Clinical candidates sharing

A tabular listing (ETA) of all biopharmaceutical studies conducted is recommended. Brief narrative descriptions (e.g., similar to an abstract for a journal article) are to share relevant features and outcomes of each study that provided important in vitro or in vivo data and information relevant to the BA and/or BE of a drug candidate. These narratives can be abstracted from clinical study reports (i.e., the synopsis of reports prepared according to ICE guideline E3) and should include reference to the full report. A comparison of results across studies, using both text and tables, is to pay particular attention to differences in in vitro dissolution, BA, and comparative BA results. This comparison is to consider... 

The discovery and development of a candidate for clinical evaluation is a long process that involves small modifications to a lead compound to improve some of its properties, such as pharmacological activity, selectivity, and pharmacokinetics. This is often achieved by the medicinal chemists by replacing a functional group with groups sharing similar physical or chemical properties and maintaining similar activity, which are defined as bioisosteres. We will hereby provide a historical overview of the development and evolution of the concepts of isosterism and bioisosterism, followed by a selection of successful examples of bioisosteric modifications reported in the literature. 

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