Drug intelligence / Profile preview

GSK-1004723

Development stage
Phase 2
Lead developer
GSK
Modality
Small Molecules
Administration
Intranasal
01

Overview

GSK-1004723 is a potent and selective small molecule antagonist of both the histamine H1 and H3 receptors, developed for intranasal administration. It was investigated primarily as a treatment for allergic rhinitis, including seasonal allergic rhinitis. The drug exhibits high affinity and slow dissociation kinetics at both H1 and H3 receptors, resulting in a long duration of action that supports once-daily dosing. Preclinical studies demonstrated its ability to reverse histamine-induced responses in human bronchus preparations with prolonged antagonism even after drug removal. In clinical trials (up to phase II), intranasal suspensions or solutions of GSK-1004723 were generally well tolerated but showed limited efficacy compared to standard antihistamines like cetirizine, particularly regarding total nasal symptom score and nasal blockage[1][2][3][6][7].

Other names
955359-72-5UNII-S08212J4ZRUNII-S-08212J4ZRUNII-S 08212J4ZR
02

Targets

HRH3 (Histamine Receptor H3)HRH1 (Histamine H1 Receptor)

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