Therapy Detail
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| Therapy Name | Dasatinib + MK2206 + Trametinib |
| Synonyms | |
| Therapy Description | |
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| Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
|---|---|---|---|---|
| Dasatinib | Sprycel | BMS-354825 | ABL Inhibitor (pan) 9 BCR-ABL Inhibitor 32 BTK inhibitor 37 CSF1R Inhibitor 28 DDR1 Inhibitor 10 DDR2 inhibitor 7 KIT Inhibitor 57 PDGFR Inhibitor (Pan) 30 SRC Inhibitor 31 TNK2 Inhibitor 6 | Sprycel (dasatinib) is an inhibitor of the SRC-family of protein kinases, BCR-ABL, and ABL, and has additional activity against other kinases including KIT, DDR1/2, PDGFRA/B, and EPHA2, which prevents cell growth (PMID: 25709401, PMID: 25284748, PMID: 18797457, PMID: 23942795). Sprycel (dasatinib) is FDA approved for both Philadelphia chromosome positive adult and pediatric chronic myelogenous leukemia and adult acute lymphoblastic leukemia (FDA.gov). |
| MK2206 | MK-2206|MK 2206 | Akt Inhibitor (Pan) 21 | MK2206 binds to and inhibits the activity of AKT in a non-ATP competitive manner, which may result in the inhibition of the PI3K/AKT signaling pathway and tumor cell proliferation (PMID: 20571069, PMID: 32194695). | |
| 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 | resistant | Dasatinib + MK2206 + Trametinib | Preclinical - Cell culture | Actionable | In a preclinical study, the addition of MK2206 did not sensitize an anaplastic thyroid cancer cell line harboring BRAF V600E and PIK3CA N1044S to Sprycel (dasatinib) and Mekinist (trametinib) combination treatment in culture (PMID: 37713162). | 37713162 |
| BRAF V600E PIK3CA E542K | anaplastic thyroid carcinoma | resistant | Dasatinib + MK2206 + Trametinib | Preclinical - Cell culture | Actionable | In a preclinical study, the addition of MK2206 did not sensitize an anaplastic thyroid cancer cell line harboring BRAF V600E and PIK3CA E542k to Sprycel (dasatinib) and Mekinist (trametinib) combination treatment in culture (PMID: 37713162). | 37713162 |
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
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