Safety, Tolerability, and Pharmacokinetics of SR 49059, a V1A Vasopressin Receptor Antagonist, After Repeated Oral Administration in Healthy Volunteers

The conventional evaluation of safety and tolerability during Phase I may not be sufficient for new exploratory non-peptide receptor antagonists as selective vasopressin (AVP) receptor antagonists. Previous research and validation of surrogate markers considerably enhance the understanding of phase I, and may even contribute with high accuracy to an early approach of dose finding.