Drug intelligence / Profile preview

GSK706769 + ketoconazole

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

Overview

GSK706769 + ketoconazole is a combination of the investigational drug **GSK706769** and the antifungal **ketoconazole**. GSK706769 is a small molecule developed for clinical use primarily in rheumatoid arthritis; its action includes occupancy and modulation of the C-C chemokine receptor type 5 (CCR5). Ketoconazole is a well-known antifungal agent and a strong inhibitor of the drug-metabolizing enzyme CYP3A4. When used together, ketoconazole can profoundly alter the pharmacokinetics of GSK706769 if metabolized by CYP3A4, raising concerns for safety and interactions. There is no evidence the combination is marketed or approved; any co-administration would be in a clinical research or experimental context with strict monitoring, given the potential for drug interactions, including increased drug exposure and cardiac risks such as QT prolongation[1][2][3][4][5][6].

Other names
GSK706769GSK-706769GSK 706769Nizoral
02

Targets

CCR5 (C-C chemokine receptor type 5)CYP3A4 (Cytochrome P450 3A4)

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