Drug intelligence / Profile preview

GSK3915393 + itraconazole

Development stage
Unknown
Lead developer
GSK
Modality
Small Molecules
Administration
Oral, Intravenous (GSK3915393), Intravenous (itraconazole)
01

Overview

GSK3915393 + itraconazole refers to the co-administration of **GSK3915393**, an investigational small molecule inhibitor of transglutaminase 2 (TG2), and **itraconazole**, an approved triazole antifungal agent. - **GSK3915393** is developed by GSK to target TG2, a key enzyme implicated in fibrotic diseases and initially in celiac disease, but now under development for idiopathic pulmonary fibrosis (IPF). Its mechanism of action is selective inhibition of transglutaminase 2, thereby potentially reducing extracellular matrix cross-linking and myofibroblast activation. - **Itraconazole** is commonly used for the treatment of various fungal infections via inhibition of ergosterol synthesis in fungal cell membranes, acting as a potent inhibitor of the cytochrome P450 enzyme CYP3A4. - This combination specifically has been studied in the context of drug-drug interaction (DDI) trials for GSK3915393, as itraconazole is a strong CYP3A4 inhibitor and relevant for understanding the metabolic profile and safety of GSK3915393 in humans. - There is no evidence of a fixed-dose combination, unique product name, or branded product for this specific pairing; rather, it refers to the pharmacological co-administration used for research (primarily DDI studies as part of the Phase 1 program for GSK3915393)[1][2][3][5].

02

Targets

CYP51A1 (Sterol 14α-demethylase)CYP3A4 (Cytochrome P450 3A4)TGM2 (Tissue Transglutaminase 2)

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