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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).|
|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|
|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|