Table 1.

Inhibition of aromatization by aminoglutethimide, second-generation aromatase inhibitors, and third-generation aromatase inhibitors

Aromatase inhibitor	Dose	Percent inhibition of aromatization (mean)
Aminoglutethimide class
Aminoglutethimide [62]	1000 mg qd	90.56
Rogletimide [62]	200 mg b.i.d.	50.6
Rogletimide [62]	400 mg b.i.d.	63.5
Rogletimide [62]	800 mg b.i.d.	73.8
Second-generation aromatase inhibitors
Fadrozole (CGS 16949A) [49]	1 mg b.i.d.	82.4
Fadrozole (CGS 16949A) [49]	2 mg b.i.d.	92.6
Formestane (4-hydroxyandrostendione) [63]	250 mg every 14 days	84.8
Formestane (4-hydroxyandrostendione) [63]	500 mg every 14 days	91.9
Formestane (4-hydroxyandrostenedione) [64]	125 mg qd	62.3
Formestane (4-hydroxyandrostenedione) [64]	125 mg b.i.d.	70.0
Formestane (4-hydroxyandrostenedione) [64]	250 mg qd	57.3
Formestane (4-hydroxyandrostenedione) [65]	500 mg weekly	91.3
Formestane (4-hydroxyandrostenedione) + aminoglutethimide [65]	500 mg weekly (4OHA) + 1000 mg qd (AG)	94.2
Third-generation aromatase inhibitors
Anastrozole [66]	1 mg qd	96.7a
Anastrozole [66]	10 mg qd	98.1a
Anastrozole [58]	1 mg qd	97.3a
Letrozole [58]	2.5 mg qd	>99.1a
Exemestane [67]	25 mg qd	97.9a

^aGeometric mean.

AG, aminoglutethimide.