Because of the shortage of raw material from the animal sources, a strong interest in the development of synthetic and biotechnology of glycomimetic based drugs has recently emerged. Synthetic heparinomimetics including the chemically synthesized pentasaccharide and its derivatives are in clinical development. Oligosaccharides with both the anti-Xa and IIa activities are developed to mimic the actions of heparin. Other synthetic oligosaccharides are designed to target adhesion molecules, growth factors and regulatory pathways are also developed using fermentation technology. Bacterial and yeast carbohydrates are transformed into products mimicking heparin glycose glycosaminoglycans. Sulfaminoheparosan and pentomannans are currently undergoing pre-clinical and clinical evaluations. Realizing the structure of endogenous proteoglycans, several glycomimetics are developed using semisynthetic approach. Such agents are useful in the management of inflammation, cancer and immunologic disorders. Although relatively weaker as anticoagulants in vitro, these agents are potent in producing the endogenous indirect anticoagulant effects by releasing several mediators such as Tissue Factor Platelet Inhibitor (TFPI). It is therefore possible to design and develop pharmacologically active glycomimetics to target various diseases. It is projected that synthetic glycomimetics will have a major impact in the management of thrombotic and cardiovascular disorders in the near future. This presentation will provide an overview in the recent developments in both the clinical and applied perspectives on the development of glycomimetics.