Pharmaceutical evaluation of early development candidates "the 100 mg-approach".

Early development candidates are often selected for pre-clinical and clinical development based primarily on pharmacological and toxicological data. In order to choose the best compounds from a biopharmaceutical point of view, physicochemical parameters such as solubility, dissolution rate, hygroscopicity, lipophilicity, pKa, stability, polymorphism and particle characteristics need to be evaluated as early as possible and above all with the highest accuracy. However, the low amounts of drug substance available in early development often compromise data quality, and therefore, hamper an early pharmaceutical assessment. This article summarises the Aventis approach on early pharmaceutical compound profiling with the aim of providing a high quality assessment requiring not more than 100 mg of drug substance. In particular, the evaluation criteria, process and miniaturised analytical technology that can be applied for this purpose are discussed.