Tyrosine Kinases are enzymes that catalyse the phosphorylation of the tyrosine residues of their substrates and activate downstream pathways involved in cellular proliferation. Their overexpression/hyper-activity is implicated in numerous different cancerous cell lines. Small molecule Tyrosine Kinase Inhibitors (TKi’s), such as Imatinib, Erlotinib and Sunitinib have been developed as targeted anti-cancer chemotherapeutics but, at the moment, their clinical usage is hindered due to acquired and innate resistance and/or dose limiting side effects. Recently, Metal-Tyrosine Kinase Inhibitor conjugates have become a promising field to overtake these drawbacks since the TKi’s show potential to improve selectivity and pharmacological properties of metal-based drugs, overcoming the resistance associated with current TKi’s. Metal-Tyrosine Kinase Inhibitor conjugates further find applications is several biological fields as dual-modal activity drugs, pro-drug systems and selective metal theragnostics. In this review, advancements over the past decade in the field of metal based-TKi conjugates are discussed and insights are provided to successfully develop metal – TKi conjugates. Three main TK targets are discussed, EGFR (Epidermal Growth Factor Receptor), PDGFR (Platelet Derived Growth Factor Receptor) VEGFR (Vascular Endothelial Growth Factor Receptor). Future perspectives and applications of this promising research area are also outlined.