Therapy Detail

Therapy Name GSK343 + Selumetinib
Therapy Description


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Drug Name Trade Name Synonyms Drug Classes Drug Description
GSK343 EZH2 inhibitor 16 GSK343 is an inhibitor of EZH2, which decreases tri-methylation of H3K27, potentially resulting in decreased growth and increased apoptosis of tumor cells (PMID: 23759589).
Selumetinib AZD6244|ARRY-142886 MEK inhibitor (Pan) 20 MEK1 Inhibitor 20 MEK2 Inhibitor 18 Selumetinib (AZD6244) inhibits mitogen-activated protein kinase kinases (MEK or MAPK/ERK kinases) 1 and 2, which may prevent the activation of MEK1/2-dependent effector proteins and transcription factors, reducing cellular proliferation in various cancers (PMID: 27467210).
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
KRAS G12C EZH2 pos lung adenocarcinoma sensitive GSK343 + Selumetinib Preclinical - Cell culture Actionable In a preclinical study, the addition of GSK343 increased sensitivity to Selumetinib (AZD6244) in EZH2-expressing lung adenocarcinoma cell lines harboring KRAS G12C in culture (PMID: 26676756). 26676756
KRAS G12D EZH2 pos lung adenocarcinoma no benefit GSK343 + Selumetinib Preclinical - Cell culture Actionable In a preclinical study, the addition of GSK343 did not increase sensitivity to Selumetinib (AZD6244) in an EZH2-expressing lung adenocarcinoma cell line harboring KRAS G12D (PMID: 26676756). 26676756
Clinical Trial Phase Therapies Title Recruitment Status