PRN1008

Rilzabrutinib (PRN1008) is a reversible covalent, selective and oral active inhibitor of Bruton’s Tyrosine Kinase (BTK), with an IC50 of 1.3 nM.

BTK: 1.3 nM (IC₅₀); BMX: 1.0 nM (IC₅₀); ITK: 440 nM (IC₅₀); TEC: 0.8 nM (IC₅₀); RLK: 1.2 nM (IC₅₀); BLK: 6.3 nM (IC₅₀); EGFR: 520 nM (IC₅₀); ERBB2: 3900 nM (IC₅₀); ERBB4: 11.3 nM (IC₅₀)

[1] Smith PF, et al. A phase I trial of PRN1008, a novel reversible covalent inhibitor of Bruton's tyrosine kinase, in healthy volunteers. Br J Clin Pharmacol. 2017 Nov;83(11):2367-2376. DOI:10.1111/bcp.13351
[2] Hill RJ, Bradshaw JM, Bisconte A, Tam D, Owens TD, Brameld KA, Smith PF, Funk JO, Goldstein DM, Nunn PA. Preclinical Characterization of PRN1008, a Novel Reversible Covalent Inhibitor of BTK that Shows Efficacy in a RAT Model of Collagen-Induced Arthritis. Annals of the Rheumatic Diseases 2015; 74(Suppl 2): 216.