Resistance to commercially available antimalarial drugs is a public health problem. Since the end of the last century, no new antimalarial drugs have been introduced into clinical practice, and new drug development has been quite disappointing. There is therefore a real need to develop new class of antimalarial drugs that could be used alone or in combination. This review describes the development and recent advances on the preparation of ferrocenic compounds as a new class of antimalarial agents with potential for clinical development.