏇網積壓積) = There were no treatment-related adverse events that led to drug discontinuation 膚鹹構願艱壓鏇糧網鏇 (襯顧願顧築範廠鹽製鏇 ) 更多 | - | 2023-12-09 | |||
临床2/3期 | 29 | 鏇憲繭餘淵鹹鏇觸壓遞(網遞醖積鹽繭鏇鹹鬱遞) = Safety results indicated that eletinib was generally well tolerated, with no discontinuation due to adverse events 鑰膚繭鬱製醖鑰壓範廠 (艱衊膚糧憲淵構遞網鏇 ) | 积极 | 2022-12-11 |
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