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DRUG:

refametinib (BAY86-9766)

i
Other names: BAY86-9766, BAY869766, AR 119, AR-119, AR119, BAY-86-9766, BAY 869766, RDEA 119, RDEA-119, RDEA119, AY-869766, AY 869766, AY869766, VRX-119, VRX 119, VRX119
Company:
AstraZeneca
Drug class:
MEK inhibitor, ERK2 inhibitor
21d
Glucokinase Regulatory Protein (GCKR) Links Metabolic Reprogramming With Immune Exclusion: Insights From a Pan-Cancer Analysis and Gastric Cancer Validation. (PubMed, Hum Mutat)
Clinically, low GCKR expression predicted poorer survival and reduced immunotherapy benefit, while higher expression indicated selective sensitivity to MEK inhibitors including refametinib and PD0325901. These findings define GCKR as both a mutation- and expression-driven biomarker that connects metabolic regulation with immune remodeling, offering translational value for prognosis and precision therapy in gastric cancer.
Journal • BRCA Biomarker • IO biomarker • Pan tumor
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BRCA (Breast cancer early onset)
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Gomekli (mirdametinib) • refametinib (BAY86-9766)
4ms
Identification of key ferroptosis-related genes associated with the development of gastric cancer: Prognostic models, molecular mechanisms and potential treatment strategies. (PubMed, Oncol Lett)
Finally, using the Genomics of Drug Sensitivity in Cancer and Cancer Therapeutics Response Portal databases, potential drugs [(5Z)-7-oxozeaenol, selumetinib, RDEA119, AZ628, dabrafenib and trametinib] were identified based on the aforementioned seven key carcinogenic genes, focusing on those that targeted multiple genes. In conclusion, the present study identified 14 key ferroptosis-related genes, and seven key carcinogenic genes, which represent promising novel molecular targets for the prognosis and treatment of GC.
Journal
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GJA1 (Gap Junction Protein Alpha 1) • AKR1C2 (Aldo-Keto Reductase Family 1 Member C2) • GABARAP (GABA Type A Receptor-Associated Protein) • MIR484 (MicroRNA 484) • NOX4 (NADPH Oxidase 4) • GABARAPL2 (GABA Type A Receptor Associated Protein Like 2) • MIR675 (MicroRNA 675) • NOX5 (NADPH Oxidase 5)
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Mekinist (trametinib) • Tafinlar (dabrafenib) • Koselugo (selumetinib) • refametinib (BAY86-9766) • AZ 628
8ms
Targeting the phosphatidylinositol-3-kinase (PI3K) and mitogen activated protein kinase (MAPK) signalling pathways to enhance chemoradiotherapy in locally advanced rectal cancer. (PubMed, Cancer Treat Res Commun)
A panel of colorectal cancer (CRC) cell lines (n = 10) with varying PI3K and MAPK mutational backgrounds were treated with combinations of 5-Flourouracil (5-FU), radiation, the PI3K inhibitor copanlisib, and/or the MEK inhibitor refametinib, and their effects on proliferation in vitro were measured...Our results suggest that activation of the kinase signalling pathway may modulate PI3K/MEK inhibitor responsiveness in colorectal cancer. Furthermore, the addition of copanlisib to 5-FU chemoradiotherapy resulted in an enhanced anti-proliferative cytotoxic effect compared to 5-FU chemoradiotherapy alone, regardless of the background mutational status, and supports further clinical development of this regimen.
Journal
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KRAS (KRAS proto-oncogene GTPase) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha)
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KRAS mutation • PIK3CA mutation • KRAS wild-type • RAS wild-type
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5-fluorouracil • Aliqopa (copanlisib) • refametinib (BAY86-9766)
8ms
Bioinformatics screened of biomarkers for the prognosis of hepatocellular carcinoma. (PubMed, Cancer Biomark)
Hub genes were enriched in various cell types. Trametinib, selumetinib, RDEA119, and teniposide were identified as potential drugs for LIHC treatment.ConclusionCDC20, TOP2A, CDK1, CAT, TAT, and FTCD may contribute to LIHC development and serve as novel prognostic biomarkers.
Journal
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TOP2A (DNA topoisomerase 2-alpha) • CDC20 (Cell Division Cycle 20) • CDK1 (Cyclin-dependent kinase 1) • FTCD (Formimidoyltransferase Cyclodeaminase)
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Mekinist (trametinib) • Koselugo (selumetinib) • refametinib (BAY86-9766) • Vumon (teniposide)
1year
Establishment of prognosis model of hepatocellular carcinoma based on prognosis related gene analysis and study on gene regulation mechanism of model. (PubMed, Heliyon)
In addition, the high expression of model gene produced drug resistance to trametinib, selumetinib and RDEA119 (refametinib). The prognostic risk model based on six prognostic related DEGs is an independent prognostic factor of HCC, which can effectively predict the survival and prognosis of HCC patients.
Journal
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TOP2A (DNA topoisomerase 2-alpha) • CCNA2 (Cyclin A2) • CDC20 (Cell Division Cycle 20) • CDK1 (Cyclin-dependent kinase 1) • BUB1 (BUB1 Mitotic Checkpoint Serine/Threonine Kinase) • CCNB1 (Cyclin B1)
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Mekinist (trametinib) • Koselugo (selumetinib) • refametinib (BAY86-9766)
over1year
Comprehensive analysis of CPNE1 predicts prognosis and drug resistance in gastric adenocarcinoma. (PubMed, Am J Transl Res)
CPNE1 could be a predictive biomarker and a potential target for biological therapy in STAD.
Journal • PARP Biomarker
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CPNE1 (Copine 1)
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Lynparza (olaparib) • Koselugo (selumetinib) • Iclusig (ponatinib) • pazopanib • Rubraca (rucaparib) • Torisel (temsirolimus) • Inlyta (axitinib) • refametinib (BAY86-9766) • AZD8055 • seliciclib (CYC202)
2years
In Silico Identification of Therapeutic Targets and Novel Drug Candidates for Malignant Peripheral Nerve Sheath Tumors. (PubMed, Front Biosci (Landmark Ed))
Overall, our results describe the importance of Twist1 in MPNST pathogenesis. Everolimus was also found to be a potential therapeutic drug for MPNSTs.
Journal
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TWIST1 (Twist Family BHLH Transcription Factor 1)
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everolimus • Cabometyx (cabozantinib tablet) • refametinib (BAY86-9766) • BGT226
over2years
Identification of a novel circRNA-miRNA-mRNA regulatory axis in hepatocellular carcinoma based on bioinformatics analysis. (PubMed, Sci Rep)
The results suggest that the sensitivity toward trametinib, refametinib (RDEA119), and selumetinib correlates to the expression of WDR76. ROC analysis showed that the area under the curve (AUC) of all genes in the regulatory axis was greater than 0.7. The identified hsa_circ_0000417/hsa_circ_0002688/hsa_circ_0001387--hsa-miR-199a-5p--WDR76 regulatory axis may provide new insights into the progression, clinical diagnosis, and treatment of HCC.
Journal • IO biomarker
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MIR199A1 (MicroRNA 199a-1) • MIR199A (MicroRNA 199a) • ACTG1 (Actin Gamma 1) • E2F3 (E2F transcription factor 3)
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Mekinist (trametinib) • Koselugo (selumetinib) • refametinib (BAY86-9766)
over3years
Integrated analysis of pivotal biomarker of LSM1, immune cell infiltration and therapeutic drugs in breast cancer. (PubMed, J Cell Mol Med)
Most importantly, pharmacogenetic analysis of BRCA cell lines revealed that LSM1 inactivation was associated with increased sensitivity to refametinib and trametinib. However, both drugs could mimic the effects of LSM1 inhibition and their drug sensitivity was associated with MEK molecules. Therefore, we investigated the clinical application of LSM1 to provide a basis for sensitive diagnosis, prognosis and targeted treatment of breast cancer.
Journal • BRCA Biomarker
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BRCA (Breast cancer early onset) • LSM1 (LSM1 Homolog, MRNA Degradation Associated)
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BRCA deletion
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Mekinist (trametinib) • refametinib (BAY86-9766)
over3years
Establishment of prognostic risk model and drug sensitivity based on prognostic related genes of esophageal cancer. (PubMed, Sci Rep)
High expression of HIST1H1E was resistant to trametinib, selumetinib, RDEA119, docetaxel and 17-AAG, High expression of UBE2C was resistant to masitinib, and Low expression of ERO1B made the EC more sensitive to FK866. We constructed an EC risk score model composed of 8 DEGs and gene resistance analysis, which can provide reference for prognosis prediction, diagnosis and treatment of the EC patients.
Journal
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UBE2C (Ubiquitin Conjugating Enzyme E2 C)
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Mekinist (trametinib) • docetaxel • Koselugo (selumetinib) • refametinib (BAY86-9766) • daporinad (APO866) • Kinaction (masitinib)
over3years
Statistics and network-based approaches to identify molecular mechanisms that drive the progression of breast cancer. (PubMed, Comput Biol Med)
Finally, we suggested KGs-guided three repurposable candidate-drugs (Trametinib, selumetinib, and RDEA119) for BC treatment by using the GSCALite online web tool and validated them through molecular docking analysis, and found their strong binding affinities. Therefore, the findings of this study might be useful resources for BC diagnosis, prognosis and therapies.
Journal
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CCNA2 (Cyclin A2) • BUB1 (BUB1 Mitotic Checkpoint Serine/Threonine Kinase) • CCNB1 (Cyclin B1) • RFC4 (Replication Factor C Subunit 4)
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Mekinist (trametinib) • Koselugo (selumetinib) • refametinib (BAY86-9766)