Phase I Study of the Novel Enhancer of Zeste Homolog 2 (EZH2) Inhibitor GSK2816126 in Patients with Advanced Hematologic and Solid Tumors.

Timothy A YapJane N WinterLisa Giulino-RothJemma LongleyJuanita LopezJean Marie MichotJohn P LeonardVincent RibragMichael T McCabeCaretha L CreasyMelissa SternTeodora Pene DumitrescuXiaowei WangSteve FreyJennifer Carver Thierry HornerChoon OhAhmed KhaledArindam Dhar Peter W M Johnson

Published in: Clinical cancer research : an official journal of the American Association for Cancer Research (2019)

The MTD of GSK2816126 was established at 2,400 mg, but the dosing method and relatively short half-life limited effective exposure, and modest anticancer activity was observed at tolerable doses.

Keyphrases

signaling pathway
pi k akt
transcription factor
binding protein
cell proliferation