Therapy Detail
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| Therapy Name | GSK126 |
| Synonyms | |
| Therapy Description |
GSK126 selectively inhibits EZH2, resulting in decreased H3K27 tri-methylation, and potentially leading to decreased tumor cell proliferation and reduced tumor growth (PMID: 23051747, PMID: 25686104). |
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| Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
|---|---|---|---|---|
| GSK126 | GSK2816126|GSK-126 | EZH2 inhibitor 18 | GSK126 selectively inhibits EZH2, resulting in decreased H3K27 tri-methylation, and potentially leading to decreased tumor cell proliferation and reduced tumor growth (PMID: 23051747, PMID: 25686104, PMID: 31471312). |
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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 |
|---|---|---|---|---|---|---|---|
| ARID1A mut PIK3CA act mut | ovarian cancer | sensitive | GSK126 | Preclinical - Cell culture | Actionable | In a preclinical study, expression of a constitutively active PIK3CA mutation in ARID1A-mutant ovarian cancer cell lines enhanced growth inhibition by GSK126 in culture (PMID: 25686104). | 25686104 |
| ARID1A mutant | ovarian cancer | sensitive | GSK126 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, GSK126 selectively inhibited growth of ARID1A-mutant ovarian cancer cells in culture, and induced tumor regression in ARID1A-mutant ovarian cancer xenograft models (PMID: 25686104). | 25686104 |
| ATRX fusion | neuroblastoma | predicted - sensitive | GSK126 | Preclinical - Cell culture | Actionable | In a preclinical study, treatment with GSK126 resulted in reduced proliferation and increased apoptosis of neuroblastoma cell lines harboring in-frame ATRX fusions in culture (PMID: 31631027). | 31631027 |
| ARID1A dec exp | ovarian cancer | sensitive | GSK126 | Preclinical - Cell culture | Actionable | In a preclinical study, GSK126 inhibited growth of ovarian cancer cells with knockdown of ARID1A expression in culture (PMID: 25686104). | 25686104 |
| ARID1A wild-type | ovarian cancer | no benefit | GSK126 | Preclinical - Cell culture | Actionable | In a preclinical study, GSK126 had no significant effect on the growth of ovarian cancer cells with wild-type ARID1A in culture (PMID: 25686104). | 25686104 |
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
|---|---|---|---|---|---|---|
| NCT02082977 | Phase I | GSK126 | A Study to Investigate the Safety, Pharmacokinetics, Pharmacodynamics and Clinical Activity of GSK2816126 in Subjects With Relapsed/Refractory Diffuse Large B Cell and Transformed Follicular Lymphoma | Terminated | USA | FRA | 1 |
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