TABLE 1

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

Company	Product	Indication	Chemistry	Initial Screen^a	Reference
Synovo	CSY1690	Cancer	AZM conjugate	Macrophage IL-10 release and p38 kinase inhibitor	(Burnet et al., 2015)
Synovo	CSY0073	CF, COPD	AZM derivative	Mouse experimental colitis	(Balloy et al., 2014; Mencarelli et al., 2011)
GSK	Compound 38	COPD	AZM derivative	Murine splenocyte LPS-induced IL-6 production	(Bosnar et al., 2012)
GSK	Macrolide-corticoid conjugates (macronolactones) and macrolide-NSAID conjugates	Asthma	AZM conjugate	Glucocorticoid receptor binding and human PBMC cytokine release	Patent WO2004094448 (Tomašković et al., 2013)
Gilead	GS-560660	COPD	AZM derivative	Phagocytosis of H. influenzae by macrophages	(Hodge et al., 2017)
Gilead	GS-459755	CF, COPD	ERY derivative	HNE-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.	EM900		ERY derivative	Monocyte differentiation to macrophages	(Sugawara et al., 2011)
Ranbaxy		Inflammatory diseases	ERY derivative	Human neutrophil LTB4 release, LPS-induced IL-1β release from human blood monocytes	Patent WO2007054904A3
Zambon	Compounds 1 and 2	Inflammatory, respiratory, and gastrointestinal pathologies	Telithromycin derivative	Mouse TPA-induced contact dermatitis	Patent 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.