Therapy Detail
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| Therapy Name | Dasatinib + Gefitinib + PLX4720 |
| 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 31 BTK inhibitor 36 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). |
| Gefitinib | Iressa | ZD1839 | EGFR Inhibitor (Pan) 61 EGFR Inhibitor 1st gen 3 | Iressa (gefitinib) is a first-generation EGFR inhibitor that binds EGFR and inhibits downstream signaling, potentially resulting in decreased growth of tumors with EGFR activation (PMID: 26980062, PMID: 25302162, PMID: 15284455). Iressa (gefitinib) is FDA approved for use in patients with non-small cell lung cancer harboring an EGFR exon 19 deletion or EGFR L858R (FDA.gov). |
| PLX4720 | PLX-4720|PLX 4720 | BRAF Inhibitor 25 | PLX4720 is a 7-azaindole derivative and RAF kinase inhibitor with greater affinity for BRAF V600E than BRAF wild-type, which may induce cell cycle arrest and apoptosis, and lead to tumor growth inhibition and regression (PMID: 18287029). |
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| Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|---|---|---|---|---|---|---|
| BRAF V600E | colorectal cancer | sensitive | Dasatinib + Gefitinib + PLX4720 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, the combination of PLX4720, Iressa (gefitinib), and Sprycel (dasatinib) inhibited tumor growth in colorectal cancer cell line xenograft models harboring BRAF V600E to a greater degree than the combinations of PLX4720 and Iressa (gefitinib) or PLX4720 and Sprycel (dasatinib) (PMID: 36759733). | 36759733 |
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
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