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DRUG CLASS:

DRD3 antagonist

7d
A PET Study of ENX-104 in Healthy Volunteers (clinicaltrials.gov)
P1, N=10, Completed, Engrail Therapeutics INC
New P1 trial
7d
New P1 trial
15d
Drug Repurposing Screen Identifies Pimozide as a ROS-Inducing Therapy With Anti-Tumor Efficacy in HNSCC PDX Models. (PubMed, Cancer Sci)
Notably, pimozide exhibited anti-tumor effects as a monotherapy and in combination with paclitaxel at clinically relevant doses. While tumor volume reduction in the combination group was not statistically greater than that in the monotherapy group, fluorescence immunohistochemistry revealed a marked decrease in undifferentiated tumor cells, indicating enhanced therapeutic effects of combination treatment. Taken together, these findings indicate that pimozide is a promising candidate for repurposing as a novel therapeutic agent against HNSCC.
Journal
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STAT3 (Signal Transducer And Activator Of Transcription 3) • DRD2 (Dopamine Receptor D2) • EGR1 (Early Growth Response 1)
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paclitaxel
16d
Enrollment change
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chlorpromazine
1m
Role of Ubiquitin-specific Protease 1 in the Pathogenesis and Treatment of Adult T-Cell Leukemia. (PubMed, Anticancer Res)
Our study supports the clinical potential of USP1 inhibitors as a novel therapy for ATL.
Journal
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MYC (V-myc avian myelocytomatosis viral oncogene homolog) • LDHA (Lactate dehydrogenase A) • CTNNB1 (Catenin (cadherin-associated protein), beta 1) • PLK1 (Polo Like Kinase 1) • USP1 (Ubiquitin Specific Peptidase 1)
1m
Antipsychotic Chlorpromazine Suppresses STAT5 Signaling, Overcomes Resistance Mediated by the Gatekeeper Mutation FLT3-ITD/F691L, and Synergizes with Quizartinib in FLT3-ITD-Positive Cells. (PubMed, Curr Issues Mol Biol)
Although FLT3 tyrosine kinase inhibitors (TKIs), such as quizartinib (Quiz) and gilteritinib, have improved clinical outcomes, secondary TKD mutations, particularly the gatekeeper mutation F691L, confer significant resistance. Expression of constitutively active STAT5 partially rescued CPZ-induced growth inhibition. These findings suggest that STAT5 suppression is a key mechanism of CPZ's antileukemic activity and support its potential as a therapeutic strategy for FLT3-ITD-positive AML.
Journal
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FLT3 (Fms-related tyrosine kinase 3) • STAT5A (Signal Transducer And Activator Of Transcription 5A)
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FLT3-ITD mutation • FLT3 mutation
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Xospata (gilteritinib) • Vanflyta (quizartinib) • chlorpromazine
1m
Bridging clinical insight and laboratory model in high-grade serous ovarian carcinoma (HGSOC) using DNA sequencing-based profiling of TP53. (PubMed, Oncoscience)
In this study, drug repurposing agent's metformin, chlorpromazine (CPZ) alone and combine were tested on both clinical and laboratory ovarian cancer samples to evaluate on hemocytometer and clonogenic assay for dead cell and proliferation respectively. The resulting data were analyzed to achieve successfully known target region and worked as a bridge between clinical and laboratory model. The insights gained from this study not only validate OVCAR3 as a representative model for HGSOC but also provide a foundation for developing targeted therapeutic strategies.
Journal
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TP53 (Tumor protein P53)
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TP53 wild-type
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metformin • chlorpromazine
3ms
Transcriptomic and proteomic analyses of SH-SY5Y neuroblastoma cells treated with amisulpride. (PubMed, Acta Neuropsychiatr)
Our data reveal novel insights into the role of amisulpride in modulating the differential expression of genes and proteins. These findings, which involve genes/proteins related to AP-1 transcription factor family gene regulation, cytoskeleton, histone binding activity, the intracellular trafficking of receptors and endocytosis of a variety of macromolecules, and nuclear localization signal, are particularly significant as they shed light on the molecular underpinnings of the clinical efficacy of amisulpride and the pathogenesis of schizophrenia.
Journal
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CLTC (Clathrin Heavy Chain) • ACTG1 (Actin Gamma 1)
4ms
The associations of suicidal ideation with psychopathology and inflammatory cytokines in patients with chronic schizophrenia. (PubMed, BMC Psychiatry)
There was higher overall risk of SI in patients with chronic schizophrenia. SI might be associated with psychotic symptoms, depression, insomnia, medication side effects, and increased levels of inflammatory cytokines. In clinical practice, doctors should take prompt preventive measures in patients combining suicidal risk factors.
Journal
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IL6 (Interleukin 6) • TNFA (Tumor Necrosis Factor-Alpha) • IL17A (Interleukin 17A) • IL1B (Interleukin 1, beta)
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chlorpromazine
4ms
Clathrin Light Chain B Drives Hepatocellular Carcinoma Progression Through Dual Mechanisms: Small Extracellular Vesicle-Mediated Angiogenesis and the NF-κB-PCLAF Signaling Axis. (PubMed, Adv Sci (Weinh))
In patient-derived xenograft (PDX) models, combined therapy of clathrin inhibitor (chlorpromazine) or SH3KBP1 silencing with sorafenib suppresses tumor growth and reduces microvascular density. This study demonstrates that CLTB promotes HCC progression through the NF-κB-PCLAF signaling axis and sEV-mediated vascular remodeling, providing a mechanistic foundation for developing combination therapies targeting CLTB.
Journal
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PCNA (Proliferating cell nuclear antigen) • PCLAF (PCNA Clamp Associated Factor)
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sorafenib • chlorpromazine
5ms
The effects of dopamine receptor antagonist and partial agonist antipsychotics on the glutamatergic system: double-blind, randomised, placebo-controlled 1H-MRS cross-over study in healthy volunteers. (PubMed, Br J Psychiatry)
One week of aripiprazole administration in healthy participants altered brain Glx levels as compared with placebo administration. These findings provide novel insights into the relationship between antipsychotic treatment and brain metabolites in a healthy participant cohort.
Journal
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DRD2 (Dopamine Receptor D2)
5ms
Substance Misuse To Psychosis for Stimulants (clinicaltrials.gov)
P2/3, N=165, Completed, The University of Hong Kong | Recruiting --> Completed | N=240 --> 165
Trial completion • Enrollment change