Therapy Detail
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| Therapy Name | Dasatinib + Gefitinib + Vemurafenib |
| 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). |
| Vemurafenib | Zelboraf | RO5185426|PLX4032 | RAF Inhibitor (Pan) 27 | Zelboraf (vemurafenib) inhibits BRAF V600E, wild-type BRAF, ARAF, and CRAF (PMID: 20179705), which may result in an inhibition of the MAPK signaling pathway resulting in a reduction of tumor cell proliferation (PMID: 20823850). Zelboraf (vemurafenib) is FDA approved for BRAF V600E-mutant melanoma and for BRAF V600-positive Erdheim-Chester disease (FDA.gov). |
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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 + Vemurafenib | Preclinical - Pdx & cell culture | Actionable | In a preclinical study, the combination of Zelboraf (vemurafenib), Iressa (gefitinib), and Sprycel (dasatinib) synergistically inhibited viability in colorectal cancer cell lines harboring BRAF V600E in culture and resulted in greater tumor growth inhibition and tumor regression in patient-derived xenograft (PDX) models to a greater degree than the doublet combinations of Zelboraf (vemurafenib) and Iressa (gefitinib) or Zelboraf (vemurafenib) 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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