ABSTRACT Introduction Corosolic acid (CRS) is a naturally occurring pentacyclic triterpenoid primarily isolated from Lagerstroemia speciosa and other medicinal plants and has attracted growing interest because of its promising anticancer properties. Objectives This review provides a comprehensive synthesis of the botanical sources, biopharmaceutical characteristics, molecular mechanisms of action, toxicological profile, and clinical evidence associated with CRS. Materials and Methods A comprehensive literature search was conducted across major scientific databases, including PubMed, Google Scholar, Web of Science, ScienceDirect, SpringerLink, and Wiley Online, covering studies published up to April 2025. Peer‐reviewed articles investigating the anticancer activity, pharmacology, toxicity, pharmacokinetics, and clinical relevance of CRS were included. Results Preclinical evidence demonstrates that CRS exerts broad‐spectrum anticancer activity by inducing apoptosis, autophagy, ferroptosis, and cytotoxicity, while inhibiting tumor cell proliferation, metastasis, and survival signaling pathways, including PI3K/Akt/mTOR, NF‐κB, STAT3, and YAP/TAZ. Emerging data also highlight its immunomodulatory role, particularly through suppression of Th17‐mediated inflammatory responses, which may further contribute to its antitumor effects. Toxicological evaluations indicate that CRS possesses a favorable safety profile at therapeutic doses; however, its clinical translation is hindered by poor aqueous solubility and limited oral bioavailability. Recent advances in formulation strategies and structural modification approaches show potential for overcoming these limitations. Conclusion Overall, this review integrates current knowledge, identifies critical research gaps, and emphasizes the need for well‐designed clinical trials to establish CRS as a viable multitarget anticancer agent.
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