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Enzymes act as biological catalysts in living organisms, by regulating the rate of chemical reactions, without themselves being altered in the process. Enzymes act as a target for drugs for the desired therapeutic effect, which are thereby called biological targets. Enzymes offer unique opportunities for drug design that are not available to cell surface receptors, nuclear hormone receptors, ion channels, transporters. Drugs that function as enzyme inhibitors constitute a significant portion of the orally bioavailable therapeutic agents that are in clinical use today. Likewise, much of drug discovery and development efforts at present are focused on identifying and optimizing drug candidates that act through inhibition of specific enzyme targets. Drugs acting on enzymes can either inhibit them or activate them. Inhibition of enzymes is a strategy which is more commonly used rather than activation of enzymes. 47% of all current drugs inhibit their enzyme targets. Enzyme activity can not only be inhibited; it can also be accelerated through biochemical modification of the enzyme. In this manuscript, the authors provide a system-wise summary of drugs acting on enzymes, microsomal enzymes targeted by drug and newly approved drugs acting on enzymes.