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DRUG CLASS:

DRD2 antagonist

1d
Pituitary Apoplexy With Marked Hyperprolactinemia in a 19-Year-Old Woman: A Case Report of Diagnostic Challenges and Surgical Management. (PubMed, Cureus)
She was initially managed conservatively with stress-dose hydrocortisone and low-dose cabergoline under close clinical and visual monitoring...Postoperatively, she developed cerebrospinal fluid rhinorrhea that resolved with lumbar drainage, as well as transient diabetes insipidus treated with desmopressin...In hemorrhagic sellar lesions, markedly elevated prolactin may reflect either a prolactinoma or stalk effect; a rapid postoperative prolactin decline supports stalk compression as the dominant mechanism. Close observation during conservative management is essential, and clinical deterioration should prompt timely surgical decompression to optimize neurological and endocrine outcomes.
Journal
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PRL (Prolactin)
1d
Recurrent nasal bleed as initial presenting complaint: a rare complication of giant prolactinoma in a 39-year-old. (PubMed, Ann Med Surg (Lond))
The objective of this report is to show the aggressive invasive nature of giant prolactinoma with rare clinical presentation of recurrent nasal bleeds and the use of cabergoline in the successful management of patients having severe symptoms of extreme headaches and bitemporal hemianopia along with intracranial invasion of tumor...In conclusion, managing giant prolactinomas requires a multidisciplinary approach, with dopamine agonists as the cornerstone of treatment. Individualized strategies, adjunctive therapies, and regular monitoring ensure comprehensive care.
Journal
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PRL (Prolactin)
1d
Risperidone Treatment in Children and Adolescents: A Naturalistic Observational Study of Metabolic, Cardiac, and Clinical Outcomes. (PubMed, J Child Adolesc Psychopharmacol)
Within 6 months of initiation, risperidone use in drug-naive pediatric patients was associated with increased weight and abdominal adiposity, early prolactin elevation, HDL reduction, and clinical improvement. Waist circumference showed a strong dose-dependent association and should be routinely monitored along with metabolic and endocrine parameters.
Clinical data • Observational data • Journal
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PRL (Prolactin)
4d
Trial completion • Head-to-Head
6d
Application of HepaRG mono- and HepaRG:THP-1 cocultures as immune responsive hepatotoxicity models. (PubMed, Toxicology)
Finally, models were exposed to iDILI drugs diclofenac (200µM), trovafloxacin (100µM) and clozapine (75µM), whereafter cell viability and cytotoxicity was measured. The iDILI drugs induced a synergistic decrease in viability in inflamed HepaRG mono- and cocultures, which showcases predictivity of the model for iDILI hepatotoxic reactions. In conclusion, HepaRG cells in monoculture and in coculture with THP-1 macrophages showed similar inflammation-driven effects on the selected endpoints, which shows that both models are promising tools to evaluate inflammation-driven effects on toxicokinetic and toxicodynamic endpoints.
Journal
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IFNG (Interferon, gamma) • IL6 (Interleukin 6) • TNFA (Tumor Necrosis Factor-Alpha) • CXCL8 (Chemokine (C-X-C motif) ligand 8) • IL1B (Interleukin 1, beta)
6d
PSY-PGx: Clinical Study Evaluating Pharmacogenomics-informed Pharmacotherapy Versus Dosing as Usual in Psychiatric Disorders (clinicaltrials.gov)
P=N/A, N=1470, Recruiting, Maastricht University Medical Center | Not yet recruiting --> Recruiting | N=820 --> 1470
Enrollment open • Enrollment change
6d
Fatty acid oxidation drives acetyl-CoA-dependent H3K9ac reprogramming to promote adaptive resistance to BRAFV600E inhibition in thyroid cancer. (PubMed, Cell Death Dis)
Through integrated transcriptomic and metabolomic analyses, we demonstrate that BRAFi by vemurafenib (PLX4032) significantly enhances FAO in thyroid cancer cells. The pharmacological inhibition of FAO via thioridazine (Thio) synergizes with BRAFi to suppress tumor growth in vitro, in vivo and in a patient-derived organoid...Consistently, functional studies confirm RUNX1's oncogenic role, as its knockdown reduces cell proliferation, migration, and invasion. In conclusion, our work reveals a metabolic-epigenetic axis underlying adaptive response to BRAFi and identifies RUNX1 as a novel oncogene in thyroid cancer.
Journal
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RUNX1 (RUNX Family Transcription Factor 1)
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BRAF V600E
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Zelboraf (vemurafenib)
7d
Co-secreting pituitary adenomas in acromegaly: Classification, diagnosis, and treatment strategies. (PubMed, Vitam Horm)
Additionally, we discuss treatment strategies, including surgical and medical approaches, highlighting the impact of the treatment with cabergoline and somatostatin receptor ligands (SRLs) in biochemical control. The predictors of surgical and medical treatment resistance, including Knosp grade, tumor size, and baseline hormone levels, are also addressed. Understanding the unique behavior of these tumors is crucial for optimizing treatment strategies and improving patient outcomes.
Review • Journal
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SSTR (Somatostatin Receptor)
7d
SLIM: Shortened LSD Intervention for Major Depressive Disorder (clinicaltrials.gov)
P1, N=10, Not yet recruiting, Johns Hopkins University
New P1 trial
11d
Pharmacologic targeting of the dopamine D2 receptor impacts the efficacy of immune checkpoint blockade in melanoma. (PubMed, J Immunother Cancer)
These findings demonstrate that pharmacologic modulation of D2R impacts the efficacy of immune checkpoint blockade in murine melanoma and raise the possibility of using FDA-approved D2R targeting therapies as cotherapeutics to overcome ICI resistance in patients with advanced melanoma.
Journal • Checkpoint inhibition • IO biomarker
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CD8 (cluster of differentiation 8) • DRD2 (Dopamine Receptor D2)
11d
circOMA1 delivered by exosomes regulates DRD2‑mediated prolactinoma resistance. (PubMed, Int J Mol Med)
Among pituitary adenomas, prolactin‑secreting pituitary neuroendocrine tumours (PRL‑PitNETs) are unique in that pharmacotherapy, specifically cabergoline (CAB), can be used as a first‑line treatment, and it is the recommended therapeutic option...Plasma exosomal circOMA1 levels were significantly elevated in PRL‑PitNET patients preoperatively. These findings established circOMA1 as a key mediator of CAB resistance and a potential prognostic indicator in patients with a PRL‑PitNET.
Journal
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DRD2 (Dopamine Receptor D2) • MIR145 (MicroRNA 145)
12d
Cannabidiol (CBD) for Clozapine Refractory Schizophrenia (CanCloz) (ACTRN12622001112752)
P2, N=88, Terminated, The University of Queensland | Recruiting --> Terminated
Trial termination