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. 2021 Dec 6;26(23):7411. doi: 10.3390/molecules26237411

Table 2.

Name, chemical structure, IC50 values of BTK and clinical phases of irreversible BTKIs under clinical and pre-clinical investigation.

Name Company Chemical
Structure		 IC50 or pIC50
Values on BTK		 Clinical
Phases		 Ref
Evobrutinib Merk graphic file with name molecules-26-07411-i006.jpg 37.9 μM Phase III [29,30]
Spebrutinib Avila Therapeutics/
Celegene		 graphic file with name molecules-26-07411-i007.jpg 0.5 μM Pre-clinical
studies		 [35]
Remibrutinib Novartis graphic file with name molecules-26-07411-i008.jpg 1.3 nM Phase II [36,37]
Tolebrutinib Sanofi/Principia Biopharma graphic file with name molecules-26-07411-i009.jpg 0.4–0.7 nM Phase III [38,39]
Olmutinib Hamni Pharmaceuticals graphic file with name molecules-26-07411-i010.jpg 1.0 nM Phase II [13,40]
Branebrutinib Bristol-Myers
Squibb		 graphic file with name molecules-26-07411-i011.jpg 0.1 nM Phase I [41,42]
TAK-020 Takeda graphic file with name molecules-26-07411-i012.jpg pIC50 > 8.7 Phase I [43,44]
Elsubrutinib AbbVie graphic file with name molecules-26-07411-i013.jpg 0.18 μM Phase II [45,46]
Rilzabrutinib Sanofi graphic file with name molecules-26-07411-i014.jpg 3.1 nM Phase III [4,7,14,47,48]