TABLE 1 

Monotherapy clinical stage covalent BTK kinase inhibitors

CompoundCompanyStage of DevelopmentaPrimary Therapeutic AreaReference
Ibrutinib (Imbruvica)J&J, AbbVieApprovedOncologyByrd et al. (2015)
Acalabrutinib (ACP-196)Acerta PharmaPhase 3OncologyByrd et al. (2016)
BGB-3111BeiGenePhase 3OncologyTam et al. (2015)
Spebrutinib (CC-292)CelgenePhase 2AutoimmuneEvans et al. (2013)
Evobrutinib (M2951)Merck SeronoPhase 2AutoimmuneGrenningloh (2016)
PRN-1008PrincipiaPhase 2AutoimmuneSmith et al. (2015)
LY3337641 (HM-71224)LillyPhase 2AutoimmunePark et al. (2016)
M7583Merck SeronoPhase 1/2OncologyBender et al. (2016)
Tirabrutinib (GS-4059)GileadPhase 1OncologyWalter et al. (2016)
AC-0058TAACEA BiosciencesPhase 1Autoimmune
  • a Development stage of most advanced clinical program, based on ClinicalTrials.gov. Additional potential covalent BTK inhibitors include CT-1530, BMS-986195, and DTRMWXHS-12.