Bruton’s tyrosine kinase (Btk) plays a critical role in B cell maturation and survival in addition to regulating myeloid cell inflammatory cytokine production, making it an attractive target for the treatment of immunological disorders such as lupus and rheumatoid arthritis (RA).<br/><br/>At Genentech, we have invented GDC-0853, a highly potent, selective, non-covalent Btk inhibitor that is currently in Phase II clinical trials for RA and Lupus. In this presentation, we will describe the SAR, preclinical <i>in vivo</i> Lupus and RA efficacy results, DMPK and toxicology investigations leading up to the discovery and selection of our lead clinical candidate, GDC-0853. Additionally, the initial results from our Phase 1 clinical trials will be shared.

Discovery of GDC-0853: A potent & selective BTK inhibitor for the treatment of lupus & rheumatoid arthritis

253rd National Meeting (2017)

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