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Updated: Jun 20, 2025

Kinase Inhibitor Screening In Self-assembled Human Protein Microarrays
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BTK inhibitors: past, present, and future

Allison Cool1, Tiffany Nong1, Skye Montoya1

  • 1Sylvester Comprehensive Cancer Center at the University of Miami Miller School of Medicine, Miami, FL, USA.

Trends in Pharmacological Sciences
|July 18, 2024
PubMed

Bruton's tyrosine kinase (BTK) inhibitors have revolutionized the treatment landscape for B cell lymphomas such as chronic lymphocytic leukemia (CLL). The first-in-class BTK inhibitor ibrutinib has recently been succeeded by covalent BTK inhibitors that are safer but still face challenges of resistance mutations. The noncovalent BTK inhibitor pirtobrutinib was recently approved for relapsed and refractory CLL, and whether noncovalent BTK inhibitors will supplant covalent BTK inhibitors as upfront treatment options either alone or in combination will be determined. Meanwhile, newer BTK inhibitors and BTK degraders are vying for their place in the potential future landscape of B cell cancers as well as autoimmune diseases. This review will cover the latest progress in BTK inhibitor development and where the field is moving in light of these recent discoveries.

Keywords:
BTK inhibitorBruton’s tyrosine kinasedegradernovel therapyresistance mechanismssmall molecule inhibitor

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