Therapy Detail
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| Therapy Name | G007-LK + Trametinib |
| Synonyms | |
| Therapy Description | |
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| Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
|---|---|---|---|---|
| G007-LK | Tankyrase Inhibitor 11 | G007-LK inhibits tankyrase, which leads to stabilization of AXIN, thereby resulting in degradation of beta-catenin and decreased growth of APC-deficient tumors (PMID: 23539443, PMID: 32575464). | ||
| 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 |
|---|---|---|---|---|---|---|---|
| APC R302* APC E1345* | colorectal cancer | sensitive | G007-LK + Trametinib | Preclinical - Cell culture | Actionable | In a preclinical study, the addition of G007-LK to Mekinist (trametinib) treatment resulted in increased inhibition of viability compared to Mekinist (trametinib) alone in a colorectal cancer patient-derived cell line harboring APC R302* and E1345* in culture (PMID: 37968472). | 37968472 |
| APC R216* | colorectal cancer | sensitive | G007-LK + Trametinib | Preclinical - Cell culture | Actionable | In a preclinical study, the addition of G007-LK to Mekinist (trametinib) treatment resulted in increased inhibition of viability compared to Mekinist (trametinib) alone in a colorectal cancer patient-derived cell line harboring APC R216* in culture (PMID: 37968472). | 37968472 |
| APC E941* APC T1459fs | colorectal cancer | sensitive | G007-LK + Trametinib | Preclinical - Cell culture | Actionable | In a preclinical study, the addition of G007-LK to Mekinist (trametinib) treatment resulted in increased inhibition of viability compared to Mekinist (trametinib) alone in a colorectal cancer patient-derived cell line harboring APC E941* and T1459fs in culture (PMID: 37968472). | 37968472 |
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
|---|
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