4 minute read
Apr. 19, 2022

Rilzabrutinib: A Billion-Dollar Reversible Covalent Inhibitor from Principia

rilzabrutinib (PRN1008)

oral reversible covalent BTK inhibitor in Ph. III for immune thrombocytopenia from structure-based drug design + opt. J. Med. Chem., March 18, 2022 Principia Biopharma (Sanofi), So. San Francisco, CA

Drug Hunter Team

PRN1008 (rilzabrutinib, Sanofi) is an oral, reversible covalent Bruton’s tyrosine kinase (BTK) inhibitor in a Ph. III trial for immune thrombocytopenia. A simultaneously published inhibitor, PRN473, is in development as a topical treatment for atopic dermatitis.

This article reviews what made the molecule notable, how it works, and how it was discovered.



Other molecules you may be interested in