fenebrutinib

inhibits Bruton's tyrosine kinase; structure in first source

Also Known As:

2-(3'-(hydroxymethyl)-1-methyl-5-((5-(2-methyl-4-(oxetan-3-yl)piperazin-1-yl)pyridin-2-yl)amino)-6-oxo-1,6-dihydro-(3,4'-bipyridin)-2'-yl)-7,7-dimethyl-3,4,7,8-tetrahydro-2H-cyclopenta(4,5)pyrrolo(1,2-a)pyrazin-1(6H)-one; GDC-0853

Networked: 20 relevant articles (1 outcomes, 8 trials/studies)

Relationship Network

Bio-Agent Context: Research Results

Heterocyclic Compounds: 198
- 1-Ring Heterocyclic Compounds
  - Pyridines: 88
    - Pyridones: 14
      - fenebrutinib: 20
  - Piperazines: 26
    - fenebrutinib: 20

Experts

1.	Chinn, Leslie W: 5 articles (11/2021 - 01/2018)
2.	Tuckwell, Katie: 4 articles (10/2021 - 01/2020)
3.	Liu, Lichuan: 4 articles (08/2020 - 01/2017)
4.	Chan, Phyllis: 3 articles (08/2022 - 01/2020)
5.	Galanter, Joshua: 3 articles (11/2021 - 04/2020)
6.	Morimoto, Alyssa M: 3 articles (10/2021 - 01/2018)
7.	Crawford, James J: 3 articles (08/2020 - 01/2017)
8.	Johnson, Adam R: 3 articles (08/2020 - 01/2017)
9.	Katewa, Arna: 3 articles (08/2020 - 01/2017)
10.	Reif, Karin: 3 articles (08/2020 - 01/2017)

Related Diseases

1.	Waldenstrom Macroglobulinemia (Macroglobulinemia) 10/12/2022 - "Battling BTK mutants with noncovalent inhibitors that overcome Cys481 and Thr474 mutations in Waldenström macroglobulinemia therapy: structural mechanistic insights on the role of fenebrutinib." 10/12/2022 - "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). "
2.	Rheumatoid Arthritis 08/01/2022 - "Two case studies provided examples in applications of MBMA in biologics (durvalumab + tremelimumab for safety) and small molecule (fenebrutinib for efficacy) to support drug development decision-making in two different but well-studied disease areas, i.e., oncology and rheumatoid arthritis, respectively.Important" 01/01/2020 - "Population Pharmacokinetics, Efficacy Exposure-response Analysis, and Model-based Meta-analysis of Fenebrutinib in Subjects with Rheumatoid Arthritis [corrected]." 01/01/2020 - "The complete title is "Population Pharmacokinetics, Efficacy Exposure-response Analysis, and Model-based Meta-analysis of Fenebrutinib in Subjects with Rheumatoid Arthritis" The original article has been corrected." 01/01/2020 - "Correction to: Population Pharmacokinetics, Efficacy Exposure-response Analysis, and Model-based Meta-analysis of Fenebrutinib in Subjects with Rheumatoid Arthritis." 01/01/2018 - "Taken together, the safety and PK/PD data support GDC-0853 evaluation in rheumatoid arthritis, lupus, and other autoimmune or inflammatory indications."
3.	Systemic Lupus Erythematosus (Libman-Sacks Disease) 10/01/2021 - "The efficacy, safety, and pharmacodynamics of fenebrutinib in systemic lupus erythematosus (SLE) were assessed in this phase II, multicenter, randomized, placebo-controlled study. " 01/01/2017 - "GDC-0853 ((S)-2-(3'-(hydroxymethyl)-1-methyl-5-((5-(2-methyl-4-(oxetan-3-yl)piperazin-1-yl)pyridin-2-yl)amino)-6-oxo-1,6-dihydro-[3,4'-bipyridin]-2'-yl)-7,7-dimethyl-3,4,7,8-tetrahydro-2H-cyclopenta[4,5]pyrrolo[1,2-a]pyrazin-1(6H)-one) is a selective and reversible oral small-molecule BTK inhibitor in development for the treatment of rheumatoid arthritis and systemic lupus erythematosus. " 10/01/2021 - "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." 01/01/2021 - "However, an increasing number of trials instead addresses autoimmunity and inflammation in multiple sclerosis, rheumatoid arthritis, pemphigus and systemic lupus erythematosus with the use of either irreversibly binding inhibitors, e.g., evobrutinib and tolebrutinib, or reversibly binding inhibitors, like fenebrutinib. "
4.	Autoimmune Diseases (Autoimmune Disease) 01/01/2022 - "A number of reversible non-covalent BTK inhibitors, including MK1026/ ARQ531, LOXO305, fenebrutinib are at different stages of clinical trials for autoimmune diseases. " 12/10/2019 - "We explored the potential to prevent FcγRIIA-induced platelet activation by BTK inhibitors (BTKi's) approved (ibrutinib, acalabrutinib) or in clinical trials (zanubrutinib [BGB-3111] and tirabrutinib [ONO/GS-4059]) for B-cell malignancies, or in trials for autoimmune diseases (evobrutinib, fenebrutinib [GDC-0853]). "
5.	Pemphigus (Pemphigus Vulgaris) 01/01/2022 - ""Next-generation" BTK inhibitors such as remibrutinib and fenebrutinib entered clinical development for chronic spontaneous urticaria (CSU); rilzabrutinib and tirabrutinib are being studied as potential treatments for pemphigus. " 01/01/2021 - "However, an increasing number of trials instead addresses autoimmunity and inflammation in multiple sclerosis, rheumatoid arthritis, pemphigus and systemic lupus erythematosus with the use of either irreversibly binding inhibitors, e.g., evobrutinib and tolebrutinib, or reversibly binding inhibitors, like fenebrutinib. " 03/04/2021 - "These include the brain-penetrant irreversible tolebrutinib and evobrutinib (against multiple sclerosis), the irreversible branebrutinib, the reversible BMS-986142 and fenebrutinib (targeting rheumatoid arthritis and lupus erythematodes), and the reversible covalent rilzabrutinib (against pemphigus and immune thrombocytopenia). "

Related Drugs and Biologics

1.	Agammaglobulinaemia Tyrosine Kinase
2.	evobrutinib
3.	acalabrutinib
4.	tirabrutinib
5.	Histamine Antagonists (Antihistamines)
6.	Adalimumab (Humira)
7.	ibrutinib
8.	ARQ531
9.	zanubrutinib
10.	NF-kappa B (NF-kB)

Related Therapies and Procedures

1.	Therapeutics
2.	Resuscitation