TABLE 3

Summary of clinical development of drug candidates targeting chemokine receptors

See Figs. 810 for structures of representative clinical candidates.

ReceptorCompanyCompoundAffinityIndicationClinical PhaseStatus
nM
CCR1Schering AG (Berlex)BX 4711.0MS, Psoriasis endometriosisIINo efficacy
CCR1MillenniumMLN 3701MS, Multiple myelomaIINo longer reported
CCR1MillenniumMLN 38972.3RA, Multiple myelomaIINo efficacy in RA
CCR1PfizerCP-481,71564RAIINo efficacy
CCR1AstraZenecaAZD48185.0COPDIINo efficacy
CCR1ChemoCentryx/GSKCCX3541.5RAIIOngoing
CCR1MerckC-4462RAIINo efficacy
CCR1MerckC-6448MSIINo efficacy
CCR2MillenniumMLN 1202aRAIINo efficacy
Atherosclerosis, MSIIOngoing
CCR2IncyteINCB8696MS, LupusINo longer reported
CCR2IncyteINCB32843.7RA, Type II diabetesIINo longer reported
CCR2ChemoCentryxCCX915MSITerminated
CCR2ChemoCentryxCCX1402.3Diabetic nephropathyIIOngoing
CCR2MerckMK-08125.0RA, MSIINo efficacy
CCR2PfizerPF-4136309PainIINo longer reported
CCR2BMSBMS-741672Diabetic neuropathyIIOngoing
CCR2Johnson & JohnsonJNJ-1716686420.0Allergic rhinitisIINo efficacy
CCR3PharmaxisASM8bAsthmaIIOngoing
CCR3GlaxoSmithKlineGSK76699410.0Asthma and allergic rhinitisIINo efficacy
CCR3DupontDPC1682.0AsthmaIDevelopment halted
CCR3BMSBMS-6396230.3AsthmaIOngoing
CCR3NovartisQAP-642Allergic rhinitisIDevelopment halted
CCR3AstraZenecaAZD37788.1Allergic rhinitisIINo longer reported
CCR4AmgenKW-0761aOncologyIIOngoing
CCR4GSKGSK223963310.0AsthmaIOngoing
CCR5PfizerUK-427,857 (Maraviroc)3.0RAIINo efficacy
AIDSApprovedRegistered Drug
CCR5Schering-PloughSCH-C2.0RAIINo efficacy
AIDSIDevelopment halted
CCR5Schering-PloughSCH-D0.45AIDSIIDevelopment halted
CCR5GlaxoSmithKlineGW22396333.0AIDSIIIDevelopment halted
CCR5IncyteINCB94713.1AIDSIIDevelopment halted
CCR5ProgenicsPro 140aAIDSIIOngoing
CCR5TobiraTAK652 (cenicroviroc)3.1eAIDSIIOngoing
CCR5AstraZenecaAZD56720.26RAIINo efficacy
CCR5NovartisNIBR-64650.8AIDSIOngoing
CCR5SangamoSB-728cAIDSIIOngoing
CCR5HGSHGS004aAIDSIOngoing
CCR9ChemoCentryx/GSKCCX282/vercirnon6.0IBD, Crohn’sIIITerminated
CXCR1/
CXCR2Schering-PloughSCH 5271233.9COPDIIOngoing
0.049
CXCR1/
CXCR2DompéReparixin1.0 (CXCR1)Pancreatic islet transplantationIIIOngoing
100 (CXCR2)
CXCR2GlaxoSmithKlineSB-6569335.1COPD, Cystic fibrosisIOngoing
CXCR2GlaxoSmithKlineGSK-1325756BCOPD?IOngoing
CXCR2AstraZenecaAZD-5069BronchiectasisIIOngoing
CXCR3AmgenAMG4878.0PsoriasisIINo efficacy
CXCR4Genzyme/Sanofi-AventisPlerixafor
(AMD3100)74Stem cell mobilization for transplantation in cancer (MM, Non-Hodgkins lymphoma)ApprovedRegistered Drug
CXCR4TaiGenBurixaforStem cell transplantationIIOngoing
CXCR4PolyphorPOL6326Stem cell transplantationIIOngoing
CXCR4MedarexMDX-1338aMultiple myelomaIOngoing
CXCR4BiokineBKT140dStem cell transplantationIOngoing
  • IBD, inflammatory bowel disease; MM, multiple myeloma; RA, rheumatoid arthritis.

  • a Neutralizing monoclonal antibodies.

  • b Antisense oligonucleotide.

  • c Zinc finger nuclease;

  • d Peptide.

  • e Also has potent antagonist activity at CCR2.