Drug intelligence / Profile preview

GSK3923868 + itraconazole

Development stage
Phase 1
Lead developer
GSK
Modality
Small Molecules
Administration
Oral, Inhalation
01

Overview

GSK3923868 + itraconazole is a combination of two drugs: GSK3923868, an investigational small molecule inhibitor of phosphatidylinositol 4-kinase (PI4K), and itraconazole, a marketed antifungal agent and potent cytochrome P450 3A4 (CYP3A4) inhibitor. This combination is studied to evaluate the potential pharmacokinetic interaction where itraconazole, by inhibiting CYP3A4, may affect the blood concentrations of GSK3923868. GSK3923868 is under development primarily for chronic obstructive pulmonary disease (COPD) and respiratory tract infections, including rhinovirus (common cold), with a mechanism that disrupts viral replication in the lung, thereby potentially reducing exacerbations in at-risk populations such as those with COPD or asthma. Itraconazole's use in studies with GSK3923868 is specifically for its known effect on drug-metabolizing enzymes to characterize GSK3923868 pharmacokinetics[1][2][3][5][8][9].

02

Targets

CYP51A1 (Sterol 14α-demethylase)PI4KA (PI4Kα)PI4KB (Phosphatidylinositol 4-kinase beta)

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