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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