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DRUG CLASS:

PLK1 inhibitor

13d
Rigosertib Plus Pembrolizumab in Treating Patients With Unresectable/Metastatic Melanoma Refractory to PD-1 Inhibitors (clinicaltrials.gov)
P2, N=7, Active, not recruiting, Vanderbilt-Ingram Cancer Center | Suspended --> Active, not recruiting | N=29 --> 7
Enrollment closed • Enrollment change • Checkpoint inhibition
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BRAF (B-raf proto-oncogene)
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BRAF mutation • BRAF V600
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Keytruda (pembrolizumab) • Estybon (rigosertib)
18d
Identification of Polo-like kinase-1 (PLK-1) inhibitors from Centella asiatica (Gotu Kola) using UHPLC and in-silico approaches. (PubMed, Nat Prod Res)
The 90% ethanol-aqueous extract of C. asiatica whole plant, which was prepared at room temperature, contained ten bioactive compounds including rutin, quercetin, kaempferol, chlorogenic acid, fisetin, apigenin, asiatic acid, fumaric acid, betulinic acid and ursolic acid identified by UHPLC method. As our findings, rutin was identified as a promising PLK-1 inhibitor that exhibited significant docking score -13.07 and high stability within the binding pockets of PLK-1 protein as compared to control drug onvansertib. Furthermore, experimental validation is urgently needed for future translational research to develop rutin as potent PLK-1 inhibitor for treating cancer.
Journal
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PLK1 (Polo Like Kinase 1)
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onvansertib (PCM-075) • chlorogenic acid
1m
The efferocytosis-related genes of SLC26A6, TYRO3, and PDK4 have been identified as predictors of prognosis in hepatocellular carcinoma and are associated with the immune status. (PubMed, Int J Med Sci)
There were 61 drugs with significant differences in IC50 between the high and low risk groups, such as BI.2536 and PD-173074...We identified three prognostic genes associated with efferocytosis in HCC and integrated them into a risk prognostic model. These genes not only serve as signatures for predicting HCC prognosis but also offer insights into the treatment of HCC.
Journal • IO biomarker
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CD4 (CD4 Molecule) • NUTM2A (NUT Family Member 2A) • PDK4 (Pyruvate Dehydrogenase Kinase 4) • MIR203A (MicroRNA 203a)
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BI2536
1m
BAL0891 in Patients With Advanced Solid Tumors or Relapsed or Refractory Acute Myeloid Leukemia (clinicaltrials.gov)
P1, N=260, Recruiting, SillaJen, Inc. | Trial completion date: Mar 2026 --> Dec 2026 | Trial primary completion date: Jul 2025 --> Dec 2026
Trial completion date • Trial primary completion date
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HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PGR (Progesterone receptor)
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HER-2 positive • HER-2 negative
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paclitaxel • Tevimbra (tislelizumab-jsgr) • BAL0891
2ms
Integrated single-cell and spatial mapping coupled with machine learning unveils core stemness landscapes and regulatory drivers in triple-negative breast cancer. (PubMed, Discov Oncol)
Our predictive model offers a novel perspective on the stemness landscape of TNBC. These core genes play key roles in maintaining stemness and also serve as potential molecular targets for personalized therapies aimed at TNBC stem-like cells.
Journal
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NOTCH1 (Notch 1)
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BI2536
2ms
Integrating bulk and single cell RNA sequencing to predict the potential therapeutic efficacy of DLX5 in hypopharyngeal squamous cell carcinoma. (PubMed, Eur J Med Res)
Through bioinformatics analysis, it was discovered that DLX5 exerts an oncogenic role in HPSCC through co-amplification with TP63 and activation of the MAPK signaling pathway, with functional assays further confirming its promotion of malignant phenotypes. High expression of DLX5 correlates positively with immunosuppressive cells, such as M2 macrophages, and negatively with antitumor CD8+ T cells, indicating an association with an immunosuppressive microenvironment. These findings highlight DLX5 as a key determinant of poor prognosis in HPSCC.
Journal
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CD8 (cluster of differentiation 8) • CD4 (CD4 Molecule) • TP63 (Tumor protein 63) • DLX5 (Distal-Less Homeobox 5)
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BI2536
2ms
GPI inactivation mediates pentose phosphate pathway flux switch-on inducing temozolomide resistance in glioma stem cell. (PubMed, Cancer Lett)
Targeting the ATM/PLK1/GPI axis through combinational treatment with rigosertib may therefore represent a therapeutic strategy. Moreover, PLK1 expression and GPI pT215 levels may serve as potential candidate markers for GBM. Collectively, activation of the ATM/PLK1/GPI axis plays a critical role in regulating PPP flux and TMZ resistance in GSCs.
Journal
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PLK1 (Polo Like Kinase 1) • GPI (Glucose-6-Phosphate Isomerase)
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temozolomide • Estybon (rigosertib)
2ms
Synergistic Anticancer Effects of the PLK1 Inhibitor BI-2536 and β-Glucan in Colon and Gastric Cancer Cells. (PubMed, Anticancer Res)
BI-2536 in combination with β-glucan exhibits synergistic anticancer effects in vitro, suggesting a promising strategy for treating colon and gastric cancers.
Journal
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PLK1 (Polo Like Kinase 1)
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BI2536
3ms
Onvansertib + Paclitaxel In TNBC (clinicaltrials.gov)
P1/2, N=50, Active, not recruiting, Antonio Giordano, MD | Trial primary completion date: Feb 2026 --> Dec 2026
Trial primary completion date
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HER-2 (Human epidermal growth factor receptor 2)
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HER-2 negative
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paclitaxel • onvansertib (PCM-075)
3ms
Selective Inhibition of Protein Kinase D2 Activity Reduces Human Neutrophil Survival. (PubMed, Anticancer Res)
PKD2 plays a crucial role in human neutrophil survival. Minimizing PKD2 inhibition during small-molecule drug design could be essential to reduce the risk of neutropenia in patients under anti-cancer treatment.
Journal
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PKD2 (Polycystin 2)
3ms
Plasma proteome mendelian randomization and network pharmacology reveal therapeutic targets for thyroid disorders. (PubMed, Mol Cell Endocrinol)
By synergizing genetic epidemiology with network pharmacology, this study delineates shared genetic architecture among thyroid disorders and nominates seven high-confidence targets with therapeutic potential. The integrative framework advances precision medicine by bridging causal plasma protein identification, mechanistic pathway mapping, and drug repurposing, offering a blueprint for multi-omics-driven drug discovery in endocrine pathologies.
Journal
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FGF19 (Fibroblast growth factor 19) • CDH1 (Cadherin 1) • RPS6KA6 (Ribosomal Protein S6 Kinase A6)
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BI2536
3ms
Artificial Intelligence Driven Virtual Screening and Molecular Docking Approaches Identified LIFR, BTG2, EPHX2, and PAK3 as Targets and BI-2536, AP-24534, and AZ-628 as Repurposed Drugs for PDAC. (PubMed, IEEE Trans Comput Biol Bioinform)
The pharmacokinetics study strengthened our results that the identified drugs can be used as a therapeutic for PDAC as they obey Lipinski's rule. In conclusion, identified genes can act as prognostic markers, and drugs could be used as potential therapeutics for PDAC.
Journal
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LIFR (LIF Receptor Subunit Alpha) • BTG2 (BTG Anti-Proliferation Factor 2)
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Iclusig (ponatinib) • AZ 628 • BI2536