Therapy Detail

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Therapy Name	GSK2126458
Synonyms
Therapy Description	Omipalisib (GSK2126458) is a dual pan-PI3K and mTOR inhibitor, which blocks PI3K/AKT signaling to prevent cell proliferation (PMID: 24900173, PMID: 32382996).

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Drug Name	Trade Name	Synonyms	Drug Classes	Drug Description
GSK2126458		GSK458\|Omipalisib	mTOR Inhibitor 51 PI3K Inhibitor (Pan) 42	Omipalisib (GSK2126458) is a dual pan-PI3K and mTOR inhibitor, which blocks PI3K/AKT signaling to prevent cell proliferation (PMID: 24900173, PMID: 32382996).

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Molecular Profile	Indication/Tumor Type	Response Type	Therapy Name	Approval Status	Evidence Type	Efficacy Evidence	References
PIK3CA mutant	breast cancer	no benefit	GSK2126458	Phase I	Actionable	In a Phase I trial, GSK2126458 was well-tolerated and resulted in some efficacy in patients with breast cancer harboring a PIK3CA mutation including stable disease in 22% (2/9), however, objective response rate was not associated with PIK3CA mutations when compared to those without PIK3CA mutations (PMID: 26603258).	26603258
BRAF V600K NRAS Q61K	melanoma	predicted - sensitive	GSK2126458	Preclinical - Cell culture	Actionable	In a preclinical study, Omipalisib (GSK2126458) inhibited the growth of melanoma cell lines harboring BRAF V600K with NRAS Q61K in culture (PMID: 22389471).	22389471
BRAF V600E	melanoma	sensitive	GSK2126458	Preclinical	Actionable	In a preclinical study, Omipalisib (GSK2126458) inhibited the growth of melanoma cell lines harboring BRAF V600E in culture (PMID: 22389471).	22389471
BRAF V600E MAP2K1 K59del	melanoma	decreased response	GSK2126458	Preclinical	Actionable	In a preclinical study, human melanoma cell lines harboring BRAF V600E and MAP2K1 K59del had reduced sensitivity to Omipalisib (GSK2126458) in comparison to parental cell lines harboring BRAF V600E in culture (PMID: 22389471).	22389471
BRAF V600E MAP2K1 P387S NRAS A146T	melanoma	decreased response	GSK2126458	Preclinical	Actionable	In a preclinical study, melanoma cell lines harboring BRAF V600E, NRAS A146T and MAP2K1 P387S had reduced sensitivity to Omipalisib (GSK2126458) in comparison to parental cell lines harboring BRAF V600E in culture (PMID: 22389471).	22389471
BRAF V600E MAP2K1 P387S NRAS Q61K	melanoma	decreased response	GSK2126458	Preclinical	Actionable	In a preclinical study, human melanoma cell lines harboring BRAF V600E, NRAS Q61K and MAP2K1 P387S had reduced sensitivity to Omipalisib (GSK2126458) in comparison to parental cell lines harboring BRAF V600E in culture (PMID: 22389471).	22389471
BRAF V600E MAP2K1 P387S NRAS Q61K NRAS A146T	melanoma	decreased response	GSK2126458	Preclinical	Actionable	In a preclinical study, melanoma cell lines harboring BRAF V600E, NRAS Q61K, NRAS A146T and MAP2K1 P387S had reduced sensitivity to Omipalisib (GSK2126458) in comparison to parental cell lines harboring BRAF V600E in culture (PMID: 22389471).	22389471
BRAF V600E NRAS A146T	melanoma	decreased response	GSK2126458	Preclinical	Actionable	In a preclinical study, melanoma cell lines harboring BRAF V600E and NRAS A146T had reduced sensitivity to Omipalisib (GSK2126458) in comparison to parental cell lines harboring BRAF V600E in culture (PMID: 22389471).	22389471
BRAF V600K	melanoma	sensitive	GSK2126458	Preclinical	Actionable	In a preclinical study, Omipalisib (GSK2126458) inhibited the growth of melanoma cell lines harboring BRAF V600K in culture (PMID: 22389471).	22389471

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