Drug design stability

J. L. Fauchere, C. Thurieau, Evaluation of the Stability of Peptides and Pseudopeptides as a Tool in Peptide Drug Design , in Advances in Drug Research , Vol. 23, Ed. B. Testa, Academic Press, London, 1992, p. 127- 159. 

In the enkephalin studies we began to see how theoretical techniques can be used to generate conformations of related molecules. With the results from GnRH and vasopressin we saw how flexible these molecules are and how the conformational fluctuations and dynamics of these molecules can be studied. We also saw how the relative stabilities of conformations of a molecular fragment can be influenced by conformational constraints of the whole molecule. In the following section we will present some ideas on how these calculations can be incorporated into a conformational based approach to drug design. 

Section 7.2.2 describes practical guidelines to design stability studies that are aligned with the guidance for industries provided by the FDA [9]. A different approach can be used depending on the characteristics of the drug product and with an appropriate scientific justification. 

Evaluation of the stability of peptides and pseudopeptides as a tool in peptide drug design, 23, 127... 

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