Table 4 —
Pharmacologic agents targeting chemokines and their receptors
| Drug | Pharmacological effects | Clinical indication | References | Stage of development |
|---|---|---|---|---|
| ALX-0651 | Anti-CXCR4 nanobody | Anti-inflammatory | NCT01374503 | Phase 1 trials |
| AMD-11070 (AMD-070) | CXCR4 antagonist | HIV-1 infection | NCT00361101 | Phase 1 trials |
| AMD-3465 | CXCR4 antagonist | Antineoplastic HIV-1 infection Anti-inflammatory | PMID: 23484027 PMID: 16011832 PMID: 19540208 | Preclinical |
| AZD-2423 | CCR2 antagonist | Neuropathic pain COPD | NCT01200524 NCT01215279 | Phase 2 trials |
| AZD-4818 | CCR1 antagonist | COPD | PMID: 20466530 | Phase 2 trials |
| BAY86-5047 (ZK-811752 or BX-471) | CCR1 antagonist | Endometriosis | PMID: 28168715 | Phase 2 trials |
| BL-8040 | CXCR4 antagonist | Stem cell mobilization | NCT03246529 | Phase 3 trials |
| Cal-1 (LVsh5/C46) | Lentiviral vector delivering shRNA down-regulating CCR5 | HIV-1 infection | NCT03593187 | Phase 2 trials |
| CCL2-LPM | CCR2 antagonist | IgA nephropathy | NCT00856674 | Phase 1 trials |
| CCX-140B | CCR2 antagonist | FSGS | NCT03703908 | Phase 2 trials |
| CCX-354-C | CCR1 antagonist | Rheumatoid arthritis | NCT01027728 | Phase 2 trials |
| CCX-507 | CCR9 antagonist | IBD | ChemoCentryx, Inc. website | Phase 2 trials |
| CCX-587 | CCR6 antagonist | Psoriasis | ChemoCentryx, Inc. website | Phase 2 trials |
| CCX-872 | CCR2 antagonist | Antineoplastic | NCT02345408 | Phase 2 trials |
| Cenicriviroc (tbr-652) | CCR2 antagonist | NAFLD | NCT02217475 NCT01338883 | Phase 2 trials |
| CNTX-6970 | CCR2 antagonist | Chronic pain disorders | NCT03787004 | Phase 2 trials |
| CP-481,715 | CCR1 antagonist | Rheumatoid arthritis | PMID: 17713973 | Phase 2 trials |
| CTCE-9908 | CXCR4 antagonist | Antineoplastic | PMID: 24472670 | Phase 2 trials |
| Danirixin | CXCR2 antagonist | COPD | NCT02130193 | Phase 2 trials |
| Elubrixin (SB-656933) | CXCR2 antagonist | IBD CF | NCT00748410 NCT00903201 | Phase 2 trials |
| Emapticap pegol (NOX-E36) | Anti-CCL2 aptamer | Diabetic nephropathy | NCT01547897 PMID: 25901662 | Phase 2 trials |
| INCB-3284 | CCR2 antagonist | Rheumatoid arthritis | PMID: 24900329 | Phase 2 trials |
| Ladarixin | CXCR1/2 antagonist | Diabetes mellitus | NCT02814838 | Phase 2 trials |
| Leronlimab (PRO 140) | Anti-CCR5 antibody | HIV-1 infection Antineoplastic | NCT02483078 NCT03838367 | Phase 3 trials |
| Maraviroc | CCR5 antagonist | HIV-1 infection HCV infection | NCT00844519 NCT02881762 | Approved (Selzentry® and Celsentri®) |
| Mavorixafor (AMD070 or X4P-001) | CXCR4 antagonist | WHIM syndrome Antineoplastic | NCT03995108 NCT02823405 | Phase 3 trials |
| MLN3897 | CCR1 antagonist | Rheumatoid arthritis | PMID: 19950299 | Phase 2 trials |
| Mogamulizumab | Anti-CCR4 antibody | Antineoplastic | NCT02705105 | Phase 2 trials |
| MSX-122 (Q-122) | CXCR4 antagonist | Vasomotor symptoms | NCT03518138 | Phase 2 trials |
| Nanobodies | Anti-CXCR2 nanobodies | Anti-inflammatory | PMID: 25468882 | Preclinical |
| Navarixin (MK-7123 or SCH-527123) | CXCR2 antagonist | Asthma COPD | NCT01006161 NCT01068145 | Phase 2 trials |
| PA-401 | CXCR1/2 antagonist | COPD | NCT01627002 | Phase 1 trials |
| Plerixa for (AMD3100) | CXCR4 antagonist | Stem cell mobilization HIV-1 infection Antineoplastic | PMID: 30776910 PMID: 9427609 PMID: 28817386 | Approved (Mozobil®) |
| Plozalizumab (MLN-1202) | Anti-CCR2 antibody | Antineoplastic | NCT01015560 | Phase 2 trials |
| Reparixin | CXCR1/2 antagonist | Diabetes mellitus Antineoplastic | NCT01220856 NCT02001974 | Phase 2 trials |
| TG-0054 | CXCR4 antagonist | Stem cell mobilization | NCT02104427 | Phase 2 trials |
| TPI-ASM8 | CCR3 antisense oligonucleotide | Asthma | NCT00550797 | Phase 2 trials |
| Ulocuplumab (BMS-936564 or MDX-1338) | Anti-CXCR4 antibody | Antineoplastic | NCT03225716 | Phase 2 trials |
| Vercirnon (Traficet-EN, CCX-282 or GSK1605786A) | CCR9 antagonist | Crohn’s disease | NCT01536418 | Phase 3 trials |
| Vicriviroc (SCH-417690 or MK-7690) | CCR5 antagonist | HIV-1 infection Antineoplastic | NCT00686829 NCT03631407 | Phase 3 trials |
CCL = CC-chemokine ligand; CCR = CC-chemokine receptor; COPD = chronic obstructive pulmonary disease; CXCR = CXC-chemokine receptor; FSGS = focal segmental glomerulosclerosis; HCV = hepatitis C virus; HIV = human immunodeficiency virus; IBD = inflammatory bowel disease; NAFLD = non-alcoholic fatty liver disease; NCT = ClinicalTrials.gov number; PMID = PubMed identifier; shRNA = short hairpin ribonucleic acid; WHIM = warts, hypogammaglobulinemia, infections and myelokathexis.