The study evaluated the effect of 5 hormonal regimes on serum levels of high-sensitivity C-reactive protein (hsCRP) and homocysteine (Hcy) in women with polycystic ovary syndrome (PCOS). Women with PCOS received (1) conjugated estrogens and cyproterone acetate (n = 22), (2) 17beta-estradiol and cyproterone acetate (n = 17), (3) ethinyl-estradiol and cyproterone acetate (high dose; n = 20), (4) ethinyl-estradiol plus cyproterone acetate (low dose; n = 12), or (5) ethinyl-estradiol plus desogetrel (n = 12). Both hsCRP and Hcy levels were measured at baseline and after 4, 7, and 12 months. The 17beta-estradiol/cyproterone acetate regime resulted in significant reduction of both hsCRP and Hcy levels (P < .001). The other 4 regimes only resulted in a reduction of Hcy levels (P < .001). In conclusion, the 17beta-estradiol/cyproterone acetate regime had the most favorable effects in women with PCOS regarding serum levels of hsCRP and Hcy.