Human saliva proteomics has proven to be a novel approach in the search for protein biomarkers for non-invasive detection of human cancers. This approach may also have implications within the process of anti-cancer drug discovery. Information from saliva proteomic measurements may contribute to the target discovery and validation, assessment of efficacy and toxicity of candidate drugs, identification of disease subgroups, and prediction of responses of individual patients. In this article, we aim to give a brief overview on human saliva proteome analysis, as well as its applications to cancer biomarker discovery. Potential applications of saliva proteomics in anticancer drug discovery and development will also be discussed.