The present invention belongs to the field of medical chemistry, and relates to an antitumour pharmaceutical composition and use thereof. In particular, the pharmaceutical composition to which the present invention relates comprises two or three ingredients of the following three ingredients A, B and C: A. dipyridamole and/or pharmaceutically acceptable derivatives thereof B. ubenimex and/or pharmaceutically acceptable derivatives thereof C. dexamethasone and/or pharmaceutically acceptable derivatives thereof optionally, the pharmaceutical composition also comprises a pharmaceutically acceptable carrier or excipient. The present invention also relates to a use of the pharmaceutical composition in preparing the antitumour drug and an antitumour method. The antitumour pharmaceutical composition in the present invention achieves the purpose of treating tumours effectively primarily by acting on the tumour microenvironment, and the features of the drug adjusting the tumour microenvironment are that it is acting on multiple targets and multiple paths, which can be expected to relieve the toxic and side effects caused by cytotoxic drugs.La présente invention appartient au domaine de la chimie médicale, et concerne une composition pharmaceutique antitumorale et son utilisation. En particulier, la composition pharmaceutique de la présente invention comporte deux ou trois ingrédients des trois composants suivants A, B et C : A. dipyridamole et/ou des dérivés pharmaceutiquement acceptables de celui-ci B ubénimex et/ou des dérivés pharmaceutiquement acceptables de celui-ci C dexaméthasone et/ou des dérivés pharmaceutiquement acceptables de celle-ci éventuellement, la composition pharmaceutique comprend également un support ou un excipient pharmaceutiquement acceptable. Linvention concerne également une utilisation de la composition pharmaceutique dans la préparation de médicaments antitumoraux et une méthode antitumorale. La composition pharmaceutique antitumorale de la pré