Kinase inhibitors are a significant and continuously developing division of target therapeutics. The drug discovery and improvement efforts have examined numerous attempts to target the signaling pathway of kinases. The Kinase inhibitors have been heralded as a game-changer in cancer treatment. For developing kinase inhibitors as a treatment for various non-malignant disorders like auto-immune diseases, is currently undergoing extensive research. It may be beneficial to investigate whether cell-specific kinase inhibitor administration enhances therapeutic efficacy and decreases adverse effects. The goal of the current review is to gain insight into the role of kinase inhibitors in facilitating effective target drug delivery for the treatment of various anti-inflammatory, auto-immune, and anticancer disorders. The aim of this review is also to shed light on drug discovery approaches for kinase inhibitors, their mode of action, and delivery approaches. The variation in the binding of kinases bestows different target approaches in drug design, which can be employed for designing the targeted molecules. Several target sites have been studied, exceeding the design of drugs for various diseases like cancer, Alzheimer’s, rheumatoid arthritis, etc. Diverse delivery approaches have also been studied for the targeted application of kinase inhibitors.