Recently, 2D transition metal carbide, nitride, and carbonitrides (MXenes) materials stand out in the field of tumor therapy, particularly in the construction of functional platforms for optimal antitumor therapy due to their high specific surface area, tunable performance, strong absorption of near‐infrared light as well as preferable surface plasmon resonance effect. In this review, we summarize the progress of MXene‐mediated antitumor therapy after appropriate modifications or integration procedures. We discuss in detail the enhanced antitumor treatments directly performed by MXenes, the significant improving effect of MXenes on different antitumor therapies, as well as the MXene‐mediated imaging‐guided antitumor strategies. Moreover, the existing challenges and future development directions of MXenes in tumor therapy are presented.This article is protected by copyright. All rights reserved