Btk Inhibitors: A Medicinal Chemistry and Drug Delivery Perspective

• Published in: International journal of molecular sciences Vol. 22; no. 14; p. 7641
• Main Authors: Brullo, Chiara, Villa, Carla, Tasso, Bruno, Russo, Eleonora, Spallarossa, Andrea
• Format: Journal Article
• Language: English
• Published: Basel MDPI AG 16-07-2021; MDPI
• Subjects: Autoimmune diseases; Binding sites; Bioavailability; Bruton's tyrosine kinase; Bruton’s kinase; Btk inhibitors; cancer treatment; Chronic infection; Clinical trials; Drug delivery; Enzymes; Hydrogen bonds; ibrutinib; Kinases; Leukemia; Ligands; Literature reviews; Lymphoma; Mutation; Protein-tyrosine kinase; Proteins; Review; Severe acute respiratory syndrome coronavirus 2; Targeted cancer therapy; Tyrosine; United States > US
• ISSN: 1422-0067; 1661-6596; 1422-0067
• DOI: 10.3390/ijms22147641

In the past few years, Bruton’s tyrosine Kinase (Btk) has emerged as new target in medicinal chemistry. Since approval of ibrutinib in 2013 for treatment of different hematological cancers (as leukemias and lymphomas), two other irreversible Btk inhibitors have been launched on the market. In the attempt to overcome irreversible Btk inhibitor limitations, reversible compounds have been developed and are currently under evaluation. In recent years, many Btk inhibitors have been patented and reported in the literature. In this review, we summarized the (ir)reversible Btk inhibitors recently developed and studied clinical trials and preclinical investigations for malignancies, chronic inflammation conditions and SARS-CoV-2 infection, covering advances in the field of medicinal chemistry. Furthermore, the nanoformulations studied to increase ibrutinib bioavailability are reported.