Safety, pharmacokinetics, and pharmacodynamics of sofnobrutinib, a novel non‐covalent BTK inhibitor, in healthy subjects: First‐in‐human phase I study

• Published in: Clinical and translational science Vol. 17; no. 11; pp. e70060 - n/a
• Main Authors: Miyamoto, Kyoko, Miller, Robert M., Voors‐Pette, Christine, Oosterhaven, Jart A. F., Dobbelsteen, Marieke, Mihara, Katsuhiro, Geldof, Marian, Sato, Yuji, Matsuda, Naomi, Kirita, Shirou, Sawa, Masaaki, Arimura, Akinori
• Format: Journal Article
• Language: English
• Published: United States John Wiley & Sons, Inc 01.11.2024; John Wiley and Sons Inc; Wiley
• Subjects: Administration, Oral; Adolescent; Adult; Agammaglobulinaemia Tyrosine Kinase - antagonists & inhibitors; Allergies; Arthritis; Autoimmune diseases; Biochemistry; Bruton's tyrosine kinase; Cell activation; Cytokines; Dosage; Dose-Response Relationship, Drug; Drug Administration Schedule; Drug dosages; Electrocardiography; Female; Females; Half-Life; Healthy Volunteers; Hematology; Humans; Investigations; Kinases; Leukocytes (basophilic); Male; Middle Aged; Pharmacodynamics; Pharmacokinetics; Plasma; Protein Kinase Inhibitors - administration & dosage; Protein Kinase Inhibitors - adverse effects; Protein Kinase Inhibitors - pharmacokinetics; Protein Kinase Inhibitors - pharmacology; Pyrimidines - administration & dosage; Pyrimidines - adverse effects; Pyrimidines - pharmacokinetics; Pyrimidines - pharmacology; Therapeutic targets; Urinalysis; Young Adult; Netherlands

Bruton's tyrosine kinase (BTK) is a potential therapeutic target for allergic and autoimmune diseases. This first‐in‐human phase I study evaluated safety, pharmacokinetic, and pharmacodynamic profiles of sofnobrutinib (formerly AS‐0871), a highly selective, orally available, non‐covalent BTK in...