The review also focuses on the anti-cancer potential of these derivatives against various cancer types, including ovarian cancer, colorectal cancer (CRC), breast cancer, and lung cancer, including the associated targets/pathways such as EGFR, KRAS, p53, tyrosine kinase, Hedgehog (Hh) pathway, etc. The outcome of studies conducted using vitamin D derivatives in combination with established drugs like 5-fluorouracil (5-FU) and tributyrin are also discussed. Here, KRAS is linked to lung cancer.