Abstract: The present invention provides coatings or coating compositions for implantable or insertable medical devices containing one or more polymers and a combination of an immunosuppressant agent and an anti-neoplastic agent. In some embodiments, the coatings or coating compositions of the invention control sustained-release of the immunosuppressant agent and the anti-neoplastic agent for at least about 4 weeks. The present invention also provides implantable or insertable medical devices and other drug delivery or eluting systems containing a coating or coating composition of the invention and uses thereof.