Therapy Detail
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| Therapy Name | Dasatinib + 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). |
| 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 H1047R | anaplastic thyroid carcinoma | sensitive | Dasatinib + Trametinib | Preclinical - Cell culture | Actionable | In a preclinical study, the combination of Sprycel (dasatinib) and Mekinist (trametinib) inhibited viability of an anaplastic thyroid cancer cell line harboring BRAF V600E and PIK3CA H1047R in culture (PMID: 37713162). | 37713162 |
| BRAF V600E | thyroid cancer | sensitive | Dasatinib + Trametinib | Preclinical - Cell culture | Actionable | In a preclinical study, Sprycel (dasatinib) and Mekinist (trametinib) synergistically inhibited proliferation and induced apoptosis in both parental thyroid cancer cell lines harboring BRAF V600E and those acquired Sprycel (dasatinib)-resistance in culture (PMID: 27222538). | 27222538 |
| HRAS G13R | thyroid cancer | sensitive | Dasatinib + Trametinib | Preclinical - Cell culture | Actionable | In a preclinical study, Sprycel (dasatinib) and Mekinist (trametinib) synergistically inhibited growth and induced apoptosis in a thyroid cancer cell line harboring HRAS G13R in culture (PMID: 27222538). | 27222538 |
| BRAF V600E PIK3CA N1044S | anaplastic thyroid carcinoma | resistant | Dasatinib + Trametinib | Preclinical - Cell culture | Actionable | In a preclinical study, an anaplastic thyroid cancer cell line harboring BRAF V600E and PIK3CA N1044S was resistant to the combination of Sprycel (dasatinib) and Mekinist (trametinib) in culture (PMID: 37713162). | 37713162 |
| BRAF V600E PIK3CA W11C PIK3CA E542K | papillary thyroid carcinoma | sensitive | Dasatinib + Trametinib | Preclinical - Cell culture | Actionable | In a preclinical study, the combination of Sprycel (dasatinib) and Mekinist (trametinib) inhibited viability of a papillary thyroid cancer cell line harboring BRAF V600E and PIK3CA E542K and W11C in culture (PMID: 37713162). | 37713162 |
| BRAF V600E PIK3CA M1043I | anaplastic thyroid carcinoma | sensitive | Dasatinib + Trametinib | Preclinical - Cell culture | Actionable | In a preclinical study, the combination of Sprycel (dasatinib) and Mekinist (trametinib) inhibited viability of an anaplastic thyroid cancer cell line harboring BRAF V600E and PIK3CA M1043I in culture (PMID: 37713162). | 37713162 |
| BRAF V600E PIK3CA E542K | anaplastic thyroid carcinoma | resistant | Dasatinib + Trametinib | Preclinical - Cell culture | Actionable | In a preclinical study, an anaplastic thyroid cancer cell line harboring BRAF V600E and PIK3CA E542K was resistant to the combination of Sprycel (dasatinib) and Mekinist (trametinib) in culture (PMID: 37713162). | 37713162 |
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
|---|
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