molecules of the month


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

Structure of TAK-020
1 min read

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 diseases based on a study in healthy volunteers. The molecule originated from a simple triazolone fragment, and overall is a remarkably efficient inhibitor. The triazolone fragment binds in an interesting way to the kinase with the highly polar triazolinone buried near the gatekeeper residue, likely contributing to its high kinase selectivity given that most kinases prefer more lipophilic motifs in that region. TAK-020 is anticipated to be efficacious at a very low dose (<5 mg) and it will be interesting to watch how it progresses in the highly competitive BTK landscape.

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