The synthesis and the electrochemical characterization of copper(II) complex containing one molecule of antiviral drug, valacyclovir (VAL), is reported. In addition to characterization, the electrochemical properties of the copper(II) complex of VAL ([Cu(VAL)Cl2]) were investigated by cyclic voltammetry (CV) using glassy carbon electrode. The redox properties of the metal complex was reversible and exhibited diffusion controlled process depending on pH. The dependence of intensities of currents and potentials on pH, concentration, scan rate, and nature of the buffer was investigated. The oxidation/reduction mechanism was proposed and discussed. Also, the interaction of copper complex of VAL- with calf thymus double-stranded DNA was studied spectrophotometrically (UV-vis) and electrochemically by using CV at glassy carbon working electrode. Additionally, the cytotoxicity activity of complex has been investigated against the bovine herpes virus type I.