Results 101 to 110 of about 580 (130)

Fenebrutinib in H1 antihistamine-refractory chronic spontaneous urticaria: a randomized phase 2 trial [PDF]

open access: yesNature Medicine, 2021
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]

open access: yesClinical Pharmacology and Therapeutics, 2020
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]

open access: yesArthritis and Rheumatology, 2021
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]

open access: yesPharmaceutical Research, 2020
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]

open access: yesJournal of Pharmacology and Experimental Therapeutics, 2019
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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Battling BTK mutants with noncovalent inhibitors that overcome Cys481 and Thr474 mutations in Waldenström macroglobulinemia therapy: structural mechanistic insights on the role of fenebrutinib

Journal of Molecular Modeling, 2022
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 and BTK inhibition: unveiling a new target for the treatment of chronic spontaneous urticaria

Allergy, 2022
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

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