Roquinimex

Roquinimex (Linomide) is an orally active immunomodulator with antineoplastic, anti-inflammatory, and antiangiogenic activity. Roquinimex suppresses TH1 lymphocyte cytokines (IL-2, IFN-γ), promotes TH2 lymphocyte cytokines (IL-4, IL-10), increases NK cell, activated monocyte, and T cell activity. Roquinimex blocks macrophage TNF-α production and suppresses IL-1/IL-6 secretion. Roquinimex exhibits in vivo antitumour activity, suppresses rodent autoimmune disease signs, and ameliorates murine colitis and psoriasis. Roquinimex can be used for the research of leukemia, inflammatory bowel disease, multiple sclerosis, and psoriasis^{[1][2][3][4][5]}. In Vitro:Roquinimex (1-100 μg/mL; 48 h) significantly reduces the number of MBP-reactive IFN-γ secreting peripheral blood MNC, but does not affect PHA-reactive IFN-γ secreting cells^[3].
Roquinimex (100 μg/mL; 48 h) reduces pro-inflammatory TNF-α mRNA expression across MBP-, PPD-, and PHA-reactive peripheral blood MNC, while increasing anti-inflammatory TGF-β and IL-10 mRNA expression in MBP- and PHA-reactive cells, with no effect on IFN-γ, LT, or IL-4 mRNA expression^[3]. In Vivo:Roquinimex (300 mg/kg/day; s.c.; daily; 8 days; strated from day 3 pre-DSS challenge) ameliorates dextran sodium sulfate (DDS) (HY-116282C)-induced murine colitis^[2].
Roquinimex ameliorates manifestations of lupus-like disease in MRL/lpr mice^[3].
Roquinimex (p.o.) provides complete protection from insulitis and maintains normal glucose tolerance for over 40 weeks in NOD mice^[3].
Roquinimex (0.5-1% w/w; topical; twice daily; 8 days) exerts antipsoriatic effects in Imiquimod (HY-B0180)-induced mice^[5].