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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, PMID: 31471312).

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Drug Name	Trade Name	Synonyms	Drug Classes	Drug Description
GSK126		GSK2816126\|GSK-126	EZH2 inhibitor 20	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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Molecular Profile	Indication/Tumor Type	Response Type	Therapy Name	Approval Status	Evidence Type	Efficacy Evidence	References
ARID1A inact mut	urinary bladder cancer	sensitive	GSK126	Preclinical - Pdx & cell culture	Actionable	In a preclinical study, GSK126 inhibited cell viability in bladder cancer cell lines harboring ARID1A inactivating mutations in culture and inhibited tumor growth in patient-derived xenograft (PDX) and cell line xenograft models of bladder cancer harboring ARID1A inactivating mutations (PMID: 35852858).	35852858
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
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 dec exp	urinary bladder cancer	sensitive	GSK126	Preclinical - Cell culture	Actionable	In a preclinical study, GSK126 inhibited viability of bladder cancer cell lines with ARID1A knockdown in culture (PMID: 35852858).	35852858
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 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
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

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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 \| GBR \| FRA	0

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