Fenebrutinib in H1 antihistamine-refractory chronic spontaneous urticaria: a randomized phase 2 trial [PDF]
AbstractBruton’s tyrosine kinase (BTK) is crucial for FcεRI-mediated mast cell activation and essential for autoantibody production by B cells in chronic spontaneous urticaria (CSU). Fenebrutinib, an orally administered, potent, highly selective, reversible BTK inhibitor, may be effective in CSU.
Martin Metz, Marcus Maurer
exaly +8 more sources
Understanding the Effect of Hydroxypropyl-β-Cyclodextrin on Fenebrutinib Absorption in an Itraconazole–Fenebrutinib Drug–Drug Interaction Study [PDF]
Cyclodextrins are widely used pharmaceutical excipients, particularly for insoluble compounds dosed orally, such as the oral solution of itraconazole, which is frequently used in clinical drug–drug interaction studies to inhibit cytochrome P450 3A. Since cyclodextrins act by forming inclusion complexes with their coformulated drug, they could have an ...
Leslie W Chinn, Emile Plise, Susan Wong
exaly +4 more sources
Efficacy, Safety, and Pharmacodynamic Effects of the Bruton’s Tyrosine Kinase Inhibitor Fenebrutinib (GDC-0853) in Systemic Lupus Erythematosus: Results of a Phase II, Randomized, Double-Blind, Placebo-Controlled Trial [PDF]
ObjectiveFenebrutinib (GDC‐0853) is a noncovalent, oral, and highly selective inhibitor of Bruton’s tyrosine kinase (BTK). The efficacy, safety, and pharmacodynamics of fenebrutinib in systemic lupus erythematosus (SLE) were assessed in this phase II, multicenter, randomized, placebo‐controlled study.MethodsPatients who had moderately to severely ...
Richard A Furie +2 more
exaly +5 more sources
Population Pharmacokinetics, Efficacy Exposure-response Analysis, and Model-based Meta-analysis of Fenebrutinib in Subjects with Rheumatoid Arthritis [PDF]
AbstractPurposeFenebrutinib (GDC-0853), a Bruton’s tyrosine kinase (BTK) inhibitor was investigated in a Phase 2 clinical trial in patients with rheumatoid arthritis (RA). Our aim was to apply a model-informed drug development (MIDD) approach to examine the totality of available clinical efficacy data.MethodsPopulation pharmacokinetics (popPK) modeling,
Phyllis Chan, Jiajie Yu, Katie Tuckwell
exaly +4 more sources
Absence of Pharmacokinetic Interactions between the Bruton’s Tyrosine Kinase Inhibitor Fenebrutinib and Methotrexate [PDF]
Fenebrutinib (GDC-0853) is an orally administered small molecule inhibitor of Bruton's tyrosine kinase being investigated for treatment of rheumatoid arthritis in patients with inadequate responses to methotrexate (MTX). This study interrogated the potential for pharmacokinetic drug interactions between fenebrutinib and MTX.
Elaine Murray +2 more
exaly +3 more sources
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Recently, the non-covalent Bruton tyrosine kinase (BTK) inhibitor fenebrutinib was presented as a therapeutic option with strong inhibitory efficacy against a single (C481S) and double (T474S/C481S) BTK variant in the treatment of Waldenström macroglobulinemia (WM). However, the molecular events surrounding its inhibition mechanism towards this variant
Aimen Aljoundi, Nader E Abo-Dya
exaly +3 more sources
Fenebrutinib is an orally administered, selective and reversible BTK inhibitor. Metz et al recently published a double-blind, placebo-controlled, phase 2 trial where fenebrutinib (50mg daily, 150mg daily or 200mg twice-daily) or placebo were randomly administered to 93 adults with CSU refractory to up-dosed H 1
Alvaro Carvallo +2 more
openaire +1 more source

