PF-06700841 tosylate

Description: PF-06700841 tosylate is a potent, selective, and conformationally constrained piperazinyl-pyrimidine Type 1 ATP site inhibitor of TYK2 and JAK1 kinases with IC50 values of 23 nM and 17 nM respectively. PF-06700841 is in Phase II clinical development (NCT02969018, NCT02958865, NCT03395184, and NCT02974868) as a potential therapeutic for the treatment of systemic lupus erythematosus and plaque psoriasis. Cytokine signaling is an important characteristic of autoimmune diseases. Many pro-inflammatory cytokines signal through the Janus kinase (JAK)/Signal transducer and activator of transcription (STAT) pathway. JAK1 is important for the gamma-common chain cytokines, interleukin (IL)-6, and type-I interferon (IFN) family, while TYK2 in addition to type-I IFN signaling also plays a role in IL-23 and IL-12 signaling. Intervention with monoclonal antibodies (mAbs) or JAK1 inhibitors has demonstrated efficacy in Phase III psoriasis, psoriatic arthritis, inflammatory bowel disease, and rheumatoid arthritis studies.

References: J Med Chem. 2018 Oct 11; 61(19):8597-8612; J Clin Pharmacol. 2018 Apr; 58(4):434-447; Conference Paper?in?Journal of the American Academy of Dermatology 76(6) · July 2017; DOI: 10.1016/j.jaad.2017.04.509}

Related CAS#: 1883299-62-4 (free base)