Drug intelligence / Profile preview

fenebrutinib + itraconazole

Development stage
Unknown
Lead developer
Genentech
Modality
Small Molecules
Administration
Oral
01

Overview

GDC-0853 (fenebrutinib) is an orally administered, highly selective, noncovalent, and reversible small molecule inhibitor of Bruton's tyrosine kinase (BTK) developed by Genentech. BTK is a cytoplasmic tyrosine kinase that plays a critical role in B-cell and myeloid cell signaling pathways, which are implicated in the pathogenesis of various autoimmune and inflammatory diseases. The specific combination of GDC-0853 and itraconazole refers to a Phase 1 drug-drug interaction study designed to evaluate the effect of itraconazole, a potent CYP3A4 inhibitor, on the pharmacokinetics of GDC-0853 in healthy volunteers. While GDC-0853 is being advanced in Phase 3 clinical trials for multiple sclerosis and has been studied in Phase 2 for rheumatoid arthritis, systemic lupus erythematosus, and chronic spontaneous urticaria, the combination with itraconazole is used for clinical pharmacology assessment rather than as a therapeutic product.

Other names
GDC-0853 + itraconazolefenebrutinib + itraconazole
02

Targets

CYP3A7 (Cytochrome P450 3A7)BTK (Bruton tyrosine kinase)ABCG2 (Breast cancer resistance protein)OATP1B1 (Organic anion transporting polypeptide 1B1)

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