Deacetylation of chitin affords chitosan, a polymer, widely studied for its pharmaceutical and nonpharmaceutical applications. The hurdle in comprehending these applications is its limited solubility. Carboxymethylation of chitosan helps to surmount this hurdle with its improved solubility in water. Though there is ample of research related to carboxymethyl chitosan (CMC) the focused review of the topic is unavailable. Hence an attempt is made in this review to cover the recent findings pertaining to synthesis, characterization of CMC and its applications especially in pharmaceutical field. CMC has been synthesized by ways as direct alkylation, reductive alkylation, Michael addition and characterized by FTIR, NMR spectroscopy, and DSC, titrimetry, viscometry, gel permeation chromatography, X-ray diffraction and capillary zone electrophoresis. The carboxymethyl group can be present at O or N or both the atoms of chitosan molecule. The CMC possess modulated physical and biological properties as chelating, sorption, moisture retention, cell functioning antioxidant, antibacterial, antiapoptotic etc. CMC is used in sustained or controlled release drug delivery, pH responsive drug delivery, DNA delivery as permeation enhancer etc. CMC can be further modified with alkylation, acylation, and grafting. Carboxyalkylation of chitosan yield carboxyethyl, carboxybutyl chitosans. These analogues of CMC may be helpful in substantiating the applications of chitosan.