MXene, a novel class of two‐dimensional (2D) materials, has garnered widespread attention from researchers worldwide due to its remarkable physicochemical properties. Its exceptional physical, chemical, optical, and electronic characteristics have opened up exciting possibilities for its application in biomedical fields. The easily modifiable surface makes it particularly attractive to be used in nanomedicine as the surface can be made hydrophilic, with facile drug loading, for imaging, anti‐microbial and photothermal applications. To fully harness its potential in biomedical field, a comprehensive understanding of its toxicological effect is of utmost importance. This review presents a concise introduction to MXene, encompassing commonly employed synthesis procedures, followed by an in‐depth exploration of biomedical studies conducted on diverse MAX and MXene phases. The use of MXene has been discussed as a cancer theranostic agent followed by its toxicity evaluation in microorganisms, zebrafish, in vitro, and in vivo toxicity. Additionally, the review emphasizes the need to advance and standardize the toxicity study. This review provides an overview on the various toxicological aspects related to the MXene nanostructures and advocate their utilization in the near future.This article is protected by copyright. All rights reserved