<p>Current efforts in anticancer drug discovery and development are focused on the synthesis and identification of novel complexes that can efficiently and selectively act on DNA and modulate the functions of target proteins. Triorganotins (R₃SnX), as one group of tin complexes, are among the most studied metal-based complexes in the field of anticancer drug development. These compounds have been reported to exhibit promising anticancer activity and provide several potential advantages, including a larger overall surface area, which contributes to increased lipophilicity and consequently higher cytotoxic effects in cancer cells. However, there is still a lack of information on the direct therapeutic targets of triorganotins, their in-depth understanding and useful therapeutic strategies. This review summarizes and critically evaluates current findings regarding triorganotin compounds in oncology research, emphasizing their potential interaction with RXR signaling pathways and the challenges associated with translating these findings into therapeutic practice.</p> Graphical abstract <p></p>