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|Therapy Name||Ibrutinib + Tazemetostat|
|Drug Name||Trade Name||Synonyms||Drug Classes||Drug Description|
|Ibrutinib||Imbruvica||PCI-32765||BTK inhibitor 22 EGFR Inhibitor (Pan) 46 HER2 Inhibitor 24||Imbruvica (ibrutinib) is a selective, irreversible inhibitor of Bruton's tyrosine kinase (BTK), which promotes apoptosis and inhibits B-cell mediated signaling pathways, and has additional activity against ERBB2 (HER2) and EGFR (PMID: 20615965, PMID: 21422473, PMID: 27678331). Imbruvica (Ibrutinib) is FDA approved for use in patients with mantle cell lymphoma, CLL/SLL and CLL/SLL with del 17p, Waldenstroem’s macroglobulinemia, marginal zone lymphoma, and in combination with Rituxan (rituximab) for untreated CLL/SLL (FDA.gov).|
|Tazemetostat||Tazverik||EPZ6438|E-7438|EPZ-6438||EZH2 inhibitor 18||Tazverik (tazemetostat) binds to and inhibits EZH2, resulting in decreased tri-methylation of H3K27, and potentially leading to inhibition of cell proliferation and tumor growth (PMID: 23620515). Tazverik (tazemetostat) is FDA approved for use in patients aged 16 years and older with metastatic or locally advanced epithelioid sarcoma not eligible for complete resection, and in adult patients with relapsed or refractory follicular lymphoma (R/R FL) harboring an EZH2 mutation after 2 prior therapies, and in patients with R/R FL without treatment options (FDA.gov).|
|Molecular Profile||Indication/Tumor Type||Response Type||Therapy Name||Approval Status||Evidence Type||Efficacy Evidence||References|
|EZH2 mutant||diffuse large B-cell lymphoma||sensitive||Ibrutinib + Tazemetostat||Preclinical - Cell culture||Actionable||In a preclinical study, Tazemetostat (EPZ-6438) and Imbruvica (ibrutinib) synergistically inhibited proliferation of diffuse large B-cell lymphoma cell lines harboring EZH2 mutations in culture (PMID: 28835384).||28835384|
|Clinical Trial||Phase||Therapies||Title||Recruitment Status|