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. 2021 Apr 15;11:591386. doi: 10.3389/fonc.2021.591386

Table 1.

CXCR4 antagonists in clinical development.

Drug Name Phase Active Indication Combination Therapy Trial number
Small Molecules
Plerixafor (AMD3100) Phase 3 Myelokathexis NCT02231879
Phase 1 Pancreas, Ovarian, Colon Cancer NCT3277209
Phase 2 Metastasis Pancreatic Cancer Cemiplimab NCT4177810
Phase 2 Wiskott-Aldrich Syndrome, Hematopoietic Stem Cell Transplantation NCT3019809
Phase 2 Acute Myeloid Leukemia, Acute Lymphoid Leukemia Busulfan, Cyclophosphamide NCT2065460
Mavorixafor (AMD11070; X4P-001) Phase 2/3 WHIM Syndrome NCT03005327
Phase 1 Waldenestrom’s Macroglobulinemia Ibrutinib NCT04274738
Phase 1 Melanoma Pembrolizumab NCT02823405
Phase 1/2 Renal Cancer axitinib NCT02667886
USL311 Phase 1/2 Solid Tumors (Phase 1), Relapsed/Recurrent GBM (Phase 2) Lomustine NCT02765165
NOX-A12 Phase 1/2 Metastatic Colorectal Cancer
Metastatic Pancreatic Cancer
Pernbrolizurnab NCT03168139
CX-01 Phase 1 Myelodysplastic Syndromes,
Acute Myeloid Leukemia
Azacitidine NCT02995655
Phase 2 Acute Myeloid Leukemia ldarubicin, Cytarabine NCT02873338
Peptide CXCR4 antagonists
Balixafortide Phase 3 Metastatic Breast Cancer Eribulin NCT03786094
LY2510924 Phase 1 Leukemia Idracibin, Cytarabine NCT02652871
[68Ga]Pentixafor Phase 1 Neuroendocrine Tumors NCT03335670
Early Phase Multiple MyelomaLymphoma NCT03436342
BL-8040 Phase 2 Metastatic Pancreatic
Adenocarcinorm
Pernbrolizurnab NCT02826486
Phase 2 Malignant Neoplasms of Digestive OrgansMetastatic Pancreatic Cancer Pernbrolizurnab NCT02907099
Phase 3 Multiple Myeloma NCT03246529
Phase 1/2 Pancreatic Adenocarcinorm PEGPH20, Cobimetinib,
Atezolizumab, Gemcitabine, Nab-
Paclitaxet Oxaliplatin, Leucovorin,
Fluorouracil
NCT03193190
Phase 1/2 Gastric Adenocarcinorm or Gastroesophageal Junction Adenocarcinorm PEGPH20, Linagliptin, Paclitaxet,
Ramucirumab, 5-Fluorouracil (5-FU)
Leucovorin, Oxaliplatin,
Atezolizurmab, Cobimetinib
NCT03281369
Phase 1/2 CarcinomaNon-Srmll-Cell Lung AtezolizurmhCobimetinih Gemicitabine, Carboplatin,
Pemetrexed, CPI-444, Tazemetostat,
Atezolizumab, Cobimetinib,
RO6958688, DOcetaxel
NCT03337698
Anti-CXCR4 antibodies
Uloccuplumab (MDX-
1338)
Phase 1/2 Waldenstrom's
Macroglobulinemia
lbtutinib NCT03225716
Phase 1/2 Leukemia Cytarabine NCT02305563
ALX-0651 Phase 1 Healthy Volunteers NCT01374503
PF-06747143 Phase 1 Acute Myeloid Leukemia Cytarabine, Daunorubicin, Azacitidine,
Decitabine
NCT02954653