Abstract : A therapeutic target can be defined as the biochemical entity by which a drug exerts its beneficial effects. Historically, most drugs have been used without a precise knowledge of their mechanism of action. The rational drug design for a predefined target has been progressively implemented during the second half of the 20th century. Recent advances in genomics have accelerated the discovery of several targets involved in many pathologies. During the recent period, there has also been a diversification of the types of targets used in therapy. Generally, the proteins modulated by drugs belonged mainly to the families of membrane receptors (receptors coupled to G proteins, ion channels, etc.), nuclear receptors or enzymes. Technological advances in the field of therapeutic antibodies and biotechnologies enabled curative agents to reach previously undruggable targets. In this article, we review these trends and illustrate them by various examples, notably in the field of anticancer drugs, lipid-lowering drugs, gene therapy or antisense therapy.