Nonantibiotic macrolide derivatives reported to exhibit immunomodulatory or anti-inflammatory properties

CompanyProductIndicationChemistryInitial ScreenaReference
SynovoCSY1690CancerAZM conjugateMacrophage IL-10 release and p38 kinase inhibitor(Burnet et al., 2015)
SynovoCSY0073CF, COPDAZM derivativeMouse experimental colitis(Balloy et al., 2014; Mencarelli et al., 2011)
GSKCompound 38COPDAZM derivativeMurine splenocyte LPS-induced IL-6 production(Bosnar et al., 2012)
GSKMacrolide-corticoid conjugates (macronolactones) and macrolide-NSAID conjugatesAsthmaAZM conjugateGlucocorticoid receptor binding and human PBMC cytokine releasePatent WO2004094448
(Tomašković et al., 2013)
GileadGS-560660COPDAZM derivativePhagocytosis of H. influenzae by macrophages(Hodge et al., 2017)
GileadGS-459755CF, COPDERY derivativeHNE-induced sodium channel activation in human airway epithelial cells; phagocytosis of H. influenzae by macrophages(Hodge et al., 2017; Tarran et al., 2013)
Taiisho/ Kitasato Inst.EM900ERY derivativeMonocyte differentiation to macrophages(Sugawara et al., 2011)
RanbaxyInflammatory diseasesERY derivativeHuman neutrophil LTB4 release, LPS-induced IL-1β release from human blood monocytesPatent WO2007054904A3
ZambonCompounds 1 and 2Inflammatory, respiratory, and gastrointestinal pathologiesTelithromycin derivativeMouse TPA-induced contact dermatitisPatent WO2008/072034, PCT/IB20067054776
  • ERY, erythromycin; LTB4, leukotriene B4; NSAID, non-steroidal anti-inflammatory drug; PBMC, peripheral blood mononuclear cell; TPA, tetradecanoyl phorbol acetate.

  • aIn addition to bacterial screen.