Drug intelligence / Profile preview

GSK2190915 + fluticasone propionate

Development stage
Phase 2
Lead developer
GSK
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral, Inhalation
01

Overview

GSK2190915 + fluticasone propionate is a combination therapy investigated for the treatment of asthma. GSK2190915 is a potent, high-affinity inhibitor of 5-lipoxygenase-activating protein (FLAP), which blocks the synthesis of leukotrienes and 5-oxo-6,8,11,14-eicosatetraenoic acid (5-oxo-ETE), key mediators in inflammatory pathways implicated in asthma. Fluticasone propionate is an inhaled synthetic glucocorticoid corticosteroid that acts as an anti-inflammatory agent by binding to the glucocorticoid receptor and modulating gene expression to reduce airway inflammation. The combination was studied as an add-on therapy to standard inhaled corticosteroid regimens in patients with uncontrolled asthma. Clinical trials showed that while there was no statistically significant improvement in primary lung function endpoints compared to placebo when adding GSK2190915 to fluticasone propionate, some secondary endpoints such as symptom-free days and reduced use of rescue medication indicated pharmacological activity[1][3][5]. Both components are developed by GSK.

02

Targets

FLAP (Arachidonate 5-lipoxygenase-activating protein)GR (Glucocorticoid receptor)

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