The aim of this study was to investigate the toxic effects on the rat testis of flutamide, bicalutamide, and cyproterone acetate using histopathological methods. Twenty-four male Sprague-Dawley rats were randomly divided into four groups, control (Group 1), flutamide (Group 2), bicalutamide (Group 3), and cyproterone acetate (Group 4). Physiological saline solution or anti-androgens were administered via oral gavage for 14 days. At the end of the study, the testes were harvested for histological toxic effect scoring. The mean histopathology scores were 0 in Group 1, 0.33 ± 0.81 in Group 2, 1.66 ± 1.36 in Group 3, and 2.93 ± 0.98 in Group 4. The histopathology score in Group 4 was significantly higher than that in Group 1 (p = 0.002), but was not significantly different to those in groups 2 and 3 (p = 0.317 and p = 0.028, respectively). No significant difference was also observed between the other groups. Cyproterone acetate, a steroidal antiandrogen, resulted in significant impairment of testis histology relative to the non-steroidal antiandrogens flutamide and bicalutamide. A non-steroidal agent such as flutamide or bicalutamide should therefore be selected if antiandrogen therapy is to be initiated for reasons such as acne, hirsutism, and paraphilias, particularly in young males.