Drug intelligence / Profile preview

baricitinib + ketoconazole

Development stage
Unknown
Lead developer
Eli Lilly
Modality
Small Molecules
Administration
Oral
01

Overview

baricitinib + ketoconazole is a theoretical combination of two oral small molecule drugs: baricitinib, a selective Janus kinase (JAK) 1 and 2 inhibitor used primarily to treat moderate to severe rheumatoid arthritis and COVID-19, and ketoconazole, an imidazole antifungal agent. Baricitinib works by inhibiting intracellular signaling related to immune activation and inflammation by blocking JAK1 and JAK2. Ketoconazole inhibits fungal sterol synthesis by blocking lanosterol 14-alpha-demethylase (a cytochrome P450 enzyme), and is also a strong inhibitor of the CYP3A4 enzyme in humans. This drug combination is not currently approved or branded as a fixed-dose therapeutic product.

02

Targets

TYK2 (Tyrosine kinase 2)JAK2 (Janus kinase 2)CYP3A4 (Cytochrome P450 3A4)JAK1 (Janus kinase 1)JAK3 (Janus kinase 3)

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