Therapy Detail
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| Therapy Name | Gefitinib + PLX4720 + Saracatinib |
| Synonyms | |
| Therapy Description | |
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| Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
|---|---|---|---|---|
| Gefitinib | Iressa | ZD1839 | EGFR Inhibitor (Pan) 62 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). | |
| Saracatinib | AZD0530 | BCR-ABL Inhibitor 32 SRC Inhibitor 31 | Saracatinib (AZD0530) is a multi-kinase inhibitor with activity against ABL and SRC, which may block proliferation, metastasis, and survival in cancer cells (PMID: 19393585, PMID: 32398945). |
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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 | Gefitinib + PLX4720 + Saracatinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, the combination of PLX4720, Iressa (gefitinib), and Saracatinib (AZD0530) 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 Saracatinib (AZD0530) (PMID: 36759733). | 36759733 |
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
|---|
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