Small molecule inhibitors targeting m⁶A regulators have emerged as promising candidates for cancer therapy. m⁶A modification, a common RNA modification, is involved in various physiological processes and is dysregulated in cancer, contributing to tumor progression, metastasis, drug resistance, and immune responses. This review summarizes the classification and functions of m⁶A regulators, their roles in cancer, and the development of small molecules targeting these regulators. The review highlights the potential of m⁶A regulators as drug targets and provides insights into their mechanisms of action, structure-activity relationships, and antitumor effects. It also discusses the therapeutic potential of m⁶A modification in cancer, emphasizing its role in tumor proliferation, metastasis, resistance, and prognosis. The review covers the functions of m⁶A writers, erasers, and readers, their interactions with cancer cells, and the development of small molecule inhibitors targeting these regulators. The review also discusses the potential of m⁶A modification in cancer therapy, highlighting its role in tumor cell proliferation, metastasis, and resistance. The review provides a comprehensive overview of the current state of research on m⁶A regulators and their potential as targets for cancer therapy.Small molecule inhibitors targeting m⁶A regulators have emerged as promising candidates for cancer therapy. m⁶A modification, a common RNA modification, is involved in various physiological processes and is dysregulated in cancer, contributing to tumor progression, metastasis, drug resistance, and immune responses. This review summarizes the classification and functions of m⁶A regulators, their roles in cancer, and the development of small molecules targeting these regulators. The review highlights the potential of m⁶A regulators as drug targets and provides insights into their mechanisms of action, structure-activity relationships, and antitumor effects. It also discusses the therapeutic potential of m⁶A modification in cancer, emphasizing its role in tumor proliferation, metastasis, resistance, and prognosis. The review covers the functions of m⁶A writers, erasers, and readers, their interactions with cancer cells, and the development of small molecule inhibitors targeting these regulators. The review also discusses the potential of m⁶A modification in cancer therapy, highlighting its role in tumor cell proliferation, metastasis, and resistance. The review provides a comprehensive overview of the current state of research on m⁶A regulators and their potential as targets for cancer therapy.