A high performance liquid chromatography tandem mass spectrometric method was developed and validated cenicriviroc quantification in human plasma and cerebrospinal fluid. The method involved precipitation with acetonitrile and injecting supernatants onto the column. Separation was achieved on an XBridge C18 column with a gradient elution of 0.1% formic acid in water and acetonitrile. Analyte detection was conducted in positive ion mode using SRM. The m/z transitions were: CVC (697.3→574.3) and CVC-d7 (704.4→574.3). Calibration curve ranged from 5-1000 ng/ml for plasma and 0.241-15.0 ng/ml for CSF. The intra and inter day precision and accuracy were <15% for both plasma and CSF across four different concentrations. Cenicriviroc recovery from plasma and artificial CSF was >90%. The method was utilised for the measurement of patients' plasma and CSF samples taking a dose of 50, 150 and 300mg qd.