The early characterisation of drug metabolism and pharmacokinetic (DMPK) properties of new chemical entities plays a key role in the pharmaceutical industry's effort to reduce attrition. Specifically, a major goal of early DMPK studies is to accurately predict the behaviour of new chemical entities in humans, thus allowing likely failures to be terminated rapidly and resource to be placed on molecules most likely to succeed. The present review summarises progress over the past several years in the key technologies used in the pharmaceutical industry to achieve these goals: namely, in vivo, in vitro and in silico/computational tools. The limitations of the various assays are discussed, with attention also given to likely future directions in this field.