Activation of the complement system plays a key role in normal inflammatory response to injury but may cause substantial injury when activated inappropriately. The cascade is activated through classical, alternative and lectin pathways. The human complement system is in most cases well controlled by the host, and inappropriate activation and host cell destruction are prevented. The control is mainly mediated by complement regulatory proteins. The use of powerful methodologies in molecular biology, biochemistry and physiology has led to impressive advances in our knowledge of the mechanisms of complement activation and regulation and its role as either a protective or pathogenic factor in human disease. With respect to disease pathogenesis, the complexity of the cascades provides opportunities for several different therapeutic targets within the pathways, and we are about to witness the availability of a variety of complement modulators for specific therapies. This article reviews biological aspects of this important immunological effector mechanism.