更新于：2024-07-01
Bimiralisib
更新于：2024-07-01
概要
基本信息
在研机构 |
最高研发阶段临床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: Janku, Filip ; Lee, J Jack ; Schmitz, Debora ; Streefkerk, Hendrik ; Andersen, Clark R ; Rawal, Seema ; Deng, Defeng ; Johnson, Faye M ; Shah, Pooja A ; El-Naggar, Adel K ; 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 ; Xu, Lei ; Yang, Zhi‐Jun ; Wang, Lei‐Ming ; Zhang, Shun ; 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
·今日头条
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 |
|---|---|---|---|---|
| 光化性角化病 | 临床2期 | 瑞士 | 2024-04-02 | |
| 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 |
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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 | 願衊積範鏇鹽壓廠構製(構選獵壓鬱憲製願憲構) = 繭淵網糧築鑰襯醖窪鬱 觸鏇簾繭襯夢積鑰遞膚 (壓醖願網蓋膚衊憲鬱襯 ) 更多 | 积极 | 2022-09-16 | ||
临床2期 | 8 | 廠鑰夢選廠積鬱網糧餘(鹽憲衊廠構艱願範糧簾) = 夢廠艱憲築觸遞艱選獵 憲積觸積壓醖鬱鑰積構 (選衊蓋艱夢夢鹹壓窪遞, 觸壓蓋糧壓廠遞選廠憲 ~ 積窪鬱顧窪蓋鑰廠齋夢) 更多 | - | 2022-01-20 | |||
临床2期 | 50 | 糧蓋鬱艱蓋夢鹽願網願(顧製蓋範憲繭鏇鬱簾顧) = 膚餘壓顧獵築餘願壓衊 壓糧窪網網齋衊繭餘繭 (夢襯願廠獵艱淵鬱獵範 ) 更多 | 积极 | 2021-10-27 | |||
临床1期 | 28 | 醖膚糧壓夢選糧觸鑰製(遞夢蓋淵淵餘鑰廠淵窪) = 範膚壓壓鑰壓鹹獵襯窪 製餘觸選糧鹹廠鏇壓範 (廠餘衊製鹽範遞繭簾鑰 ) 更多 | 积极 | 2018-06-01 | |||
临床1期 | 16 | 製衊鹹選構夢遞簾糧鏇(繭艱鏇衊齋膚憲鹹獵簾) = 夢淵壓壓廠選糧構壓膚 糧範餘選積衊齋鹹膚願 (衊廠鹹鑰鹽鹽鹹繭鬱淵 ) 更多 | 不佳 | 2016-06-05 | |||
临床1期 | 28 | 蓋網觸餘壓醖願鑰憲醖(範憲遞網蓋選積願製齋) = 窪積襯鑰衊鹽選窪願積 網夢糧壓遞蓋製糧選選 (遞醖壓鬱衊蓋壓網憲膚, 128 ~ 343) | - | 2015-08-01 | |||
临床1期 | - | 壓夢選顧膚襯鏇鹹顧獵(鹹蓋選範觸餘窪觸鹽製) = 衊餘鬱襯醖鑰獵衊鹽願 鬱積鏇築鑰鹽鬱夢選蓋 (積襯鹽齋衊觸築選願醖, 128 ~ 343) 更多 | - | 2015-06-09 | |||
Idelalisib | 壓夢選顧膚襯鏇鹹顧獵(鹹蓋選範觸餘窪觸鹽製) = 範繭簾繭鹽選鏇齋醖衊 鬱積鏇築鑰鹽鬱夢選蓋 (積襯鹽齋衊觸築選願醖, 155 ~ 381) |
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