Linomide Explained

Linomide (Roquinimex) is a quinoline derivative immunostimulant which increases NK cell activity and macrophage cytotoxicity. It also inhibits angiogenesis and reduces the secretion of TNF alpha.

Linomide has been investigated as a treatment for some cancers (including as adjuvant therapy after bone marrow transplantation in acute leukemia) and autoimmune diseases, such as multiple sclerosis[1] [2] and recent-onset type I diabetes.[3] Several trials have been terminated due to serious cardiovascular toxicity.

Synthesis

Ethyl 2-(methylamino)benzoate is condensed with ethyl malonate. Amine-ester interchange of that compound with N-methylaniline results in formation of the amide linomide.

Notes and References

  1. Weilbach EX, Hartung HP . [Immune modulation in multiple sclerosis: linomide] . German . Der Nervenarzt . 67 . 8 . 701–5 . August 1996 . 8805117 . 10.1007/s001150050044 . 31845910 .
  2. Hedlund G, Link H, Zhu J, Xiao BG . Effects of Linomide on immune cells and cytokines inhibit autoimmune pathologies of the central and peripheral nervous system . International Immunopharmacology . 1 . 6 . 1123–30 . June 2001 . 11407306 . 10.1016/s1567-5769(01)00041-8 .
  3. Gross DJ, Weiss L, Reibstein I, Hedlund G, Dahlén E, Rapoport MJ, Slavin S . The immunomodulator Linomide: role in treatment and prevention of autoimmune diabetes mellitus . International Immunopharmacology . 1 . 6 . 1131–9 . June 2001 . 11407307 . 10.1016/s1567-5769(01)00042-x .

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