A viable cost-effective and isocratic approach employing C-18 column (250 mm • 4.6 mm, 5 lm) based HPLC has been utilized to separate and estimate the drug, tranexamic acid in pharmaceutical formulations. Tranexamic acid contains no p-electrons to act as fluorophore or chromophore hence pre-column derivatization was performed with benzene sulfonyl chloride in aqueous medium at room temperature. The derivatized drug was then estimated using C-18 column by exploiting a 25:75 (v/v) solvent mixture of acetonitrile and 0.1 M ammonium acetate (pH 5.0) as the mobile phase. The flow rate of mobile phase was 1 mL/min and detection was performed at a wavelength of 232 nm using UV detector. Retention time of tranexamic acid was 4.42 min. The method followed linear regression equation in the concentration range of 1-100 lg/mL with coefficient of determination equal to 0.9994. The limit of detection and limit of quantitation were 0.3 and 1 lg/mL, respectively. The relative standard deviation and recovery ranges for tranexamic acid were found to be 0.11-2.47% and 97.60-103.25%, respectively. The suggested method is very sensitive and may have the potential to be used for tranexamic acid detection in medicinal formulations.