Therapy Detail
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| Therapy Name | Selumetinib + ZSTK474 |
| Synonyms | |
| Therapy Description | |
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| Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
|---|---|---|---|---|
| Selumetinib | Koselugo | AZD6244|ARRY-142886 | MEK inhibitor (Pan) 26 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). |
| ZSTK474 | ZSTK-474 | PI3K Inhibitor (Pan) 42 | ZSTK474 is a pan-PI3K inhibitor, which blocks PI3K/AKT signaling to prevent cell growth (PMID: 16622124, PMID: 30205797). |
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| Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|---|---|---|---|---|---|---|
| BRAF V600E/K PIK3CA wild-type | melanoma | sensitive | Selumetinib + ZSTK474 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Selumetinib (AZD6244) and ZSTK474 combination treatment inhibited proliferation of melanoma cell lines harboring BRAF V600E/K and wild-type PIK3CA in culture, and synergistically inhibited tumor growth in cell line xenograft models (PMID: 26137449). | 26137449 |
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
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