Therapy Detail
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| Therapy Name | Everolimus + Selumetinib |
| Synonyms | |
| Therapy Description | |
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| Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
|---|---|---|---|---|
| Everolimus | Afinitor | RAD001|Zortress | mTORC1 Inhibitor 9 | Afinitor (everolimus) binds to FKBP-12 and allosterically inhibits mTOR, leading to decreased mTORC1 signaling and potentially resulting in decreased tumor cell growth (PMID: 17766661, PMID: 28400999). Afinitor (everolimus) is FDA approved for use in neuroendocrine tumors of pancreatic, lung or gastrointestinal tract origin, advanced renal cell carcinoma, in adult and pediatric patients aged 1 year and older with tuberous sclerosis complex who have subependymal giant cell astrocytoma, and in combination with Aromasin (exemestane) in hormone receptor-positive, HER2-negative breast cancer (FDA.gov). |
| 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 wild-type | high grade glioma | predicted - sensitive | Everolimus + Selumetinib | Preclinical - Cell culture | Actionable | In a preclinical study, Afinitor (everolimus) and Selumetinib (AZD6244) synergistically inhibited growth and induced apoptosis in glioma cell lines in culture (PMID: 27217440). | 27217440 |
| HRAS G12V | urinary bladder cancer | sensitive | Everolimus + Selumetinib | Preclinical - Cell culture | Actionable | In a preclinical study, the combination of Selumetinib (AZD6244) and Afinitor (everolimus) reduced phosphorylation of ERK and S6 and worked synergistically to inhibit growth of a bladder cancer cell line harboring HRAS G12V in culture (PMID: 26544513). | 26544513 |
| BRAF V600E | high grade glioma | predicted - sensitive | Everolimus + Selumetinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Selumetinib (AZD6244) and Afinitor (everolimus) synergistically inhibited growth and induced apoptosis in glioma cell lines in culture, resulted in prolonged survival in cell line xenograft models (PMID: 27217440). | 27217440 |
| HRAS Q61L | lung squamous cell carcinoma | sensitive | Everolimus + Selumetinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, the combination of Selumetinib (AZD6244) and Afinitor (everolimus) inhibited growth of a lung squamous cell carcinoma cell line harboring HRAS Q61L in culture, and inhibited tumor growth in xenograft models, with increased efficacy compared to either agent alone (PMID: 26544513). | 26544513 |
| PIK3CA wild-type PTEN loss | breast cancer | no benefit | Everolimus + Selumetinib | Preclinical - Cell culture | Actionable | In a preclinical study, breast cancer cells harboring PIK3CA wild-type and PTEN loss did not demonstrate any benefit when treated with a combination of Afinitor (everolimus) and Selumetinib (AZD6244) (PMID: 21358673). | 21358673 |
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
|---|
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