Abstract: The era of cancer cell-cycle therapeutics has come. Proteins that directly regulate cell cycle progression, such as cyclin-dependent kinases (CDKs), checkpoint kinases(CHKs), Aurora kinases, Polo-like kinases, and the WEE1 kinase, are the main targets of cellcycle therapeutics. In addition to the regulation of G1-S-phase progression, cell-cycle therapeutics also trigger anti-tumor immunity, regulate metabolism, and control transcription reprogramming. Combinations of cell cycle therapeutics with hormone therapy, phosphatidylinositol 3-kinase (PI3K) inhibitors, epidermal growth factor receptor (EGFR) inhibitors, and autophagy inhibitors provide new therapeutic strategies for cancer treatment. Cancer cell-cycle therapeutics constitute a novel strategy for precision oncology in the age of integrative genomics. This review basically summarizes the targets and mechanisms of cancer cell-cycle therapeutics.