molecules of the month

Context. JNJ-64264681 (Janssen) is a covalent Bruton’s tyrosine kinase (BTK) inhibitor being developed for hematological malignancies. The first-in-class irreversible BTKi (ibrutinib) was approved in 2013, while many others have been approved or are in clinical development with potentially reduced off-target effects. We recently covered another covalent BTKi, rilzabrutinib, (PRN1008; Sanofi), currently in Ph. III for immune thrombocytopenia. JNJ-64264681 demonstrates nanomolar oral efficacy in both lymphoma and autoimmune models and improved kinase selectivity. It is currently in early clinical development as both a single agent and combination therapy with an aim to reduce adverse effects and patient relapse rates and improve efficacy compared to other BTKi’s on the market. ibrutinib rilzabrutinib Editor Commentary. This is an interesting example of an oral…