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DRUG CLASS:

DRD2 antagonist

1m
A Novel DRD2 Antagonist, SD2-2305, Exerts Anticancer Effects in Colorectal Cancer Cells through G1 Arrest and Caspase-Dependent Apoptosis. (PubMed, Biomol Ther (Seoul))
While key survival pathways (JAK2/STAT3, PI3K/Akt, and MAPK) remained relatively unaffected, SD2-2305 modulated growth factor receptors post-transcriptionally, decreasing HER2/ErbB2 and increasing TGF-beta receptor 1 expression. Collectively, these findings demonstrate that the DRD2 antagonist SD2-2305 exerts potent anticancer effects through the induction of cell cycle arrest and apoptosis, and suggest that the anticancer activity of SD2-2305 is associated with coordinated modulation of growth factor receptor signaling and cell-cycle regulators in CRC cells.
Journal • IO biomarker
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HER-2 (Human epidermal growth factor receptor 2) • BCL2 (B-cell CLL/lymphoma 2) • JAK2 (Janus kinase 2) • CASP3 (Caspase 3) • CCNA2 (Cyclin A2) • CDK2 (Cyclin-dependent kinase 2) • TGFB1 (Transforming Growth Factor Beta 1) • CASP9 (Caspase 9) • CASP7 (Caspase 7) • CDK1 (Cyclin-dependent kinase 1) • CDKN1A (Cyclin-dependent kinase inhibitor 1A) • ANXA5 (Annexin A5) • DRD2 (Dopamine Receptor D2)
1m
Enrollment open • Trial initiation date • Head-to-Head
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chlorpromazine
2ms
Symptomatic hyperprolactinemia mimicking pituitary pathology in a child with Landau-Kleffner syndrome, autism spectrum disorder, and intellectual disability: a case report. (PubMed, J Med Case Rep)
The case shows the significance of following prolactin levels in children who are on risperidone therapy particularly those who are non-verbal or those who cannot communicate any discomfort. Clinicians are to remember that risperidone leads to hyperprolactinemia which can simulate pituitary malfunctions. Early identification, educating caregivers, and substitution of prolactin-stimulating drugs with prolactin-sparing ones like olanzapine will allow avoiding unnecessary investigations and enhancing the clinical and family outcomes.
Journal
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PRL (Prolactin)
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olanzapine
2ms
Characterization of SF3B1 role in prolactin-secreting pituitary tumors. (PubMed, Endocr Relat Cancer)
Aims of the study were to: 1) test the effects of SF3B1 inhibitor pladienolide B in tumoral lactotroph cells expressing wild-type or mutated SF3B1R625H; 2) investigate SF3B1 impact on tumoral cells responsiveness to DRD2 agonist cabergoline...Indeed, SF3B1 inhibitor pladienolide B exerted antitumoral actions in PRL-PitNET cells bearing wild-type or mutated SF3B1. Moreover, both SF3B1R625H overexpression and SF3B1 genetic silencing reduced DRD2 expression and signaling.
Journal
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SF3B1 (Splicing Factor 3b Subunit 1) • CCND3 (Cyclin D3) • DRD2 (Dopamine Receptor D2)
2ms
Efficacy and Mechanism of IPSRT for Bipolar II Disorder (clinicaltrials.gov)
P2, N=216, Not yet recruiting, First Affiliated Hospital of Zhejiang University
New P2 trial
2ms
BARD1 phase separation orchestrates a repair hub by enriching XRCC5 to drive chemoresistance in glioma. (PubMed, Life Sci)
Through structure-based virtual screening, our results suggest that Ziprasidone and Apomorphine may disrupt the BARD1-XRCC5 interaction...Our findings unveil a novel LLPS-mediated mechanism by which BARD1 confers TMZ resistance in GBM, positioning it as a prognostic marker and a therapeutic target. Targeting the BARD1-XRCC5 axis presents a promising strategy to overcome chemoresistance.
Journal • BRCA Biomarker
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BRCA1 (Breast cancer 1, early onset) • BARD1 (BRCA1 Associated RING Domain 1)
2ms
Beyond inhibition: harnessing the DRD2-VEGF-A feedback loop for precision anti-angiogenesis therapy in cancer. (PubMed, Front Oncol)
By utilizing FDA-approved DRD2 agonists as functional probes, clinicians can implement a dopaminergic challenge to identify windows of maximal VEGF-dependency via dynamic imaging. This approach transforms anti-angiogenic interventions from empirical into a precision theranostic platform, enabling real-time assessment of tumor VEGF-dependency and rational treatment selection that maximizes efficacy while minimizing toxicity.
Journal
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DRD2 (Dopamine Receptor D2)
2ms
Risperidone regulates the expression of schizophrenia-related genes in the forebrain of adult male mice. (PubMed, Front Mol Neurosci)
Together, these findings indicate that acute treatment with risperidone in male mice exerts pronounced molecular effects in medial and ventral forebrain regions with high oligodendrocyte and glial cell abundance. Moreover, enrichment analysis points to a molecular convergence between risperidone-induced transcription and genetic pathways implicated in schizophrenia.
Preclinical • Journal
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OLIG2 (Oligodendrocyte Transcription Factor 2)
2ms
NCI-2018-02438: Haloperidol and Lorazepam in Controlling Symptoms of Persistent Agitated Delirium in Patients With Advanced Cancer Undergoing Palliative Care (clinicaltrials.gov)
P2/3, N=110, Active, not recruiting, M.D. Anderson Cancer Center | Trial completion date: Dec 2026 --> Dec 2028 | Trial primary completion date: Feb 2026 --> Dec 2028
Trial completion date • Trial primary completion date
2ms
New P3 trial
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olanzapine