Bruton's tyrosin kinase (BTK) is a kinase that functions downstream of multiple receptors in various hematologic cells. The non-catalytic cystein 481 close to ATP binding pocket provides a unique opportunity for designing a covalent inhibitor. Ibrutinib (PCI-32765), a potent BTK inhibitor currently in Phase III clinical trials for lymphoma, has demonstrated remarkable efficacy and very reasonable safety profile. This presentation will discuss our approach and strategies towards designing potent, selective and efficacious covalent BTK inhibitors.

Design and discovery of small molecules covalently inhibiting Bruton's tyrosin kinase

246th National Meeting (2013)

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