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midazolam + fenebrutinib
- Development stage
- Unknown
- Lead developer
- Genentech
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
This drug combination consists of midazolam and fenebrutinib (GDC-0853). Fenebrutinib is a potent, highly selective, and non-covalent inhibitor of Bruton's tyrosine kinase (BTK), an enzyme critical for B-cell receptor signaling and myeloid cell activation via Fcγ receptors. Midazolam is a short-acting benzodiazepine that functions as a positive allosteric modulator of the GABA-A receptor, commonly used as a sedative and a sensitive probe for CYP3A4/5 enzymatic activity. This specific combination was evaluated in Phase 1 clinical pharmacology studies by Genentech to characterize the drug-drug interaction potential of fenebrutinib, specifically its effect on the pharmacokinetics of CYP3A substrates. Fenebrutinib is being developed for the treatment of various autoimmune and inflammatory diseases, including multiple sclerosis, systemic lupus erythematosus, and chronic spontaneous urticaria.
- Brand names
- Versed
- Other names
- midazolam + GDC-0853fenebrutinib + midazolam
02
Targets
ABCG2 (Breast cancer resistance protein)GABAA (Gamma-aminobutyric acid receptor)CYP3A4 (Cytochrome P450 3A4)SLCO1B3 (Organic anion transporting polypeptide 1B3)BTK (Bruton tyrosine kinase)OATP1B1 (Organic anion transporting polypeptide 1B1)
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