Although the illness malaria is caused by the asexual blood stages, the presence of gametocytes is directly responsible for the infection of the vector Anopheles, thus perpetuating the plasmodial cycle. Fight against malaria is more than ever a current problem, and the solution will probably go through the development of efficient molecules against gametocytes. Knowledge of the pharmacological properties of antiplasmodials is helpful in term of using relevant molecules to treat malaria and to eradicate this dramatic public health problem. The effects of the major antiplasmodial drugs including artemisinin-based combination therapies on gametocyte load are thus reviewed herein, making the difference whenever possible between the effects on gametocytogenesis and the gametocytocidal activity. Current status on the portfolio of the most promising anti-gametocytes compounds is also presented. A close analysis of the relationship between chemical structure and antiplasmodial activity should help the design of novel antimalarial drugs targeting Plasmodium sexual stages.