Table 2.

Chemokine–receptor antagonists with therapeutic potential for cardiovascular disease

Compound	Target	Study outcome	References
TAK779	CCR5/CXCR3	Reduction of atherosclerosis in mice	van Wanrooij et al (2005)
NBI-74330	CXCR3	Reduction of atherosclerosis in mice	van Wanrooij et al (2008)
SB-517785-M	CXCR2	Reduced arteriolar leukocyte arrest in rats	Navab et al (2004)
MLN1202	CCR2	Reduction of plasma CRP levels in patients	Gilbert et al (2011)
CCX140	CCR2	Phase II clinical trial completeda,b	Charo & Taub (2011)
INCB-3344	CCR2	No reduction of atherosclerosis in mice	Aiello et al (2010)
ABX-IL8	CXCL8	Poor results in a Phase II clinical trialb	Mahler et al (2004)
ABN-912	CCL2	Ineffective in a Phase II clinical trialb	Haringman et al (2006)
HGS004	CCR5	Phase I clinical trial completedb	Lalezari et al (2008)
MDX-1100	CXCR3	Phase II clinical trial completedb	Yellin et al (2009)
AMD3465	CXCR4	Reduction of neointima formation, increase of atherosclerosis in mice	Karshovska et al (2008), Zernecke et al (2008)
Met-RANTES	CCR1, -5	Reduction of neointima formation and atherosclerosis in mice	Schober et al (2002), Veillard et al (2004)
[44AANA47]-CCL5	CCL5	Reduction of atherosclerosis and ischemia–reperfusion injury in mice	Braunersreuther et al (2010, 2008)
PA508	CCL2	Reduction of neointima formation and ischemia–reperfusion injury in mice	Liehn et al (2010)
M-T7	Chemokinesc	Inhibition of transplant vasculopathy in mice	Dai et al (2010)
CKBP	Chemokinesd	Not yet assessed	Smith et al (2005)
Evasin-1, -3, -4	Chemokinese	Reduction of ischemia–reperfusion injury in mice (Evasin-3)	Montecucco et al (2010)
MKEY	CCL5/CXCL4f	Reduction of atherosclerosis in mice	Koenen et al (2009)
Anti-CCL17-Ab	CCL17	Reduction of atherosclerosis in mice	Weber et al (2011)

CRP, C-reactive protein; Ab, antibody.

^aResults from animal models not disclosed by company (ChemoCentryx).

^bClinical trials were performed for diseases other than atherosclerosis.

^cM-T7 inhibits chemokine binding to GAGs.

^dCKBP inhibits various chemokines of the CC-, CXC- and CX₃C-classes.

^eEvasins inhibit various chemokines of the CC- and CXC-classes.

^fMKEY inhibits the heterophilic interaction between CCL5 and CXCL4.