The use of gonadotropin therapy for infertility is now a common practice worldwide. However, the quest to develop safe and effective products was a journey spanning more than a century of research and discoveries. From the first evidence of pituitary regulation of the gonads back in 1910, to the evolution of readily available gonadotropin therapies nowadays. We will review the important milestones that establish current practice, enabling women and men who were considered sterile in the past to conceive and parent offspring. Starting from early attempts to extract and purify gonadotropin preparations from animals, human cadavers, and human menopausal urine to the production of FSH and LH using recombinant DNA technology. This chapter will chronicle the events leading to the development of a safe and effective gonadotropin therapy and offer a glance to future perspectives of this market.