Cancer Drug Discovery and Development: New Paradigms for a New Millennium
Edward A. Sausville, J I Johnson, Gordon M. L. Cragg, Shannon Decker · ACS symposium series · 2001
A revolution of information on the causes of the cancer phenotype is resulting in the former "empirical" drug development paradigm being replaced by a "rational" paradigm which emphasizes the effect of a test agent on a molecular drug target rather than on maximal tolerated dose. The new paradigm utilizes tools such as combinatorial chemistry, in vitro target-based testing, and data mining algorithms. Potential new anticancer therapeutics developed using the rational paradigm are now reaching human clinical trials. The optimal path for cancer drug discovery will likely result from a marriage of "informed empiricism" in generating new lead structures and rational design of eventual drug candidates, building on biological and structural data.