NRX-0492 is an orally administered compound that efficiently degrades Brutons tyrosine kinase (BTK) by catalyzing its ubiquitylation and subsequent proteasomal degradation, achieving half-maximal degradation concentrations (DC50) of ≤0.2 nM and 90% degradation concentrations (DC90) of ≤0.5 nM. Additionally, NRX-0492 suppresses B-cell receptor (BCR) signaling, transcriptional activities, and chemokine production by linking a noncovalent BTK-binding domain to Cereblon, an adaptor protein within the E3 ubiquitin ligase complex [1].
