Aritinercept (AUR-200) is a recombinant fusion protein targeting TNFSF13B/BAFF/CD257. Aritinercept neutralizes BAFF and APRIL (TNFSF13), reduces B cell proliferation, suppresses peripheral B cells, lowers serum immunoglobulins. Aritinercept reduces renal damage markers, decreases IFNγ, IL-17A, and anti-dsDNA autoantibodies, and improves survival in a mouse model of SLE. ritinercept can be used for the research of systemic lupus erythematosus [1].
In Vivo, Aritinercept (1-10 mg/kg; s.c.; weekly; 6 weeks) significantly improves survival, reduces proteinuria and renal histologic damage, lowers proinflammatory cytokines, and dose-dependently decreases anti-dsDNA autoantibodies in a mouse model of SLE[1]. Aritinercept (1 mg/kg; s.c.; single dose) suppresses peripheral B cells, and (5-80 mg/kg; s.c.; weekly; 4 weeks) induces sustained reductions in all serum immunoglobulins in healthy cynomolgus monkeys[1].
In Vitro, Aritinercept exhibits high binding affinity (Kd) to human BAFF (117 pM), human APRIL (25 pM), mouse BAFF (31 pM), and mouse APRIL (505 pM) in a cell-free surface plasmon resonance binding assay[1]. Aritinercept potently inhibits human APRIL (IC50 = 0.002 nM), mouse BAFF (IC50 = 1.5 nM), and mouse APRIL (IC50 = 2.7 nM) in a cell-free competitive ELISA, with no detectable inhibition of human BAFF[1]. Aritinercept reduces BAFF and APRIL-costimulated proliferation of human primary B cells and mouse splenocytes[1].
References:
[1]. Morales S, et al. AUR200: An Improved BAFF/APRIL Inhibitor with Increased Potency and Safety for the Treatment of B Cell-Mediated Diseases[C]//ARTHRITIS & RHEUMATOLOGY. 111 RIVER ST, HOBOKEN 07030-5774, NJ USA: WILEY, 2022, 74: 3237-3239.
In Vivo, Aritinercept (1-10 mg/kg; s.c.; weekly; 6 weeks) significantly improves survival, reduces proteinuria and renal histologic damage, lowers proinflammatory cytokines, and dose-dependently decreases anti-dsDNA autoantibodies in a mouse model of SLE[1]. Aritinercept (1 mg/kg; s.c.; single dose) suppresses peripheral B cells, and (5-80 mg/kg; s.c.; weekly; 4 weeks) induces sustained reductions in all serum immunoglobulins in healthy cynomolgus monkeys[1].
In Vitro, Aritinercept exhibits high binding affinity (Kd) to human BAFF (117 pM), human APRIL (25 pM), mouse BAFF (31 pM), and mouse APRIL (505 pM) in a cell-free surface plasmon resonance binding assay[1]. Aritinercept potently inhibits human APRIL (IC50 = 0.002 nM), mouse BAFF (IC50 = 1.5 nM), and mouse APRIL (IC50 = 2.7 nM) in a cell-free competitive ELISA, with no detectable inhibition of human BAFF[1]. Aritinercept reduces BAFF and APRIL-costimulated proliferation of human primary B cells and mouse splenocytes[1].
References:
[1]. Morales S, et al. AUR200: An Improved BAFF/APRIL Inhibitor with Increased Potency and Safety for the Treatment of B Cell-Mediated Diseases[C]//ARTHRITIS & RHEUMATOLOGY. 111 RIVER ST, HOBOKEN 07030-5774, NJ USA: WILEY, 2022, 74: 3237-3239.