Article
A phase I study to evaluate the safety, pharmacokinetics, and pharmacodynamics of PF-06939999 (PRMT5 inhibitor) in patients with selected advanced or metastatic tumors with high incidence of splicing factor gene mutations.
ESMO open - 1 Apr 2024
Rodon J, Rodriguez E, Maitland M L, Tsai F Y-C, Socinski M A, Berlin J D, Thomas J S, Al Baghdadi T, Wang I-M, Guo C, Golmakani M, Clark L N, Gazdoiu M, Li M, Tolcher A W
Abstract excerpt
BACKGROUND: Protein arginine methyltransferase 5 (PRMT5) methylates multiple substrates dysregulated in cancer, including spliceosome machinery components. PF-06939999 is a selective small-molecule PRMT5 inhibitor. PATIENTS AND METHODS: This phase I dose-escalation and -expansion trial (NCT03854227) enrolled patients with selected solid tumors. PF-06939999 was administered orally once or twice a day (q.d./b.i.d.)...
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