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DRUG CLASS:

CXCR4 antagonist

6d
HSCT: Mozobil for Autologous Hematopoietic Stem Cell Transplantation (clinicaltrials.gov)
P2, N=100, Recruiting, Thomas Jefferson University | Not yet recruiting --> Recruiting
Enrollment open
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Neupogen (filgrastim) • plerixafor
10d
Photo-immunomodulatory multifunctional nanoliposomes targeting myeloid derived suppressor cells augment antitumor immunity for colon cancer. (PubMed, Colloids Surf B Biointerfaces)
To address this, we developed a TME-responsive nanoliposome for the co-delivery of the photosensitizer chlorin e6 (Ce6) and the immunomodulatory agent AMD3100...This profound antitumor effect was driven by a significant enhancement of dendritic cell (DC) maturation (31.1 %) and a 1.62-fold increase in tumor infiltration of CD8 + T cells, coupled with a 76.11 % reduction in MDSC accumulation. In conclusion, this multifunctional nanoliposome, which synergizes immunogenic PDT with targeted MDSC regulation, presents a highly effective strategy for colon cancer treatment and opens a new avenue for advanced photoimmunotherapy.
Journal
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CD8 (cluster of differentiation 8) • CXCL12 (C-X-C Motif Chemokine Ligand 12) • HMGB1 (High Mobility Group Box 1) • CALR (Calreticulin)
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plerixafor
21d
A Study of Mavorixafor in Participants With Congenital and Acquired Primary Autoimmune and Idiopathic Chronic Neutropenic Disorders Who Are Experiencing Recurrent and/or Serious Infections (clinicaltrials.gov)
P3, N=176, Recruiting, X4 Pharmaceuticals | Trial completion date: Aug 2026 --> Nov 2027 | Trial primary completion date: Jul 2026 --> Sep 2027
Trial completion date • Trial primary completion date
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Xolremdi (mavorixafor)
25d
CXCR4 Inhibition Induces Tumor Necrosis by Selectively Targeting the Proliferating Blood Vessels in Oral Squamous Cell Carcinoma. (PubMed, J Cancer)
A previous study reported that inhibiting CXCR4 with AMD3100 induces tumor cell death and enhances the efficacy of the chemotherapeutic agent cisplatin. Treatment with AMD3100 leads to a marked reduction in the CD105+ vessels and impairs the maturation of tumor micro-vessels, explaining the cause of observed necrosis. Thus, CXCR4 serves as a promising biomarker in OSCC, and its inhibition with AMD3100 offers the therapeutic potential, particularly in cases with advanced pathological grades.
Journal
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CXCR4 (Chemokine (C-X-C motif) receptor 4) • ENG (Endoglin)
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cisplatin • plerixafor
1m
White matter injury in young rats with cerebral palsy: the role of massage in regulating exosomes via the chemokine axis. (PubMed, J Stroke Cerebrovasc Dis)
Massage is associated with enhanced motor function and white matter restoration in cerebral palsy, potentially through mechanisms involving the SDF-1/CXCR4 axis, increased homing of BMSCs-Exo to the brain, and enhanced oligodendrocyte attachment.
Preclinical • Journal
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CXCL12 (C-X-C Motif Chemokine Ligand 12)
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plerixafor
2ms
Efficacy of chemotherapy with G-CSF versus plerixafor with G-CSF in autologous stem cell mobilization for lymphoma patients. (PubMed, Am J Cancer Res)
Mobilization with G-CSF plus plerixafor is associated with higher CD34+ cell yields, faster hematologic and immune recovery, lower complication rates, and better QoL outcomes compared with G-CSF plus chemotherapy in lymphoma patients undergoing ASCT.
Journal
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CD8 (cluster of differentiation 8) • CD34 (CD34 molecule)
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plerixafor
2ms
Exploring the Relationship Between Daratumumab Treatment and Stem Cell Collection in Newly Diagnosed Multiple Myeloma (NDMM) Patients Undergoing Transplantation: Insights From a Single-Center Investigation. (PubMed, Indian J Hematol Blood Transfus)
Patients on daratumumab induction regimen exhibited an increased use of plerixafor when compared to non-daratumumab induction regimen (p < 0.001). The addition of daratumumab in induction therapy of multiple myeloma did not affect stem cell yield but increased dependence on plerixafor during mobilization therapy.
Journal
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CD34 (CD34 molecule)
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Darzalex (daratumumab) • plerixafor
2ms
Remodeling the Tumor Immune Environment in Breast Cancer via Bortezomib-based Combination Therapy. (PubMed, Int J Biol Sci)
Their study reveals that bortezomib, combined with either tetrathiomolybdate or AMD3100, synergistically kills breast cancer by downregulating expression of the proteasome subunit PSMB5. Crucially, the in vivo antitumor efficacy of these combinations is strictly dependent on an intact immune system, enabling cytotoxic CD8⁺ T cell responses. Although this study raises important mechanistic questions for future investigation, it significantly opens new avenues for expanding the therapeutic application of proteasome inhibitors in solid tumors.
Journal
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CD8 (cluster of differentiation 8)
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bortezomib • plerixafor
2ms
A pan-cancer single-cell analysis reveals the effect of PD-1 blockades on tumor angiogenesis by inhibiting the endothelial CXCL12-CXCR4 axis. (PubMed, Cancer Immunol Immunother)
Using a murine tumor model built with Lewis Lung Carcinoma cell line, we further validated our findings that a PD-1 blockade, as well as a CXCR4 antagonist AMD3100, inhibited EC population in tumors and their CXCL12 expression...Moreover, we predicted MYC to be the potential regulator through which PD-1 blockades affect ECs. Together, our results suggest that PD-1 blockades have an anti-angiogenic effect besides boosting T cell immunity, and the CXCL12/CXCR4 pathway is a potential target for enhancing the effectiveness of PD-1 blockades.
Journal • PD(L)-1 Biomarker • IO biomarker • Pan tumor
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CXCL12 (C-X-C Motif Chemokine Ligand 12)
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plerixafor
2ms
Endothelial cell-derived SDF-1α elicits stemness traits of glioblastoma via dual-regulation of GLI1. (PubMed, Theranostics)
Preclinical studies indicated that the combination of the CXCR4 antagonist AMD3100 and the AKT inhibitor GSK690693 synergistically inhibits GBM cell progression. Our findings unveil a novel signaling axis between ECs and tumor cells that directly impacts the acquisition of stemness traits, suggesting that targeting this pathway could represent a promising therapeutic strategy against GBM.
Journal
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CXCL12 (C-X-C Motif Chemokine Ligand 12) • GLI1 (GLI Family Zinc Finger 1)
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GSK690693 • plerixafor
2ms
Targeting the CXCR4/CXCL12 Axis to Overcome Drug Resistance in Triple-Negative Breast Cancer. (PubMed, Cells)
Notably, CXCR4 antagonists like plerixafor, balixafortide, and POL5551 have shown encouraging preclinical and clinical results, particularly when combined with chemotherapy or immunotherapy. Despite persistent challenges such as tumour heterogeneity and potential toxicity, growing clinical evidence supports the translational relevance of this axis. This manuscript provides an in-depth analysis of CXCR4/CXCL12-mediated drug resistance in TNBC and evaluates current and emerging therapeutic interventions.
Review • Journal • IO biomarker
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HER-2 (Human epidermal growth factor receptor 2) • CXCL12 (C-X-C Motif Chemokine Ligand 12)
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balixafortide (POL 6326) • plerixafor