Drug intelligence / Profile preview

GSK256066 + azelastine hydrochloride

Development stage
Unknown
Lead developer
GSK
Modality
Small Molecules
Administration
Intranasal
01

Overview

GSK256066 + azelastine hydrochloride is a combination investigational product pairing two agents:\n- **GSK256066**: a highly potent and selective inhaled phosphodiesterase 4 (PDE4) inhibitor, primarily developed for its anti-inflammatory activity in airway diseases. It acts by inhibiting PDE4, resulting in increased intracellular cAMP and suppression of inflammatory mediator release, targeting diseases such as asthma and chronic obstructive pulmonary disease (COPD)[1][2][8].\n- **Azelastine hydrochloride**: a well-established second-generation antihistamine with additional mast cell-stabilizing and anti-inflammatory effects, mainly used for the symptomatic treatment of allergic rhinitis via intranasal administration. It acts as an antagonist to the histamine H1 receptor.\n\nThe combination was evaluated in a phase II clinical trial for seasonal allergic rhinitis, using **intranasal administration** of both compounds over a short-term dosing regimen[3][5]. The rationale is to provide rapid symptomatic relief (via azelastine's antihistaminic action) and prolonged anti-inflammatory benefit (via PDE4 inhibition by GSK256066).

02

Targets

HRH1 (Histamine H1 Receptor)ADRA1A (α1A)KCNH2 (Voltage-gated potassium channel subfamily H member 2)PDE4 (Phosphodiesterase 4A1)HRH3 (Histamine Receptor H3)

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