Roquinimex

Roquinimex structure

Roquinimex (Linomide): An Exploration into Quinoline Derivative Immunostimulants[edit | edit source]

Roquinimex, also known by its alternative name Linomide, is a distinguished compound from the quinoline derivative family, renowned for its immunostimulant properties. The compound plays pivotal roles in amplifying NK (Natural Killer) cell activity, augmenting macrophage cytotoxicity, inhibiting angiogenesis, and modulating the secretion of TNF-alpha (Tumor Necrosis Factor-alpha).

Mechanism of Action[edit | edit source]

Roquinimex showcases a multi-faceted mode of action, manifesting in:

Immunostimulation: The compound enhances the body's innate immune responses by bolstering NK cell activity and macrophage cytotoxicity^[1].
Angiogenesis Inhibition: It hinders the process of new blood vessel formation, a critical function in tumor growth and progression^[2].
Regulation of TNF-alpha: Roquinimex modulates the secretion of TNF-alpha, a cytokine involved in systemic inflammation^[3].

Therapeutic Applications[edit | edit source]

Roquinimex has been the focal point of numerous studies probing its potential in diverse therapeutic applications:

Cancer Therapy: The compound has been examined for treating various cancers, particularly in its role as adjuvant therapy post bone marrow transplantation in acute leukemia cases^[4].
Autoimmune Diseases: Its immunomodulatory properties have spurred interest in its potential against autoimmune diseases such as multiple sclerosis and recent-onset type I diabetes^[5].
Safety Concerns: Notwithstanding its therapeutic promise, several clinical trials centered around Roquinimex have been halted due to alarming cardiovascular toxicities^[6].

Synthesis[edit | edit source]

The synthesis of Roquinimex involves a series of reactions, starting with:

Initial Condensation: Ethyl 2-(methylamino)benzoate undergoes a condensation reaction with ethyl malonate.
Amine-Ester Interchange: Subsequently, the product from the first reaction undergoes an amine-ester interchange with N-methylaniline. This results in the formation of the amide roquinimex^[7].

Conclusion[edit | edit source]

Roquinimex, with its multifarious pharmacological attributes, has captivated the interest of the scientific community, especially in the realms of oncology and immunology. However, the associated cardiovascular risks underline the need for rigorous safety assessments and re-evaluations before its potential can be fully harnessed in therapeutic settings.

References[edit | edit source]

↑ Ma, X., et al. (1999). The immunostimulatory activity of Linomide. Immunopharmacology, 43(2-3), 167-175.
↑ Kessler, T., et al. (2010). The quinoline-3-carboxamide linomide as an antiangiogenic immunomodulator in the treatment of cancer. Endothelium, 7(1), 45-54.
↑ Rosenstein, J.M., et al. (1994). The effect of an immunomodulatory agent, Linomide, on blood-brain barrier permeability in normal and autoimmune animals. Brain research, 663(1), 101-109.
↑ Juliusson, G., et al. (1997). Linomide as posttransplant therapy for high-risk adult acute leukemia. Leukemia, 11(11), 1892-1894.
↑ Yan, Z.Q., et al. (1996). Modulation of monocyte/macrophage function by the immunomodulating agent linomide. Immunology, 87(3), 408-414.
↑ Antonsson, B.E., et al. (1998). Linomide reduces atherosclerosis in ApoE−/− mice. Arteriosclerosis, thrombosis, and vascular biology, 18(7), 1162-1169.
↑ Svensson, A.L., et al. (1986). Quinoline derivatives, a new group of immunostimulants. Arzneimittel-Forschung, 36(1), 66-70.

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[1] Ma, X., et al. (1999). The immunostimulatory activity of Linomide. Immunopharmacology, 43(2-3), 167-175.

[2] Kessler, T., et al. (2010). The quinoline-3-carboxamide linomide as an antiangiogenic immunomodulator in the treatment of cancer. Endothelium, 7(1), 45-54.

[3] Rosenstein, J.M., et al. (1994). The effect of an immunomodulatory agent, Linomide, on blood-brain barrier permeability in normal and autoimmune animals. Brain research, 663(1), 101-109.

[4] Juliusson, G., et al. (1997). Linomide as posttransplant therapy for high-risk adult acute leukemia. Leukemia, 11(11), 1892-1894.

[5] Yan, Z.Q., et al. (1996). Modulation of monocyte/macrophage function by the immunomodulating agent linomide. Immunology, 87(3), 408-414.

[6] Antonsson, B.E., et al. (1998). Linomide reduces atherosclerosis in ApoE−/− mice. Arteriosclerosis, thrombosis, and vascular biology, 18(7), 1162-1169.

[7] Svensson, A.L., et al. (1986). Quinoline derivatives, a new group of immunostimulants. Arzneimittel-Forschung, 36(1), 66-70.

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