The advent of rapid DNA sequencing technologies is generating vast quantities of raw genomic information ranging from in-depth analysis of the expressed genes to complete sequencing of genomes at an increasing rate (bioinformatics). However, it is the functional characterisation of a specific gene product that is the key limiting factor for validation as targets for high throughput assay development. The challenge is to obtain the raw genomic information from parasites of economic importance and to effectively integrate broad technologies such as gene disruption and over-expression, DNA arrays, proteomics, antisense RNAs, with bioinformatics in a timely fashion to identify relevant biological targets. Screening of validated targets in a strategy that includes large numbers of chemistries with high diversity and predictive in vitro and in vivo assays should permit the successful identification of novel chemical entities with high specificity to the target parasite. It is proposed that this rational approach will permit the identification of new antiparasitic therapies able to surpass the current toxicological, environmental, and economic challenges of the marketplace.