Therapy Detail
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| Therapy Name | GSK2126458 |
| Synonyms | |
| Therapy Description |
GSK2126458 is a dual pan-PI3K and mTOR inhibitor, which blocks PI3K/AKT signaling to prevent cell proliferation (PMID: 24900173). |
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| Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
|---|---|---|---|---|
| GSK2126458 | GSK458|Omipalisib | mTOR Inhibitor 51 PI3K Inhibitor (Pan) 37 | 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 |
|---|---|---|---|---|---|---|---|
| NOTCH1 G192* | head and neck squamous cell carcinoma | predicted - sensitive | GSK2126458 | Preclinical - Cell culture | Actionable | In a preclinical study, a head and neck squamous cell carcinoma cell line harboring NOTCH1 G192* demonstrated apoptotic activity and reduced colony growth when treated with GSK2126458 in culture (PMID: 30770351). | 30770351 |
| BRAF V600K NRAS Q61K | 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 |
| PDGFRA D842V | Advanced Solid Tumor | sensitive | GSK2126458 | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing PDGFRA D842V demonstrated sensitivity to GSK2126458 (omipalisib) in culture, resulting in decreased cell proliferation (PMID: 30389923). | 30389923 |
| 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 |
| Unknown unknown | Advanced Solid Tumor | not applicable | GSK2126458 | Phase I | Actionable | In a Phase I trial, GSK2126458 demonstrated safety and preliminary efficacy in patients with advanced solid tumors (J Clin Oncol (Meeting Abstracts) 2011 29: 3018). | detail... |
| Unknown unknown | urinary bladder cancer | not applicable | GSK2126458 | Phase I | Actionable | In Phase I trial, GSK2126458 treatment was well-tolerated and resulted in a partial response and stable disease in two patients and one patient with bladder cancer, respectively (PMID: 26603258). | 26603258 |
| NOTCH1 C478F | head and neck squamous cell carcinoma | predicted - sensitive | GSK2126458 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, a head and neck squamous cell carcinoma cell line harboring NOTCH1 C478F demonstrated apoptotic activity and reduced colony growth in culture and tumor regression in cell line xenograft models when treated with GSK2126458 (PMID: 30770351). | 30770351 |
| 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 |
| Unknown unknown | renal cell carcinoma | not applicable | GSK2126458 | Phase I | Actionable | In a Phase I trial, GSK2126458 treatment was well-tolerated and resulted in some efficacy in renal cell carcinoma patients including stable disease in 13% (3/24), one patient with a complete response, and one patient with a partial response (PMID: 26603258). | 26603258 |
| 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 |
| NOTCH1 Q1957* | head and neck squamous cell carcinoma | predicted - sensitive | GSK2126458 | Preclinical - Cell culture | Actionable | In a preclinical study, a head and neck squamous cell carcinoma cell line harboring NOTCH1 Q1957* demonstrated apoptotic activity and reduced colony growth when treated with GSK2126458 in culture (PMID: 30770351). | 30770351 |
| PDGFRA V561D | Advanced Solid Tumor | sensitive | GSK2126458 | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing PDGFRA V561D demonstrated sensitivity to GSK2126458 (omipalisib) in culture, resulting in decreased cell proliferation (PMID: 30389923). | 30389923 |
| NOTCH1 H2018fs | head and neck squamous cell carcinoma | predicted - sensitive | GSK2126458 | Preclinical - Cell culture | Actionable | In a preclinical study, a head and neck squamous cell carcinoma cell line harboring NOTCH1 H2018fs demonstrated apoptotic activity and reduced colony growth when treated with GSK2126458 in culture (PMID: 30770351). | 30770351 |
| NOTCH1 E694* | head and neck squamous cell carcinoma | predicted - sensitive | GSK2126458 | Preclinical - Cell culture | Actionable | In a preclinical study, a head and neck squamous cell carcinoma cell line harboring NOTCH1 E694* demonstrated apoptotic activity and reduced colony growth when treated with GSK2126458 in culture (PMID: 30770351). | 30770351 |
| 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 |
| Unknown unknown | endometrial cancer | not applicable | GSK2126458 | Phase I | Actionable | In a Phase I trial, GSK2126458 treatment was well-tolerated and resulted in some efficacy in endometrial cancer patients including stable disease in 27% (4/15) and one patient with a partial response (PMID: 26603258). | 26603258 |
| PDGFRA Y288C | Advanced Solid Tumor | sensitive | GSK2126458 | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing PDGFRA Y288C demonstrated sensitivity to GSK2126458 (omipalisib) in culture, resulting in decreased cell proliferation (PMID: 30389923). | 30389923 |
| 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 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 |
| Unknown unknown | breast cancer | not applicable | GSK2126458 | Phase I | Actionable | In a Phase I trial, GSK2126458 was well-tolerated and resulted in some efficacy in patients with breast cancer, including stable disease in 31% (7/22) and one patient with a partial response (PMID: 26603258). | 26603258 |
| 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 |
| NOTCH1 V489fs | head and neck squamous cell carcinoma | predicted - sensitive | GSK2126458 | Preclinical - Cell culture | Actionable | In a preclinical study, a head and neck squamous cell carcinoma cell line harboring NOTCH1 V489fs demonstrated apoptotic activity and reduced colony growth when treated with GSK2126458 in culture (PMID: 30770351). | 30770351 |
| NOTCH1 E1679* | head and neck squamous cell carcinoma | predicted - sensitive | GSK2126458 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, a head and neck squamous cell carcinoma cell line harboring NOTCH1 E1679* demonstrated apoptotic activity and reduced colony growth in culture and tumor regression in cell line xenograft models when treated with GSK2126458 (PMID: 30770351). | 30770351 |
| NOTCH1 C344fs | head and neck squamous cell carcinoma | predicted - sensitive | GSK2126458 | Preclinical - Cell culture | Actionable | In a preclinical study, a head and neck squamous cell carcinoma cell line harboring NOTCH1 C344fs demonstrated apoptotic activity and reduced colony growth when treated with GSK2126458 in culture (PMID: 30770351). | 30770351 |
Filtering
- Case insensitive filtering will display rows where any text in any cell matches the filter term
- Simple literal full or partial string matches
- Separate multiple filter terms with a spaces, order doesn't matter (a b c and c b a are equivalent )
- Filtering will only apply to rows that are already loaded on the page, filtering has no impact on query parameters
- Use quotes to match a longer phrase which contains spaces "mtor c1483f"
Sorting
- Generally, the default sort order for tables is set to be first column ascending, however, specific tables may set a different default sort order.
- Click on any column header arrows to sort by that column
- Hold down the Shift key and click multiple columns to sort by more than one column, be sure to set ascending or descending order for a given column, before moving on to the next column.
| Clinical Trial | Phase | Therapies | Title | Recruitment Status |
|---|
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