Preferred Label : Dual IRAK1/4 Inhibitor R906289 Monosodium;
NCIt synonyms : R289 Na; R906289 Monosodium; IRAK1/4 Inhibitor R289 Na;
NCIt definition : An orally bioavailable, monosodium salt form of R906289, a prodrug of R835, a small
molecule inhibitor of interleukin-1 receptor-associated kinases 1 (IRAK1) and 4 (IRAK4),
with potential immunomodulating and anti-inflammatory activities. Upon oral administration,
R906289 is converted to its active metabolite R835. R835 targets, binds to, and inhibits
the activity of IRAK1 and IRAK4. This inhibits lipopolysaccharide (LPS)/Toll-like
receptor 4 (TLR4) signaling and LPS/TLR4-induced proinflammatory cytokine production.
This may inhibit inflammation and immune-mediated cell destruction in inflammatory
and auto-immune diseases where TLR or interleukin 1 receptor (IL-1R) signaling is
overactivated. IRAK1 and IRAK4, serine/threonine-protein kinases, play key roles in
signaling downstream of TLR and IL-1R, and TLR/IL-1R-induced production of proinflammatory
cytokines.;
NCI Metathesaurus CUI : CL1793580;
Origin ID : C188461;
UMLS CUI : C5707793;
Semantic type(s)
- concept_is_in_subset
- has_target
