Table 1.

Pharmacological and clinical properties of FDA approved second-generation anti-androgens.

	Compound	Target	IC50	Adverse effects	Applications	FDA pipeline
Biosynthesis Inhibitors	Abiraterone acetate	CYP17	72 nM (cell free) (27)	Hypertension, hypokalemia, edema, hepatotoxicity, adrenocortical insufficiency (33)	AAP for metastatic CRPC, and metastatic high-risk castration-sensitive PC (33–35, 37–39)	Approved
Androgen Receptor Blockers	Enzalutamide	AR antagonist	36 nM (LNCaP cells) (40)	Fatigue, hypertension, hot flush, dizziness, nausea and falls; elevated risk of seizure (41)	non-metastatic CRPC, metastatic CRPC (41–47)	Approved
	Apalutamide	Selective and competitive AR inhibitor	16 nM (cell free) (48)	Fatigue, hypertension, rash, diarrhea, nausea, weight loss, arthralgia, fall, hot flush, decrease in appetite, features and peripheral edema (49, 50)	non-metastatic CRPC (49–53)	Approved
	Darolutamide	AR antagonist	26 nM (AR-HEK293 cells) (54)	Fatigue, nausea, pain in extremities, rashes, ischemia and heart failure (55–58)	non-metastatic CRPC (58)	Approved