Table 1.

Key Differences Of Selected Next-Generation AR Antagonists

	Bicalutamide	Enzalutamide	Apalutamide	Darolutamide
AR inhibition	Yes, also a partial agonist	Full antagonist (IC50 219 nM)*	Full antagonist (IC50 200 nM)*	Full antagonist (IC50 26 nM)*
Inhibition of Nuclear Translocation	No	Yes	Yes	Yes
Activation of mutant AR	Yes (W742L)	Yes (F877L)	Yes (F877L)	None described
Increase of serum testosterone levels	Yes	Yes	Yes	No
Blood-brain barrier penetration	Negligible	Yes	Yes	Negligible

Note: *Transactivation assays in AR-HEK293 cells stably expressing full-length AR. Data from Moilanen et al.³⁶

Abbreviations: AR, androgen receptor; IC₅₀, half maximal inhibitory concentration.