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DRUG CLASS:

DRD4 antagonist

3d
Chlorpromazine inhibits EAG1 channels by altering the interdomain coupling. (PubMed, Biophys J)
This further suggests that if chlorpromazine binding alters coupling between the PAS/CNBH domain ring, VSD and pore, as predicted by the network analysis, these alterations occur at potential more depolarized than the ones eliciting the Cole-Moore shift. Taken together, our study provides an insight into the allosteric pathways of EAG1 channel regulation by small molecule PAS domain binders.
Journal
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SPR (Sepiapterin Reductase)
5d
Chlorpromazine activates cGAS-STING signaling and reprograms the immune response in glioblastoma. (PubMed, Front Immunol)
We demonstrate that CPZ, alone or in combination with temozolomide (TMZ), the current standard of care, activates the cGAS-STING signaling pathway, thus promoting anti-tumor immune responses. This study uncovers that CPZ exerts a previously unrecognized anti-cancer immunomodulatory activity, remodeling the immune microenvironment and enhancing the anti-tumor immune response. By overcoming TMZ resistance, CPZ not only exerts a direct anti-neoplastic effect, but also sensitizes GBM cells to standard therapy.
Journal • PD(L)-1 Biomarker • IO biomarker
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PD-L1 (Programmed death ligand 1)
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PD-L1 expression
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temozolomide
1m
C-Cog in Early Course Schizophrenia Study (clinicaltrials.gov)
P4, N=1, Terminated, University of Miami | N=60 --> 1
Enrollment change
1m
New trial
4ms
Enrollment change
4ms
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)
5ms
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
7ms
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)
7ms
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
8ms
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
8ms
Toward pharmacologic therapy for glioblastoma: Identifying inhibitors of very long-chain acyl-CoA synthetase 3 (ACSVL3). (PubMed, bioRxiv)
These included drugs triflupromazine, phenazopyridine, chlorpromazine, emodin, and perphenazine which are approved for treating other conditions. Although secondary screening will likely exclude many or all of these, our findings support the notion that we have developed a viable method for detecting potential ACSVL3 inhibitors. Further characterization may reveal candidate pharmacologic agents for treatment of GBM and other cancers.
Journal
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ACSL3 (Acyl-CoA Synthetase Long Chain Family Member 3)
8ms
MainRexult: Real-life Assessment of Abilify Maintena + Rexult in Schizophrenia (clinicaltrials.gov)
P=N/A, N=10, Recruiting, The University of Hong Kong | Trial completion date: Jun 2025 --> Jan 2026 | Trial primary completion date: Dec 2024 --> Oct 2025
Trial completion date • Trial primary completion date