Figure 2. Pharmacodynamic assessments.
A. Fold-change from baseline in whole blood RNA expression of BET inhibitor target genes CCR1, IL1RN, IL-8, MYC, and GPR183 by ZEN-3694 dose level. B. Correlation between fold change from baseline in whole blood RNA expression of BET inhibitor target genes with AUC0–24 of ZEN-3694 + ZEN-3791 indicates strong PK-PD relationship. C. Gene set enrichment analysis of change from baseline in gene expression by RNA-Seq in paired metastatic tumor biopsies. Down-regulation of MYC signaling pathway is observed in on-treatment versus baseline tumor biopsy.