Therapy Detail
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| Therapy Name | PLX4720 + Selumetinib |
| Synonyms | |
| Therapy Description | |
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| Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
|---|---|---|---|---|
| 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). | |
| Selumetinib | Koselugo | AZD6244|ARRY-142886 | MEK inhibitor (Pan) 24 MEK1 Inhibitor 26 MEK2 Inhibitor 24 | Koselugo (selumetinib) inhibits mitogen-activated protein kinase kinases (MEK or MAPK/ERK kinases) 1 and 2, which may prevent the activation of MEK1/2-dependent effector proteins and transcription factors, reducing cellular proliferation in various cancers (PMID: 27467210). Koselugo (selumetinib) is FDA approved for use in pediatric patients of 2 years or older with neurofibromatosis type 1 (NF1) who have symptomatic, inoperable plexiform neurofibromas (FDA.gov). |
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| Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|---|---|---|---|---|---|---|
| BRAF V600E MAP2K1 P124L | melanoma | sensitive | PLX4720 + Selumetinib | Preclinical | Actionable | In a preclinical study, combined treatment with Koselugo (selumetinib) and PLX4720 inhibited growth of melanoma cells harboring BRAF V600E and expressing MAP2K1 P124L in culture (PMID: 19915144). | 19915144 |
| BRAF V600E | high grade glioma | predicted - sensitive | PLX4720 + Selumetinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Selumetinib (AZD6244) and PLX4720 synergistically inhibited growth and induced apoptosis in glioma cell lines in culture, resulted in prolonged survival in cell line xenograft models (PMID: 27217440). | 27217440 |
| BRAF V600E | melanoma | sensitive | PLX4720 + Selumetinib | Preclinical | Actionable | In a preclinical study, PLX4720 and Selumetinib (AZD6244) worked synergistically to inhibit cell growth in PLX4720-resistant melanoma cell lines harboring BRAF V600E in culture (PMID: 26461489). | 26461489 |
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
|---|
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