Discovery of PF-184298, a dual serotonin/noradrenaline reuptake inhibitor

MEDI 19

Gavin A. Whitlock, gavin.whitlock@pfizer.com, Discovery Chemistry, Pfizer Global Research & Development, Ramsgate Road, Sandwich, United Kingdom, Florian Wakenhut, florian.wakenhut@pfizer.com, Discovery Chemistry, Pfizer Global R & D, Ramsgate Road, Sandwich, United Kingdom, Alan Stobie, Pfizer Global Research and Development, Sandwich Laboratories, Paul V. Fish, Discovery Chemistry, Pfizer Global Research and Development, Sandwich Laboratories, Ramsgate Road, Sandwich, CT13 9NJ, United Kingdom, and M. Jonathan Fray, jonathan_fray@sandwich.pfizer.com, Pfizer Global Research and Development, Sandwich, United Kingdom.
Stress urinary incontinence (SUI) is characterized by the involuntary loss of urine due to a sudden increase in intra-abdominal pressure (eg from coughing, sneezing or exercise). Inhibition of serotonin and noradrenaline reuptake (SNRI) has been shown to be an attractive dual pharmacology mechanism for the treatment of SUI.

This presentation will highlight the SNRI medicinal chemistry program at Pfizer including optimization of potency, selectivity, P450 inhibition, CPY2D6 metabolism and pharmacokinetics, which led to the identification of the SNRI clinical development candidate PF-184298.

The detailed in vitro, in vivo and human pharmacokinetic profile of PF-184298 will be presented.

 

First Time Disclosure of Clinical Candidates
1:30 PM-5:30 PM, Sunday, March 25, 2007 McCormick Place Lakeside -- Room E353 A/B, Level 3, Oral

Division of Medicinal Chemistry

The 233rd ACS National Meeting, Chicago, IL, March 25-29, 2007