Drug intelligence / Profile preview

GSK2881078 + itraconazole

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

Overview

GSK2881078 + itraconazole is a combination of two drugs: **GSK2881078**, a nonsteroidal, selective androgen receptor modulator (SARM) developed for the prevention or treatment of muscle wasting (sarcopenia, cachexia) in patients with chronic and acute illnesses, and **itraconazole**, a triazole antifungal agent commonly used for systemic fungal infections. GSK2881078 promotes lean muscle mass accrual by modulating the androgen receptor, and its pharmacokinetics can be influenced by CYP3A4 inhibitors such as itraconazole. The combination has been specifically studied in the context of evaluating drug-drug interaction, with itraconazole used to assess the impact of CYP3A4 inhibition on GSK2881078 pharmacokinetics. There is no primary therapeutic indication for the combination beyond this interaction assessment in clinical pharmacology studies[1][3][4].

02

Targets

AR (Adrenergic receptors)CYP51A1 (Sterol 14α-demethylase)

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