Despite the clinical success of five boronic acid-based organoboron compounds, the literature highlights a critical gap in our understanding of amine-borane adducts, a highly promising class of boron compounds. The objective of this paper is to classify data regarding the mechanisms of action of existing boron-based pharmaceuticals, while assessing the structural, stability, and biological properties of amine-borane adducts as future therapeutic candidates. This analytical review examines organoborane pharmacophores, specifically analyzing the donor-acceptor properties of the B-N bond and how electronic and steric factors influence them. It also summarizes the in vitro and in vivo pharmacological test results for various amine-boranes, including adducts of alpha amino acids, nucleosides, and heterocyclic amines. The study’s core methodologies included evaluating structural activity relationships and testing antitumor, anti-inflammatory, lipid-lowering, and pain-relieving effects in standard preclinical models (e. g., Ehrlich ascites, L1210, P388, HLB, SW480, and edema/pleurisy models). Additionally, cytotoxicity was measured using ED50 values across various tumor cell lines. In summary, amine-borane complexes are a highly promising class of compounds with proven antitumor, anti-inflammatory, and lipid-lowering properties, which are strongly dictated by their structures. Nevertheless, their successful translation into clinical drugs relies on closely examining the stability of the B-N coordination bond and their reactivity under physiological conditions, including hydrolysis, oxidative stress, and interactions with biological nucleophiles in vivo.