This chapter focuses on the potential future developments in the field of gonadotrophins, and describes where the pharmaceutical companies are focusing their efforts to provide better, cheaper, and safer molecules. Follicle-stimulating hormone (FSH) purified from urine or prepared through recombinant technology is central to current therapy for infertile couples, and different companies are developing new formulations and new devices to inject the different products. An alternative approach to solve the pharmacological issue about recombinant and urinary products is the route of small molecule or hormone mimetic. Over the past few years, various companies have filed different patent applications claiming a variety of small-molecule leutenizing hormone receptor (LHR) and FSH receptor (FSHR) agonists and antagonists. Two new long-acting gonadotrophins developed by fusing the carboxyterminal peptides (CTP) of human chorionic gonadotropin (hCG) to native recombinant human FSH (hFSH) have been reported. Small-molecule gonadotrophin mimetics are currently reported to be in development.