Therapy Detail
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| Therapy Name | GSK2334470 + Trametinib |
| Synonyms | |
| Therapy Description | |
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| Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
|---|---|---|---|---|
| GSK2334470 | GSK-470 | PDPK1 Inhibitor 10 | GSK2334470 is a small molecule inhibitor of PDPK1, which subsequently results in suppression of Akt and may result in antiproliferative activity (PMID: 29658600, PMID: 32188393). | |
| Trametinib | Mekinist | GSK1120212 | MEK inhibitor (Pan) 26 MEK1 Inhibitor 26 MEK2 Inhibitor 24 | Mekinist (trametinib) inhibits MEK 1 and 2, which potentially leads to reduced tumor cell proliferation (PMID: 27956260). Mekinist (trametinib) is FDA approved for melanoma patients harboring BRAF V600E or BRAF V600K mutations, and in combination with Tafinlar (dabrafenib) for BRAF V600E/K-mutant melanoma, BRAF V600E- mutant non-small cell lung cancer, BRAF V600E-mutant anaplastic thyroid cancer, for adult and pediatric patients of 6 years or older with unresectable or metastatic solid tumors harboring BRAF V600E, and for pediatric patients of 1 year or older with low-grade glioma harboring BRAF V600E (FDA.gov). |
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| Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|---|---|---|---|---|---|---|
| BRAF V600E PIK3CA N1044S | anaplastic thyroid carcinoma | sensitive | GSK2334470 + Trametinib | Preclinical - Cell culture | Actionable | In a preclinical study, the addition of GSK2334470 sensitized an anaplastic thyroid cancer cell line harboring BRAF V600E and PIK3CA N1044S to Mekinist (trametinib) treatment as demonstrated by a reduction in viability in culture (PMID: 37713162). | 37713162 |
| BRAF V600E PIK3CA E542K | anaplastic thyroid carcinoma | sensitive | GSK2334470 + Trametinib | Preclinical - Cell culture | Actionable | In a preclinical study, the addition of GSK2334470 sensitized an anaplastic thyroid cancer cell line harboring BRAF V600E and PIK3CA E542K to Mekinist (trametinib) treatment as demonstrated by a reduction in viability in culture (PMID: 37713162). | 37713162 |
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
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