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DRUG:

serdemetan (JNJ-26854165)

i
Other names: JNJ-26854165
Associations
Trials
Company:
J&J
Drug class:
MDM2 inhibitor
Associations
Trials
3ms
p27 Cell Cycle Inhibitor and Survival in Luminal-Type Breast Cancer: Gene Ontology, Machine Learning, and Drug Screening Analysis. (PubMed, J Breast Cancer)
The integration of ML and bioinformatic analyses of p27 has the potential to enhance risk stratification and facilitate personalized treatment strategies for patients with breast cancer.
Journal • Machine learning
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ER (Estrogen receptor) • PGR (Progesterone receptor) • CD8 (cluster of differentiation 8) • CDKN2B (Cyclin Dependent Kinase Inhibitor 2B) • CDKN1A (Cyclin-dependent kinase inhibitor 1A) • CDKN1B (Cyclin dependent kinase inhibitor 1B)
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CDKN1B expression
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serdemetan (JNJ-26854165) • voxtalisib (SAR245409)
3ms
Analysis of the role of CHPF in colorectal cancer tumorigenesis and immunotherapy based on bioinformatics and experiments. (PubMed, Discov Oncol)
CHPF could promote the proliferation and migration of CRC cells and lead to poor prognosis, possibly through wnt pathways as well as changes in TME. Patients with high expression of CHPF had poor efficacy in immunotherapy, which might be related to Tregs cell infiltration. Above all, it might offer more reliable guidance for future immunotherapy.
Journal • Tumor mutational burden • MSi-H Biomarker • PD(L)-1 Biomarker • IO biomarker
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TMB (Tumor Mutational Burden) • MSI (Microsatellite instability) • PD-1 (Programmed cell death 1) • CHPF (Chondroitin Polymerizing Factor)
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MSI-H/dMMR
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Mekinist (trametinib) • serdemetan (JNJ-26854165) • telatinib (BAY 57- 9352)
over2years
A novel immune-related epigenetic signature based on the transcriptome for predicting the prognosis and therapeutic response of patients with diffuse large B-cell lymphoma. (PubMed, Clin Immunol)
According to the prediction, EC1 was more sensitive to vorinostat, serdemetan and navitoclax. However, ruxolitinib, cytarabine and CP466722 were more suitable treatments for EC2. The novel immune-related epigenetic signature exhibits promising clinical predictive value for diffuse large B-cell lymphoma (DLBCL), particularly for guiding epigenetic therapeutic regimens. R-CHOP (rituximab, cyclophosphamide, doxorubicin, vincristine, and prednisone) based combination treatment regimens are suggested.
Journal
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TP53 (Tumor protein P53) • MYD88 (MYD88 Innate Immune Signal Transduction Adaptor) • CD8 (cluster of differentiation 8) • KMT2D (Lysine Methyltransferase 2D) • B2M (Beta-2-microglobulin) • CD70 (CD70 Molecule)
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KMT2D mutation • EZH2 mutation
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Rituxan (rituximab) • cytarabine • doxorubicin hydrochloride • Jakafi (ruxolitinib) • cyclophosphamide • vincristine • Zolinza (vorinostat) • navitoclax (ABT 263) • serdemetan (JNJ-26854165)
almost3years
MDM2 inhibition as a non-hormone dependent radiosensitizing strategy in p53 wild-type breast cancer models (AACR 2022)
In vivo efficacy of combination therapy was evaluated with CAL-51 and CAL-51 p53 CRISPR xenograft models. An MDM2 inhibitor (JNJ-26854165) was nominated as an effective drug in treatment for RT-resistant BC cell lines (R2 = 0.43, p value 10μm)... These results demonstrate the combination of RT and MDM2 inhibition may be an effective therapeutic strategy in patients with p53-wild type breast cancer, regardless of hormone receptor status.
Preclinical
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ER (Estrogen receptor) • MDM2 (E3 ubiquitin protein ligase)
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TP53 mutation • ER positive • TP53 wild-type • TP53 expression • MDM2 overexpression
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navtemadlin (KRT-232) • alrizomadlin (APG-115) • serdemetan (JNJ-26854165)
over3years
Gain-of-Function Mutant TP53 R248Q Overexpressed in Epithelial Ovarian Carcinoma Alters AKT-Dependent Regulation of Intercellular Trafficking in Responses to EGFR/MDM2 Inhibitor. (PubMed, Int J Mol Sci)
Previously, we have demonstrated that the combined inhibition of EGFR and MDM2-p53 pathways, by gefitinib and JNJ-26854165, exerts a strong synergistic lethal effect on HGSOC cells. Our findings suggested that the R248Q mutation of p53 in HGSOC caused significant changes in signaling protein function and trafficking, under EGFR/MDM2-targeted inhibition. Such knowledge could help to advance our understanding of the role of mutant p53 in ovarian carcinoma and to improve the prognosis of patients receiving EGFR/MDM2-targeted therapies.
Journal
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EGFR (Epidermal growth factor receptor) • TP53 (Tumor protein P53) • AKT1 (V-akt murine thymoma viral oncogene homolog 1) • MDM2 (E3 ubiquitin protein ligase)
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TP53 mutation • EGFR mutation • EGFR overexpression • TP53 overexpression • AKT1 overexpression • TP53 R248Q
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gefitinib • serdemetan (JNJ-26854165)
almost4years
[VIRTUAL] The role of MDM2 inhibition in the radiosensitization of ER+ breast cancers (AACR 2021)
yH2AX immunofluorescence was used to measure dsDNA breaks.Results​: A MDM2 inhibitor (JNJ-26854165) was nominated as an effective drug in treatment for RT-resistant BC cell lines (R2​ = 0.43, p-value <0.01) in our novel radiosensitizer screen...AMG-232 and RT combined led to an increase in apoptosis compared to RT alone in ER+ p53 WT cells but not p53 MT cells...​G1 cell cycle arrest was a secondary effect of MDM2 inhibition and radiation. Experiments investigating the role of dsDNA breaks in radiosensitization are ongoing.Conclusions​: Our novel radiosensitizer screen identifies MDM2 as a potential mediator of radioresistance in ER+ BC in a p53-dependent manner and suggests that MDM2 targeting concurrent with RT may represent a tractable clinical strategy in women with locally advanced ER+, p53 WT BC.
PARP Biomarker
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ER (Estrogen receptor)
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TP53 mutation • ER positive • TP53 expression • MDM2 overexpression
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navtemadlin (KRT-232) • serdemetan (JNJ-26854165)
over4years
EPHA5 mutation predicts the durable clinical benefit of immune checkpoint inhibitors in patients with lung adenocarcinoma. (PubMed, Cancer Gene Ther)
In addition, patients with EPHA5 mutations tended to be more sensitive to certain targeted molecular inhibitors, including serdemetan, lox2, and PF1-1. Collectively, our results suggest that identifying mutations in the EPHA5 gene may provide insight into the genome-wide mutational burden and may serve as a biomarker to predict the immune response of patients with LUAD.
Clinical • Journal • Checkpoint inhibition • Tumor Mutational Burden
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TMB (Tumor Mutational Burden)
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TILs
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serdemetan (JNJ-26854165)
over4years
[VIRTUAL] A radiosensitizer screen identifies a novel role for MDM2 inhibition in the radiosensitization of ER+ breast cancers in a p53 dependent manner (AACR-II 2020)
AlamarBlue was used to determine IC50 values of the MDM2 inhibitor AMG-232. Western blot analysis of Cleaved PARP was used to measure apoptosis and Cyclins A and E to measure cell cycle progression. Our radiosensitizer screen nominated the MDM2 inhibitor (JNJ-26854165) as one of the most effective drugs in treating RT-resistant BC cell lines (R2= 0.43, p-value <0.01)... Our novel radiosensitizer screen identifies MDM2 as a potential mediator of radioresistance in ER+ BC. Additionally, MDM2 inhibition confers radiosensitization in a p53 dependent manner in ER+ BC and may represent a tractable clinical strategy in women with p53 WT BC.
PARP Biomarker
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ER (Estrogen receptor) • MDM2 (E3 ubiquitin protein ligase)
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TP53 mutation • ER positive • TP53 expression
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navtemadlin (KRT-232) • serdemetan (JNJ-26854165)