Structure of TAK-020

oral covalent BTK inhibitor

>80% BTK occupancy <5 mg (Ph. I dose esc.)

from fragment-based screen of 11k cmpds

Journal of Medicinal Chemistry

Takeda, San Diego, CA, USA

The Takeda covalent BTK inhibitor clinical candidate, TAK-020, is a highly selective oral covalent BTK inhibitor with safety and tolerability profiles that are promising for both hematologic malignancies and autoimmune…

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