PF-06826647: A TYK2-Selective Kinase Inhibitor
PF-06826647
TYK2-selective kinase inhibitor (JH1 domain) in Ph. II for inflamm. conditions (oral, QD) from structure-based design J. Med. Chem., Aug. 5, 2020 Pfizer, Cambridge, MA / Groton, CT
Other molecules you may be interested in
NT-0796
NT-0796 is NodThera's pro-drug inhibitor of the NLRP3 inflammasome. NT-0796 is currently in a Ph. Ib/IIa trial in obese individuals at risk of developing atherosclerotic cardiovascular diseases. NT-0796 has the potential to reduce neuroinflammation in Parkinson’s disease. The NLRP3 inflammasome has emerged as a hot target due to its connection to Alzheimer’s disease, Parkinson’s disease, gout, and other diseases. Here is a detailed review of the role of NLRP3 inhibition in treating atherosclerosis, how NT-0796 was identified, and what makes it special, clinical development, and more.
rilzabrutinib (PRN1008)
PRN1008 (rilzabrutinib, Sanofi) is an oral, reversible covalent Bruton’s tyrosine kinase (BTK) inhibitor in a Ph. III trial for immune thrombocytopenia. A simultaneously published inhibitor, PRN473, is in development as a topical treatment for atopic dermatitis. Following target discovery in 1993, and subsequent approval of the first [...]
CVN293
Cerevance’s CVN293 is an oral, CNS-penetrant, selective inhibitor of potassium efflux-mediated NLRP3-inflammasome activation in microglia for the treatment of neurodegenerative disorders. Cerevance’s NETSseq platform was used to discover a microglia-specific potassium efflux channel, KCNK13, which allows modulation of the NLRP3-inflammasome in the CNS without affecting peripheral innate immunity. Read the full article to discover highlights on the CNS-penetration of highly polar compounds and how particle size can be key to oral bioavailability
compound 1
The Janssen non-ATP competitive HPK1 inhibitor, “ compound 1 ,” was identified from a screening cascade specifically looking for allosteric inhibitors, which may provide a selectivity advantage over ATP-competitive starting points. Reviewer Adi Murthy says, “ Specificity may prove challenging for HPK active site inhibitors since it belongs to [...]
compound 23
Context. “Compound 23” (LEO Pharma) is an oral IL-17A protein−protein interaction modulator being developed for psoriasis and other inflammatory diseases . Like most cytokines, the involvement of IL-17A in chronic inflammatory diseases has been well-researched . IL-17A is the key cytokine that mediates psoriasis , and targeting it or its [...]