Bioorganic and Medicinal Chemistry p. 498 - 509 (2012)
Update date:2022-07-30
Topics:
Rawson, David J.
Ballard, Stephen
Barber, Christopher
Barker, Laura
Beaumont, Kevin
Bunnage, Mark
Cole, Susan
Corless, Martin
Denton, Stephen
Ellis, David
Floc'H, Marion
Foster, Laura
Gosset, James
Holmwood, Frances
Lane, Charlotte
Leahy, David
Mathias, John
Maw, Graham
Million, William
Poinsard, Cedric
Price, Jenny
Russel, Rachel
Street, Stephen
Watson, Lesa
This paper describes our recent efforts to design and synthesise potent and selective PDE5 inhibitors and the use of in vitro predictors of clearance, absorption and permeability to maximise the potential for dose-proportional pharmacokinetics and good oral bioavailability in man. Optimisation of the preclinical profile resulted in the identification of UK-369003 (19a) and its nomination as a clinical candidate. The clinical pharmacokinetic and safety profile has enabled us to progress the compound to test its efficacy in patients with lower urinary tract symptoms (LUTS) associated with benign prostatic hyperplasia (BPH) and a paper describing its efficacy has recently been published.2,3.
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