Malaria has been, and remains, one of the biggest global health concerns as far as infectious diseases are concerned, with yearly incidence and mortality figures running into millions. One of the major drawbacks to the control of this disease has been the emergence of drug resistant strains of the causative agent, which limits the successful use of many clinically available antimalarial drugs. This review discusses chloroquine resistance; it highlights some of the proposed molecular mechanisms of chloroquine resistance, but dwells more on efforts at reversing chloroquine resistance and the concept of chloroquine resistance-reversal agents.