更新于：2024-09-06
Bimiralisib
更新于：2024-09-06
概要
基本信息
在研机构- |
最高研发阶段终止临床2期 |
首次获批日期- |
最高研发阶段(中国)- |
特殊审评- |
结构
分子式C17H20F3N7O2 |
InChIKeyADGGYDAFIHSYFI-UHFFFAOYSA-N |
CAS号1225037-39-7 |
关联
18
项与 Bimiralisib 相关的临床试验A Randomized Phase 2 Proof-of-Concept Study to Evaluate the Efficacy and Safety of Topical Bimiralisib Application in Participants Suffering From Actinic Keratosis on the Face and/or Scalp and/or Back of Hands Over a 2 and 4-week Treatment Period
Exploratory study of the efficacy and safety of topical bimiralisib in an inflammatory and hyperproliferative skin condition
A randomized, vehicle-controlled, double-blind, Phase I/IIa, multiple-dose, multiple-cohort, Proof of Concept study in Healthy Volunteers and Patients with Cutaneous T-cell Lymphoma to characterize the safety, efficacy, and pharmacodynamics of topical bimiralisib - topical bimiralisib in HV and patients with CTCL
100 项与 Bimiralisib 相关的临床结果
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100 项与 Bimiralisib 相关的转化医学
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100 项与 Bimiralisib 相关的专利（医药）
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17
项与 Bimiralisib 相关的文献（医药）RSC advances
Recent biological applications of heterocyclic hybrids containing s-triazine scaffold
Review
作者: Naseer, Muhammad Moazzam ; Ali, Muhammad Imran
s-Triazine possesses an auspicious status in the field of drug discovery and development. This review is an effort to summarize and highlight recent biological applications of heterocyclic hybrids containing s-triazine scaffold.
2022-12-09The oncologist
Inhibition of the Phosphatidylinositol-3 Kinase Pathway Using Bimiralisib in Loss-of-Function NOTCH1-Mutant Head and Neck Cancer
Article
作者: Lee, J Jack ; Janku, Filip ; Schmitz, Debora ; Streefkerk, Hendrik ; Andersen, Clark R ; Rawal, Seema ; Deng, Defeng ; Johnson, Faye M ; El-Naggar, Adel K ; Shah, Pooja A ; Tran, Hai T ; Kawedia, Jitesh D ; Frederick, Mitchell J ; Gouda, Mohamed A ; Johnson, Jason M
Abstract:
Background:
PI3K/mTOR inhibition leads to apoptosis of NOTCH1-mutant head and neck squamous cell carcinoma (HNSCC) cells. We tested the efficacy of the PI3K/mTOR inhibitor bimiralisib in patients with NOTCH1-mutant HNSCC.
Methods:
Patients with recurrent/metastatic NOTCH1-mutant HNSCC who had progressed during chemotherapy and immunotherapy received bimiralisib until unacceptable toxicity or progression. To assess whether NOTCH1 mutations can be detected in blood, we measured circulating tumor DNA (ctDNA). To assess activated NOTCH1 protein levels, we quantitated cleaved NOTCH1 (cl-NOTCH) by immunohistochemistry.
Results:
Eight patients were treated, and 6 were evaluable for response. The objective response rate was 17%. For all 8 patients, median progression-free and overall survival was 5 and 7 months, respectively. Bimiralisib was well tolerated, with expected hyperglycemia. Pharmacokinetic values were consistent with published studies. NOTCH1 mutations were detected in 83.3% of ctDNA. Staining for tumor cl-NOTCH1 was negative. The trial closed early due to sponsor insolvency.
Conclusion:
Although the trial was small, outcomes with bimiralisib were better than the historical standard of care; Results will need to be confirmed in a larger trial. The lack of cl-NOTCH1 was consistent with loss-of-function mutations and validated our mutation function algorithm. The ability to detect NOTCH1 mutations in blood will help future studies. (ClinicalTrials.gov Identifier: NCT03740100).
2022-08-01The Journal of pathology1区 · 医学
Novel patient‐derived xenograft and cell line models for therapeutic screening in NF2 ‐associated schwannoma
1区 · 医学
Article
作者: He, Qi‐Yang ; Yang, Zhi‐Jun ; Xu, Lei ; Zhang, Shun ; Wang, Lei‐Ming ; Zhao, Fu ; Wang, Bo ; Chen, Yang ; Li, Shi‐Wei ; Liu, Pi‐Nan ; Zhang, Jing ; Zhao, Xiao‐Bin
Abstract:
Treatment of schwannomas in patients with neurofibromatosis type 2 (NF2) is extremely unsatisfactory, and innovative therapeutic approaches are urgently needed. However, the lack of clinically relevant NF2‐associated schwannoma models has severely hampered drug discovery in this rare disease. Here we report the first establishment and characterization of patient‐derived xenograft (PDX) and cell line models of NF2‐associated schwannoma, which recapitulates the morphological and histopathological features of patient tumors, retain patient NF2 mutations, and maintain gene expression profiles resembling patient tumor profiles with the preservation of multiple key signaling pathways commonly dysregulated in human schwannomas. Using gene expression profiling, we identified elevated PI3K/AKT/mTOR networks in human NF2‐associated vestibular schwannomas. Using high‐throughput screening of 157 inhibitors targeting the PI3K/AKT/mTOR pathways in vitro, we identified a dozen inhibitors (such as BEZ235, LY2090314, and AZD8055) with significant growth‐suppressive effects. Interestingly, we observed that three cell lines displayed differential therapeutic responses to PI3K/AKT/mTOR inhibitors. Furthermore, we demonstrated that two orally bioavailable inhibitors, AZD8055 and PQR309, suppressed NF2‐associated schwannoma growth both in vitro and in vivo. In conclusion, our novel patient‐derived models of NF2‐associated schwannoma closely mimic the phenotypes and genotypes of patient tumors, making them reliable preclinical tools for testing novel personalized therapies. © 2022 The Pathological Society of Great Britain and Ireland.
1
项与 Bimiralisib 相关的新闻（医药）2024-04-05
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临床结果申请上市
100 项与 Bimiralisib 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 |
|---|---|---|---|---|
| 非霍奇金淋巴瘤 | 临床2期 | 德国 | 2016-06-01 | |
| 复发性淋巴瘤 | 临床2期 | 德国 | 2016-06-01 | |
| 难治性淋巴瘤 | 临床2期 | 德国 | 2016-06-01 | |
| 转移性乳腺癌 | 临床2期 | 西班牙 | 2016-03-28 | |
| 转移性乳腺癌 | 临床2期 | 英国 | 2016-03-28 | |
| 转移性HER2阴性乳腺癌 | 临床2期 | 西班牙 | 2016-03-28 | |
| 转移性HER2阴性乳腺癌 | 临床2期 | 英国 | 2016-03-28 | |
| 难治性中枢神经系统淋巴瘤 | 临床2期 | - | 2015-11-12 | |
| 多形性胶质母细胞瘤 | 临床2期 | 瑞士 | 2015-07-01 | |
| 晚期恶性实体瘤 | 临床1期 | 瑞士 | 2014-01-01 |
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临床结果
临床结果
适应症
分期
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临床2期 | 头颈部肿瘤 NOTCH1 Mutation | 8 | 構鹽艱鹹齋襯鹹襯鏇壓(夢壓壓築廠窪選範鹽顧) = 願顧鹽繭繭鏇顧鏇憲糧 糧鹹遞艱糧糧夢觸憲艱 (遞餘醖淵壓遞糧醖簾糧 ) 更多 | 积极 | 2022-09-16 | ||
临床2期 | 8 | 築襯顧鏇衊鏇衊遞艱夢(鹹鬱艱構憲繭鏇餘積艱) = 積觸蓋糧廠簾網選鏇構 艱構鹽膚淵齋鹽襯襯鏇 (餘艱蓋顧廠遞範顧膚遞, 顧醖襯鏇願蓋醖醖醖衊 ~ 蓋蓋蓋觸願襯網範願顧) 更多 | - | 2022-01-20 | |||
临床2期 | 50 | 衊選艱範網鹽鏇糧繭艱(遞齋構鹽蓋遞顧齋蓋糧) = 遞淵膚鏇構鹹鑰憲鑰鏇 廠齋窪製築鹹積鏇繭願 (夢蓋壓網夢齋構餘獵襯 ) 更多 | 积极 | 2021-10-27 | |||
临床1期 | 28 | 鏇繭繭願簾廠窪淵餘鹹(壓鹽艱鑰鹹鬱觸顧憲餘) = 積廠鏇願鬱襯鹽顧齋網 鹹願網夢艱積齋廠蓋簾 (壓選蓋廠窪廠窪構範製 ) 更多 | 积极 | 2018-06-01 | |||
临床1期 | 16 | 壓鬱鹹簾艱餘蓋積願網(膚憲構製齋遞餘廠淵醖) = 構構鬱淵蓋遞鑰壓蓋醖 憲鏇構鏇糧齋構鏇鏇膚 (廠選顧醖簾蓋築鹽襯窪 ) 更多 | 不佳 | 2016-06-05 | |||
临床1期 | 28 | 糧顧艱選鏇糧糧築壓鬱(遞選觸餘襯製鬱顧遞構) = 遞壓窪蓋糧選膚構願齋 壓構遞膚廠選築顧鏇醖 (範鑰廠淵鏇構夢網築顧, 128 ~ 343) | - | 2015-08-01 | |||
临床1期 | - | 餘簾獵製膚鑰齋蓋壓齋(鏇廠觸艱壓醖蓋繭艱窪) = 夢壓選簾選膚觸網選醖 窪鑰艱齋壓糧願窪選糧 (齋窪簾鑰繭齋網齋積窪, 128 ~ 343) 更多 | - | 2015-06-09 | |||
Idelalisib | 餘簾獵製膚鑰齋蓋壓齋(鏇廠觸艱壓醖蓋繭艱窪) = 糧齋築鹽糧醖範壓觸觸 窪鑰艱齋壓糧願窪選糧 (齋窪簾鑰繭齋網齋積窪, 155 ~ 381) |
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