Therapeutic peptides can generally be designed to have very high potency and exquisite selectivity for their molecular targets. Peptides also offer a relative safety advantage over small molecules as they are confined to the extracellular space and tend to be used in small doses. However, the design of peptidic drugs with dosing intervals appropriate to the clinical indication and route of administration is challenging.  Examples of tailoring this interval by manipulation of their physicochemical properties and clearance will be discussed. Degarelix, a GnRH antagonist currently on the market for the treatment of prostate cancer is injected s.c. at monthly intervals. FE 203799, a novel GLP-2 analogue has been designed for weekly or biweekly dosing by the subcutaneous route. FE 202158, a selective V1a agonist currently in Phase II for the treatment of vasodilatory hypotension was purposely designed with short half life for rapid up and down titration by intravenous infusion.

Peptidic drugs with tailored duration of action

244th National Meeting (2012)

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