Half of all cancer treatments worldwide involve the use of Pt chemotherapeutics but despite their wide clinical usage, Pt drugs have severe disadvantages, including cell toxicity. Sunitinib is a FDA approved Tyrosine Kinase Inhibitor which selectively targets renal cell carcinoma due to the overexpression of its receptors such as vascular endothelial growth factor receptor (VEGFR) and platelet derived growth factor receptor (PDGFR). Here, a family of three Pt(IV) prodrugs, based on the clinically approved cisplatin, oxalilplatin and carboplatin, bearing sunitinib-derived axial ligands have been developed with the aim to overcome healthy cell toxicity. This study highlights the first Pt(IV) complexes targeting renal carcinoma tumours overexpressing VEGFR. Conjugation of the sunitinib-based ligand was shown not to jeopardize its kinase inhibitory activity. In vitro cytotoxicity proved the cisplatin prodrug derivative to be 36 times more active to cisplatin chemotherapy and 3D spheroids assays reinforced this superior activity. The cisplatin-based prodrug was tested in vivo against renal carcinoma xenografts, revealing exceptional superior activity to cisplatin control. This work demonstratesthe excellent potential of Pt(IV)-Sunitinib conjugates for the treatment of Renal cell carcinoma, as they display far enhanced tumour reduction and lower systemic toxicity when compared to cisplatin chemotherapy.