The lactam-derived PF-06821497 [142] and SHR25 are both orally bioavailable EZH2 antagonists, and currently under investigation in phase I dose-escalation trials on patients with R/R follicular lymphoma and DLBCL (NCT03460977) and R/R mature lymphoid neoplasms (NCT03603951). Here, EZH2 is linked to follicular lymphoma.