更新于：2024-12-25
Penfluridol
五氟利多
更新于：2024-12-25
概要
基本信息
原研机构 |
在研机构 |
非在研机构- |
最高研发阶段批准上市 |
首次获批日期- |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构
分子式C28H27ClF5NO |
InChIKeyMDLAAYDRRZXJIF-UHFFFAOYSA-N |
CAS号26864-56-2 |
关联
1
项与 五氟利多 相关的临床试验Effectiveness of penfluridol (oral long acting neuroleptic) as compared to second generation oral neuroleptics in psychotic disorder patients: an open label randomized controlled trial. - The One for Seven Study
100 项与 五氟利多 相关的临床结果
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100 项与 五氟利多 相关的转化医学
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100 项与 五氟利多 相关的专利（医药）
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262
项与 五氟利多 相关的文献（医药）2024-12-01PHARMACOLOGICAL RESEARCH
Penfluridol suppresses MYC-driven ANLN expression and liver cancer progression by disrupting the KEAP1–NRF2 interaction
Article
作者: Kim, Sang Geon ; Lee, Gi Jeong ; Kang, Gyeoung Jin ; Lee, Chang Hoon ; Nguyen, Minh Tuan ; Kim, Boram ; Kim, Eun Ji ; Tak, Jihoon ; Lee, Kyung ; Lee, Ho ; Rho, Seung Bae ; Park, Mi Kyung ; Kim, Hyun Ji
Hepatocellular carcinoma (HCC) comprises the majority of primary liver cancers and possesses a low 5-year survival rate when in the advanced stages. Anillin (ANLN), a key player in cell growth and cytokinesis, is implicated in HCC development. Currently, no treatment agents are known to suppress ANLN. Analysis of The Cancer Genome Atlas data showed that high ANLN expression is associated with poor prognosis and survival in HCC patients. ANLN knockdown was shown to inhibit proliferation, cell cycle progression, and PD-L1 expression in liver cancer cells. The antipsychotic drug penfluridol was identified to suppress ANLN expression in the Connectivity Map analysis. Penfluridol downregulated ANLN at both the mRNA and protein levels, leading to G2/M cell cycle arrest and reduced colony formation in liver cancer cells. Mechanistically, penfluridol inhibited the transcription factor MYC from binding to an E-box motif in the ANLN promoter. This process was mediated by penfluridol-induced upregulation of NRF2, which competitively bound and sequestered MYC away from the ANLN promoter. Penfluridol inhibited the interaction between NRF2 and KEAP1, increasing NRF2. In a syngeneic mouse model, penfluridol suppressed liver tumour growth accompanied by increased NRF2 and decreased MYC and ANLN expression. These findings suggest penfluridol can be applied as the first ANLN blocker to modulate the MYC/NRF2/KEAP1 axis.
2024-10-29Nederlands tijdschrift voor geneeskunde
[Shortage antipsychotic medication supply hits vulnerable patients most].
Article
作者: Jacobsen, Bettina ; TeStroet, Martijn A J ; Moerkens, S A
Medication shortages in The Netherlands are getting worse since 2019, with numbers increasing every year. In September 2023, during our work in a psychiatric outpatient clinic, we were confronted with the consequences of these rising numbers. There was an acute shortage of penfluridol, an antipsychotic medication. Soon thereafter, another shortage occurred. The intramuscular depot of olanzapine (Zypadhera) was not available over a long period of time. Shortages of antipsychotic medication supply could have severe consequences. Stopping or switching medication can lead to psychotic decompensation. During a psychotic episode, a patient can lose his mental stability and all facets of life can be affected. Therefore, the medication shortages can have a life altering effect. As healthcare workers we feel obliged to report about the consequences of the severity of the rising number of medication shortages and highlight the consequences of the vulnerability of psychiatric patients.
2024-10-01MedComm
Penfluridol inhibits melanoma growth and metastasis through enhancing von Hippel‒Lindau tumor suppressor‐mediated cancerous inhibitor of protein phosphatase 2A (CIP2A) degradation
Article
作者: Sun, Qingxiang ; Xia, Yong ; Pu, Wenchen ; Li, Jiao ; Peng, Yong ; Ai, Min ; Li, Zhang ; Xu, Xiaomin ; Zhang, Tingting ; Yang, Yang ; Xu, Fuyan ; Qi, Yucheng ; Yuan, Zhu ; Ming, Yue ; Li, Cong
Abstract:
Melanoma's high metastatic potential, especially to the brain, poses significant challenges to patient survival. The blood‒brain barrier (BBB) is a major obstacle to the effective treatment of melanoma brain metastases. We screened antipsychotic drugs capable of crossing the BBB and identified penfluridol (PF) as the most active candidate. PF reduced melanoma cell viability and induced apoptosis. In animal models, PF effectively inhibited melanoma growth and metastasis to the lung and brain. Using immunoprecipitation combined with high‐resolution mass spectrometry, and other techniques such as drug affinity responsive target stability, we identified CIP2A as a direct binding protein of PF. CIP2A is highly expressed in melanoma and its metastases, and is linked to poor prognosis. PF can restore Protein Phosphatase 2A activity by promoting CIP2A degradation, thereby inhibiting several key oncogenic pathways, including AKT and c‐Myc. Additionally, von Hippel‒Lindau (VHL) is the endogenous E3 ligase for CIP2A, and PF enhances the interaction between VHL and CIP2A, promoting the ubiquitin‒proteasome degradation of CIP2A, thereby inhibiting melanoma growth and metastasis. Overall, this study not only suggests PF's potential in treating melanoma and its brain metastases but also highlights CIP2A degradation as a therapeutic strategy for melanoma.
100 项与 五氟利多 相关的药物交易
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 精神分裂症 | 中国 | - |
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适应症
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N/A | - | 繭憲淵構選醖襯築鏇糧(餘膚繭遞鬱鑰積餘襯製) = 蓋範壓鹽餘窪網夢範糧 膚蓋鹽窪顧鑰繭網鹽鏇 (鬱鏇築築鹹範膚築憲鏇 ) 更多 | - | 2017-07-01 |
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