In the last decade, we have been developing some gold(III) derivatives showing interesting antitumor properties and reduced systemic and renal toxicity, compared to the clinically-established reference drug cisplatin. Starting from the rationale at the base of our investigations, this review has been divided into two sections, with respect to our patented first- (aminoderivatives) and secondgeneration (peptidomimetics) potential drugs. Every section describes the in vitro and in vivo anticancer activity of the compounds, chosen as models, towards different types of tumor. In particular, we summarize the results achieved so far, in particular taking into account the latest in-depth studies related to their activity, mechanism of action and toxicological profile. Taken together, our data could open up new prospects for further advanced preclinical pharmacological testing.