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Anisodus tanguticus (Maxim.) Pascher has been documented in Tibetan ethnomedicine. Traditional records indicate that A. tanguticus has traditionally been used to relieve pain, treat parasitic infections, and heal skin wounds caused by viral infections. A. tanguticus is rich in tropane alkaloids, including anisodamine, scopolamine, and atropine, which are pharmacologically active constituents with well-known parasympatholytic effects. These alkaloids have shown promise in controlling cancer cell proliferation and metastasis, with preclinical studies indicating antitumor activity against liver, breast, and colorectal cancers. The extraction of A. tanguticus traditionally involves methods such as juice pressing or boiling; however, modern techniques like ultrasonic, reflux, and supercritical fluid extraction have enhanced alkaloid yield and quality. While the pharmacological properties of A. tanguticus suggest that some constituents of A. tanguticus may have preclinical antitumor relevance, most studies remain preclinical, and clinical data is limited. This review highlights the need for further pharmacological, toxicological, and translational studies. Current evidence suggests that A. tanguticus and several of its constituents exhibit preclinical antitumor activity; however, their clinical relevance remains uncertain, and further pharmacological, toxicological, and clinical validation is required. This narrative review summarizes the traditional use, phytochemical composition, extraction methods, antitumor-related findings, and proposed mechanisms of A. tanguticus, while highlighting the need for further pharmacological, toxicological, and translational studies.