Therapy Name | GSK343 + Selumetinib |
Therapy Description |
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 |
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Clinical Trial | Phase | Therapies | Title | Recruitment Status |
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