This paper examines the synthesis of mononuclear chelates of cadmium(II), zirconium(IV), zinc(II), as well as copper(II) by the interaction of the antiepileptic drug pregabalin (Preg) in conjunction with 2,2′-bipyridine (Bipy) at a molar ratio of 1:1:1. FT-IR, H NMR, XRD, UV-vis. spectra, mass spectrometry, thermal analyses (TG- DTG), molar conductance, and magnetic moment readings were utilized to figure out how the two ligands coordinated to metal ions. The FT-IR and 1 H NMR spectra demonstrated that Preg functions as a bidentate ligand, coordinating with the metal ions through the oxygen atom of the carboxylic group and the nitrogen atom of the amino group, while Bipy coordinates via the two nitrogen atoms, resulting in the formation of octahedral complexes. Thermodynamic parameters, including Ea, ΔH*, ΔS*, or ΔG*, were derived from TG-DTG curves. XRD data indicated that all compounds were polycrystalline with monoclinic systems. The antimicrobial activity of all compounds has been attempted against several types of bacteria and fungi. Study investigates the impact of Preg and its metal complexes on testicular apoptosis in male Wistar rats. Preg administration led to significant alterations in serum sex hormone levels, including elevated follicle-stimulating- hormone, luteinizing-hormone and prolactin, alongside a marked decrease in testosterone, indicative of testicular toxicity or dysfunction. Immunoblotting revealed upregulation of a pro-apoptotic BAX (Bcl-2-associated-X) protein-(BAX) protein in testicular tissues following Preg exposure. Complexes of Zn(II) and Cu(II) mitigated Preg-induced apoptosis, while Cd(II) complex exacerbated apoptotic response. Findings suggest metal complexes may offer a viable approach to alleviate Preg-induced testicular apoptosis, highlighting the need for further research to optimize therapy while minimizing cytotoxicity.