Recent advancements in theranostic properties of carbon nanodots have positioned them as a promising tool in cancer examination. Their distinctive physicochemical properties offer diverse benefits, making them a compelling option for potential theranostic applications. The benefits of carbon nanodots include biocompatible behavior, surface conjugation and functionalization abilities, and adjustable size, making them a targeted nanoplatform for drug delivery and bioimaging of cancerous tumor cells. However, several challenges must be addressed to realize their full potential, such as understanding pharmacokinetics and biodistribution patterns comprehensively, addressing potential safety and toxicity concerns and developing robust synthesis methods to improve their therapeutic responses. This chapter aims to provide a succinct review of research on carbon nanodots within the fields of medicinal and biomedical sciences, emphasizing the available opportunities and current obstacles in utilizing them as a novel nanoplatform for cancer treatment employing therapeutic and diagnostic imaging.