This paper describes the determination of aminocaproic acid in human plasma by simple, sensitive, and rapid liquid chromatography-tandem mass spectrometry (LC-MS/MS) method using aminocaproic D6 acid as the internal standard (ISD). Extraction of aminocaproic acid and ISD was achieved from 200 μL plasma through protein precipitation with acetonitrile. Acetonitrile and 5 mM ammonium acetate buffer in the ratio 60:40 was used as the mobile phase at the flow rate of 1.0 mL/min. The method was developed with a short chromatographic run time of 3.0 min using Ace phenyl column. The retention times of both analyte and ISD were found to be 1.50 ± 0.1 min. The quantification of the separated components was done in positive ion mode by Multiple Reaction Monitoring (MRM) with mass transitions from m/z 132.2 (parent ion) to m/z 79.2 (product ion) for aminocaproic acid and from m/z 138.2 (parent ion) to m/z 74.3 (product ion) for the ISD. The method was validated as per the USFDA guidelines. The linearity was established over the concentration range of 0.3-80 μg/ mL with r2>0.98. The % recovery was 86.69 % and 98.29 %, respectively for aminocaproic acid and ISD. The inter- and intra- day accuracy and precision (%CV) were in the range of 100.91 to 103.80 % and 0.91 to 3.63 %, respectively. The developed method was successfully applied for pharmacokinetic study in twelve healthy adult male subjects under fasting conditions and the results were authenticated by performing incurred sample reanalysis.