Therapy Detail

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 Akt Inhibitor (Pan) 17 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).

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  • Case insensitive filtering will display rows where any text in any cell matches the filter term
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  • Use quotes to match a longer phrase which contains spaces "mtor c1483f"

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Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
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
BRAF V600X PTEN neg melanoma sensitive Uprosertib Preclinical - Cell culture Actionable In a preclinical study, lack of PTEN expression was associated with increased sensitivity to GSK2141795 in BRAF V600-mutant melanoma cell lines in culture (PMID: 24265152). 24265152
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 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
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
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
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...

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Clinical Trial Phase Therapies Title Recruitment Status


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