BI 705564 / Boehringer Ingelheim - LARVOL DELTA

Bleeding by Bruton Tyrosine Kinase-Inhibitors: Dependency on Drug Type and Disease. (PubMed, Cancers (Basel)) - "However, mild bleeding is frequent in patients with B-cell malignancies treated with the irreversible BTKi ibrutinib and the recently approved 2nd generation BTKi acalabrutinib, zanubrutinib and tirabrutinib, and also in volunteers receiving in a phase-1 study the novel irreversible BTKi BI-705564...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). Remibrutinib, a novel highly selective covalent BTKi, is currently in clinical studies of autoimmune dermatological disorders...By focusing on their pharmacological properties, targeted disease, bleeding side effects and actions on platelets it attempts to clarify the mechanisms underlying bleeding. Specific platelet function tests in blood might help..."

Journal • Review • CNS Disorders • Complement-mediated Rare Disorders • Dermatology • Hematological Disorders • Immunology • Infectious Disease • Inflammatory Arthritis • Lupus • Multiple Sclerosis • Novel Coronavirus Disease • Oncology • Rheumatoid Arthritis • Rheumatology • Thrombocytopenia • Thrombocytopenic Purpura

Safety, pharmacokinetics and pharmacodynamics of BI 705564, a highly selective, covalent inhibitor of Bruton's tyrosine kinase, in Phase I clinical trials in healthy volunteers. (PubMed, Br J Clin Pharmacol) - "BI 705564 showed efficient target engagement through durable TO and inhibition of ex vivo B-cell activation, and PoM through effects on allergic skin responses. Mild bleeding-related adverse events were likely related to inhibition of platelet aggregation by BTK inhibition."

Clinical • Journal • P1 data • PK/PD data • Complement-mediated Rare Disorders • Glomerulonephritis • Immunology • Inflammatory Arthritis • Lupus • Lupus Nephritis • Nephrology • Systemic Lupus Erythematosus