Therapy Detail
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| Therapy Name | Everolimus + MK2206 |
| 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). |
| MK2206 | MK-2206|MK 2206 | Akt Inhibitor (Pan) 22 | MK2206 binds to and inhibits the activity of AKT in a non-ATP competitive manner, which may result in the inhibition of the PI3K/AKT signaling pathway and tumor cell proliferation (PMID: 20571069, PMID: 32194695). |
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| Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|---|---|---|---|---|---|---|
| PIK3CA E418K PIK3CA E453K | breast cancer | sensitive | Everolimus + MK2206 | Preclinical - Cell culture | Actionable | In a preclinical study, treatment with the combination of MK2206 and Afinitor (everolimus) synergistically inhibited proliferation, decreased Akt phosphorylation, and increased apoptosis in a breast cancer cell line harboring PIK3CA E418K and E453K in culture (PMID: 38909932). | 38909932 |
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
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