Despite the proliferation of medications and therapies for cancer patients, cancer is an illness that significantly influences the expectancy and quality of life. Globally, there is a severe public health issue with cancer. Up-regulated differentiation, uncontrolled proliferation, and immortality are the most significant characteristics of cancer cells. Polyphenols, flavonoids, carotenoids, alkaloids, and other naturally occurring chemicals obtained from plants can be physiologically active and have various impacts. Crocin and crocetin, two carotenoids found in saffron (Crocus sativus Linn.), have mostly been investigated for their antioxidant characteristics and protective benefits. Being a water-soluble carotenoid and a bioactive component of saffron, crocin has antioxidant, antihyperlipidemic, memory-improving, and tumor growth-inhibiting properties. The current review sheds light on saffron and its phytoconstituents, crocin's anticancer mechanism, crocin in the treatment of various cancers, crocin-based nano drug delivery systems, crocin's toxicity, and safety issues, as well as patents for cancer treatments based on saffron phytoconstituents.