tazemetostat

Overview

Tazemetostat is an oral EZH2 inhibitor (histone methyltransferase inhibitor) that blocks H3K27 methylation. It is structurally related to the tool compound EPZ011989 used in preclinical SCLC studies. Tazemetostat is FDA-approved for epithelioid sarcoma and relapsed/refractory follicular lymphoma.

Evidence in the corpus

• Tazemetostat (structurally related to EPZ011989 used in SCLC PDX experiments) is proposed as a clinical EZH2 inhibitor for combination with cisplatin/etoposide or irinotecan in SCLC; tolerability data from 82 NHL patients showed grade ≥3 thrombocytopenia in 11% and grade ≥3 neutropenia in 6%, supporting feasibility of combination with cytotoxic chemotherapy; the paper argues against single-agent activity and recommends combination strategies evaluated early in clinical development PMID:28196596.

Resistance mechanisms

• Not reported in corpus.

Cancer types (linked)

• SCLC (proposed combination strategy)

Sources

• PMID:28196596 — SCLC PDX study; tazemetostat cited as clinical EZH2 inhibitor structurally related to EPZ011989; proposed combination with cisplatin/etoposide or irinotecan to prevent SLFN11 silencing and re-sensitize chemoresistant SCLC.

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