Malaria has been a major epidemic that has ravaged millions predominantly in the developing countries of the world with variability in symptoms, causative agents and use of chemotherapy or vector control as preventive measures. Malaria transmission occurs primarily in tropical and subtropical regions in the sub-Saharan Africa, Central and South America. Currently, malaria diagnosis rests mainly on the microscopic detection of parasites in blood samples or rapid diagnostic test (RDT). Preventing drug resistance involves orientation programmes, identification of new treatment modalities, artemisinin (ACT) etc. Treatment failures has been reported for these ACTs leading to an urgency in the need for further novel discoveries and advances in the fight against this menance (antimalarial drug resistance) in developing countries of the world. Understanding the mechanism of action of the antimalarial drugs and most significantly, monitoring the drug resistance to the available antimalarial drugs via regular molecular investigations of resistant markers would definitely aid implementation of effective drug policy.