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A considerable body of literature is accumulating regarding the therapeutic potential of androgens in women with sexual dysfunction. Most of the studies point to a beneficial role of androgens in improving sexual function in women with limited adverse events. Nevertheless, use of androgens in women remains highly debated and controversial. With the advent of new testosterone preparations for women, albeit not FDA approved, it is anticipated that renewed interest in androgen therapy in women will emerge. It is expected that the availability of new androgen preparations will spur both consumer interest and scientific interest and will lead to additional basic and clinical research. As new clinical data become available, issues pertaining to safety and efficacy of androgens in management of women with sexual dysfunction will be resolved. The emerging consensus on androgen insufficiency in pre- and post-menopausal women and the prevalence of sexual dysfunction, together with data from clinical and pre-clinical studies necessitate development of new strategies towards evidence-based management of women's sexual dysfunction with androgen therapy. The focus of this review article is to: 1) provide an historical perspective of use of androgen in women, 2) review the basic biochemistry of the biosynthesis and metabolism of androgens in women and 3) summarize new information from clinical studies to provide new insight for potential use of androgens as therapeutic agents in the treatment of women with sexual dysfunction. The overall aim of this review is to discuss the role of androgens in overall women's health, sexual function and dysfunction.