Roquinimex

Title: Roquinimex
CAS Registry Number: 84088-42-6
CAS Name: 1,2-Dihydro-4-hydroxy-N,1-dimethyl-2-oxo-N-phenyl-3-quinolinecarboxamide
Additional Names: N-phenyl-N-methyl-1,2-dihydro-4-hydroxy-1-methyl-2-oxoquinoline-3-carboxamide; 1,2-dihydro-4-hydroxy-N,1-dimethyl-2-oxo-3-quinolinecarboxanilide
Manufacturers' Codes: LS-2616
Trademarks: Linomide (Pfizer)
Molecular Formula: C18H16N2O3
Molecular Weight: 308.33
Percent Composition: C 70.12%, H 5.23%, N 9.09%, O 15.57%
Literature References: Biological response modifier. Prepn: E. Eriksoo et al., EP 59698; eidem, US 4738971 (1982, 1988 both to AB Leo). Immunopharmacology: A. Tarkowski et al., Immunology 59, 589 (1986). Mechanism of action study: E.-L. Larsson et al., Int. J. Immunopharmacol. 9, 425 (1987). Clinical evaluation in cancer patients: J. C. S. Bergh et al., Cancer Invest. 15, 204 (1997).
Properties: Crystals from pyridine, mp 200-204°.
Melting point: mp 200-204°
Therap-Cat: Antineoplastic.
Keywords: Antineoplastic; Immunomodulators.
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Roquinimex
Roquinimex.svg
Systematic (IUPAC) name
4-hydroxy-N,1-dimethyl-2-oxo-N-
phenyl-1,2-dihydroquinoline-3-carboxamide
Clinical data
Legal status  ?
Pharmacokinetic data
Half-life 26-42 hours
Identifiers
CAS number 84088-42-6 YesY
ATC code L03AX02
PubChem CID 55197
UNII 372T2944C0 YesY
Chemical data
Formula C18H16N2O3 
Mol. mass 308.331 g/mol
 YesY (what is this?)  (verify)

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

Roquinimex 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 and recent-onset type I diabetes. Several trials have been terminated due to serious cardiovascular toxicity.