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Androgen plays an essential role in the pathophysiology of acne. The combination with anti-androgen agents may be an ideal option for the treatment of female patients with acne who poorly respond to antibiotics and tretinoins regardless of their blood level of androgens, although the exact therapeutic mechanism has not been well understood up to now. Anti-androgen agents can be classified into 4 groups, i.e., androgen receptor antagonists, adrenal gland-derived inhibitors on androgen production, ovary-derived inhibitors on androgen production, and enzyme inhibitors. Topical anti-androgen agents may become a hot spot in future research on the treatment of acne. This paper presents the advances in therapeutic mechanisms and modalities of anti-androgen treatment of acne.