The re gulators of renin-angiotensin system （RAS） include renin inhibitors ，angiotensin converting enzyme inhibitors，angiotensin Ⅱ receptor blockers ，angiotensin Ⅱ receptor agonists and angiotensin 1-7. This paper summarizes and analyzes the adjuvant effects of RAS regulators on antitumor drugs by searching the literature published from January 1992 to June 2021. The regulators of RAS can reduce the cardiotoxicity ，hematological toxicity and peripheral neurotoxicity of antitumor drugs ， and has renal protective effect ；the regulators of RAS combined with other chemotherapy drugs show favorable effects on promoting chemotherapeutic drugs delivery ，improving anti-angiogenesis and bypass activation of targeted drugs ，enhancing tumor immune response of immune checkpoint inhibitors ，so as to improve therapeutic efficacy of antitumor drugs. The combination of RAS regulators with antitumor drugs is expected to reduce the side effects of antitumor drugs ，enhance its efficacy and improve the prognosis of patients.