Therapy Detail
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| Therapy Name | Uprosertib |
| Synonyms | |
| Therapy Description |
Uprosertib (GSK2141795) is an ATP-competitive inhibitor of AKT, which leads to inhibition of PI3K/AKT signaling potentially resulting in inhibition of cell proliferation and anti-tumor growth (PMID: 24978597). |
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| Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
|---|---|---|---|---|
| Uprosertib | GSK2141795|GSK-2141795|GSK 2141795 | Akt Inhibitor (Pan) 19 AKT Inhibitor (Pan) - ATP competitive 7 | Uprosertib (GSK2141795) is an ATP-competitive inhibitor of AKT, which leads to inhibition of PI3K/AKT signaling potentially resulting in inhibition of cell proliferation and anti-tumor growth (PMID: 24978597, PMID: 32062691). |
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| Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|---|---|---|---|---|---|---|
| AKT1 S266L FGFR1 amp | lung cancer | predicted - sensitive | Uprosertib | Preclinical - Cell culture | Actionable | In a preclinical study, lung cancer cells harboring FGFR1 amplification and AKT1 S266L demonstrated sensitivity to Uprosertib (GSK2141795) in culture, showing decreased phosphorylation of Akt1 targets and reduced cell growth (PMID: 30140389). | 30140389 |
| AKT1 E17K | melanoma | sensitive | Uprosertib | Preclinical - Cell culture | Actionable | In a preclinical study, Uprosertib (GSK2141795) inhibited the growth of melanoma cells harboring AKT1 E17K in culture (PMID: 24735930). | 24735930 |
| AKT1 wild-type | ovarian cancer | predicted - sensitive | Uprosertib | Phase I | Actionable | In a Phase I trial, GSK2141795 treatment resulted in Akt inhibition and clinical benefit in 27% (3/11) of ovarian cancer patients (PMID: 26429956). | 26429956 |
| AKT1 E17K | cancer | sensitive | Uprosertib | Preclinical | Actionable | In a preclinical study, the pan AKT inhibitor GSK2141795 displayed similar levels of inhibition against ATK1 E17K (activating mutation) as ATK1 wild-type (PMID: 24978597). | 24978597 |
| PIK3CA mutant | Advanced Solid Tumor | predicted - sensitive | Uprosertib | Phase I | Actionable | In a Phase I clinical trial, GSK2141795 demonstrated safety and preliminary efficacy in patients with advanced solid tumors, with 4 patients with PIK3CA mutations and/or PTEN loss achieving stable disease for greater than 6 months (J Clin Oncol 29: 2011 (suppl; abstr 3003)). | detail... |
| AKT1 wild-type | cancer | sensitive | Uprosertib | Preclinical | Actionable | In a preclinical study, GSK2141795 inhibited all isoforms of AKT in human cancer cell lines (PMID: 23795919). | 23795919 |
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
|---|
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