The occurrence of reproductive infertility has become an increasing concern in the developed world, particularly following the recent trend of attempts at pregnancy later in maternal life. Most existing therapies for infertility, such as clomiphene and gonadotropins, aim to manipulate the traditional components of the hypothalamic-pituitary-gonadal axis. Several secretagogues of gonadotropin-releasing hormone (GnRH) have been identified, including glutamate, neuropeptide tyrosine (NPY) and substance P; however, the broad array of action of these secretagogues in the CNS make them unsuitable as therapeutic targets. In the last 5 years, the Kisspeptin system has emerged as a critical regulator of reproduction and as a putative novel target of therapy for reproductive disorders. This review summarizes the relevant contemporary literature related to Kisspeptin, and assesses the potential applications of this group of peptides as a novel therapeutic target.