Table II.

PK and PD of Nonsteroidal Antiandrogens

ID	Compound structure	RBAa (%)	Orally available
R-Bicalutamide		0.4 (73)	F = 0.7 (rat) (1 mg/kg) (74) F = 0.1 (rat) (250 mg/kg) F≈1 (human) (50 mg) (31)
Hydroxy-flutamide		0.1 (73)	Yes
Nilutamide		0.08 (22)	F = 1 (rat) (26)
RU58642		6 (52)	Yes
RU58841		5 (42)	No
BMS-25		N/A	Yes
BMS-7		N/A	Yes
BMS-9		N/A	Yes
LG120907		14 (45)	Yes
LG105		11 (45)	Yes

	Intact male rat model
In vivo half life	Prostate	L.A.	Serum T
17–21 h (rats) (30) 6 days (human) (29)	35% intact level @ 25 mg/kg, po (33)	55% intact level @ 8 mg/kg, sc	3 ng/ml @ 25 mg/kg, po (33)
4–22 h (human) (23)	45% intact level @ 25 mg/kg, sc (53)	70% intact level @ 25 mg/kg, sc (53)	18 ng/ml @ 25 mg/kg, sc (53)
6 h (rat) (26) 6 days (human) (26)	60% intact level @ 30 mg/kg, po (35)	N/A	6 ng/ml @ 25 mg/kg, po (35)
N/A	30% intact level @ 30 mg/kg, po (35)	N/A	7 ng/ml @ 30 mg/kg, po (35)
N/A	N/A	N/A	N/A
N/A	Modest inhibition @ 100 mg/kg, po (40)	Modest inhibition @ 100 mg/kg, po (40)	N/A
N/A	Modest inhibition @ 100 mg/kg, po (40)	Modest inhibition @ 100 mg/kg, po (40)	N/A
N/A	Modest inhibition @ 100 mg/kg, po (40)	Modest inhibition @ 100 mg/kg, po (40)	N/A
N/A	65% intact level @ 30 mg/kg, po (75)	N/A	Intact level @ 40 mg/kg, po (76)
N/A	33% intact level @ 30 mg/kg, po (75)	N/A	N/A

^aRBA: Relative binding affinity compared to DHT.