TABLE 2.

Experimental and clinical trials with drug targeting H3 methylation modulators in prostate cancer.

Target	Drug	Combination	Tumor type	Status	Trial number	References
EZH2	CPI-1205	Enzalutamide/Abiraterone or Prednisone	mCRPC	active	NCT03480646	Taplin et al. (2018)
	PF06821 497	SOC	CRPC	recruiting	NCT03460977	Pfizer (2018)
	Tazemetostat (EPZ-6438)	Enzalutamide/Abiraterone or Prednisone	mPCa	recruiting	NCT04179864	Epizyme Inc. (2019a)
	SHR2554	Abiraterone/Prednisone or Ezalutamide	mCRPC	terminated	NCT03741712	Jiangsu HengRui Medicine Co. Ltd. (2018)
	DS3201	Ipilimumab	mCRPC	recruiting	NCT04388852	M.D. Anderson Cancer Center (2020)
WDR5–MLL	OICR- 9429	Cisplatin	PCa	experimental	-	Zhou et al. (2021)
Menin-MLL	MI-503	-	CRPC	experimental	-	Brzezinka et al. (2020)
LSD1	CC-90011	Abiraterone, Prednisone	PCa	Not yet recruiting	NCT04628988	Celgene (2020)
	Phenelzine	Monotherapy/Doxetacel	PCa/CRPC	Completed	NCT01253642	OHSU Knight Cancer Institute (2010)
	SP-2577 (Seclidemstat)	-	Advanced solid tumors	Phase I	NCT03895684	Salarius Pharmaceuticals LLC (2019)
G9a	CM-272	-	2D and 3D in vitro models for mCRPC	Not in clinical trial	-	Moreira-Silva et al. (2022)