Therapy Detail
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| Therapy Name | Regorafenib + Trametinib |
| Synonyms | |
| Therapy Description | |
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| Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
|---|---|---|---|---|
| Regorafenib | Stivarga | BAY 73-4506 | BRAF Inhibitor 24 CRAF Inhibitor 12 KIT Inhibitor 56 PDGFR Inhibitor (Pan) 30 RET Inhibitor 52 VEGFR Inhibitor (Pan) 36 VEGFR2 Inhibitor 37 | Stivarga (regorafenib) is an inhibitor of several kinases including VEGFR, RET, KIT, PDGFR and RAF, thereby inhibiting tumor angiogenesis and tumor cell proliferation (PMID: 24756792). Stivarga (regorafenib) is FDA approved for colorectal cancer, hepatocellular carcinoma, and GIST (FDA.gov). |
| Trametinib | Mekinist | GSK1120212 | MEK inhibitor (Pan) 23 MEK1 Inhibitor 25 MEK2 Inhibitor 23 | 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 |
|---|---|---|---|---|---|---|---|
| FGFR1 over exp | stomach cancer | sensitive | Regorafenib + Trametinib | Preclinical - Cell culture | Actionable | In a preclinical study, the addition of Mekinist (trametinib) restored sensitivity of gastric cancer cells with FGFR1 overexpression to Stivarga (regorafenib) treatment, demonstrating decreased Erk phosphorylation and reduced cell proliferation in culture (PMID: 33563752). | 33563752 |
| FGFR2 amp | stomach cancer | sensitive | Regorafenib + Trametinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, the addition of Mekinist (trametinib) restored sensitivity of gastric cancer cells with FGFR2 amplification to Stivarga (regorafenib) treatment, demonstrating decreased Erk phosphorylation and reduced cell proliferation in culture, and in cell line xenograft models led to inhibition of tumor growth (PMID: 33563752). | 33563752 |
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
|---|
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