Preparation and biological activities of macromolecule-anticancer drug conjugates are reviewed under the following headlines : 1) introduction, 2) characteristics of macromolecular drugs, 3) biological activities of conjugates, 3.1) therapeutic effects enhanced by lysosomotropism, 3.2) therapeutic effects enhanced by slow release, 3.3) decreased side effects, 3.4) overcoming of drug resistance, 3.5) effects against metastasis, 3.6) targeting of drugs to tumors, 4) preparation of conjugates, 4.1) selection of macromolecules and drugs, 4.2) preparation and purification of conjugates, and 5) closing remarks.