TYK2/JAK1 Dual Inhibition Platform
The TYK2 and JAK1 signal transduction pathways mediate highly complementary immune and inflammatory signalling events. Dual inhibition of TYK2 and JAK1 can effectively block Th17 cell …
Design of a potent and selective dual JAK1/TYK2 inhibitor
Nov 15, 2024 · Janus kinase (JAK) inhibitors have gathered interest as treatments for several inflammatory and autoimmune diseases. The four first marketed inhibitors target JAK1, with varying …
BHV-8000, a Selective Brain-Penetrant TYK2/JAK1 Inhibitor in ...
Apr 7, 2025 · BHV-8000 is a novel, brain-penetrant, oral small molecule highly selective against the TYK2 and JAK1 enzymes within the JAK-STAT pathway, avoiding the safety liabilities of JAK2/3 …
Brepocitinib, a potent and selective TYK2/JAK1 inhibitor ... - PubMed
Jul 15, 2024 · Brepocitinib is an oral, once-daily, novel, and specific TYK2/JAK1 inhibitor. Brepocitinib's potent inhibition of TYK2 and JAK1 reduces the signalling of pro-inflammatory cytokines, including …
Allosteric TYK2 inhibition: redefining autoimmune disease therapy ...
Aug 14, 2023 · Deucravacitinib, a first-in-class allosteric TYK2 inhibitor, represents a remarkable advancement in the field. Rather than competing at kinase domain catalytic sites as classical JAK1-3 …
Biohaven Enrolls First Patient into Phase 2/3 Trial in Early Parkinson ...
May 29, 2025 · In addition to their well-known roles in inflammatory and autoimmune diseases, TYK2 and JAK1 are also implicated in driving neuroinflammation and neurodegeneration via their effects in …
JAK inhibitor selectivity: new opportunities, better drugs?
Sep 9, 2024 · Januse kinase (JAK) inhibitors show equivalent or superior efficacy compared with biologic DMARDs in several autoimmune and inflammatory diseases. The use of JAK inhibitors has …
Biohaven Enrolls First Patient into Phase 2/3 Trial in Early Parkinson ...
May 29, 2025 · A brain penetrant inhibitor of TYK2/JAK1, such as BHV-8000, has the potential to leverage these validated immune targets to treat brain disorders.
Allosteric TYK2 inhibition: redefining autoimmune disease therapy ...
Deucravacitinib, a first-in-class allosteric TYK2 inhibitor, represents a remarkable advancement in the field. Rather than competing at kinase domain catalytic sites as classical JAK1-3 inhibitors, …
Dual Inhibition of TYK2 and JAK1 for the Treatment of Autoimmune ...
Aug 16, 2018 · JAK1 is important for the γ-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 …