Effects of Urotensin II Receptor Antagonist, GSK1440115, in Asthma.

ABSTRACT:

Background

Urotensin II (U-II) is highly expressed in the human lung and has been implicated in regulating respiratory physiology in preclinical studies. Our objective was to test antagonism of the urotensin (UT) receptor by GSK1440115, a novel, competitive, and selective inhibitor of the UT receptor, as a therapeutic strategy for the treatment of asthma.

Methods

Safety, tolerability, and pharmacokinetics (PK) of single doses of GSK1440115 (1-750 mg) were assessed in a Phase I, placebo controlled study in 70 healthy subjects. In a Phase Ib study, 12 asthmatic patients were randomized into a two-period, single-blind crossover study and treated with single doses of 750 mg GSK1440115 or placebo and given a methacholine challenge.

Results

Administration of GSK1440115 was

SUBMITTER: Portnoy A 

PROVIDER: S-EPMC3638148 | biostudies-literature | 2013

REPOSITORIES: biostudies-literature