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DRUG CLASS:

CXCR4 antagonist

2d
Oral CXCR4 inhibition with mavorixafor: Emerging therapeutic applications in WHIM syndrome, chronic neutropenia, oncology, and stem cell mobilization. (PubMed, Curr Res Transl Med)
Furthermore, this review positions mavorixafor within the broader CXCR4-targeted therapeutic landscape, identifying current research gaps and suggesting directions for future studies. In conclusion, by integrating mechanistic insights with preclinical and clinical findings, this article highlights mavorixafor's promise as a targeted therapy with the potential to transform treatment paradigms for CXCR4-driven diseases.
Review • Journal
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CXCR4 (Chemokine (C-X-C motif) receptor 4) • CXCL12 (C-X-C Motif Chemokine Ligand 12)
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Xolremdi (mavorixafor)
11d
PAMD-Ch17, a Polymeric Analog of Plerixafor, Induces Mitochondrial Dysfunction in T-ALL Cells Independent of CXCR4. (PubMed, Mol Cancer Ther)
Collectively, our results indicate that PAMD-Ch17 has anti-leukemic effects against T-ALL cells but not healthy cells, likely mediated through a CXCR4 independent, mitochondrial based mechanism. These findings support further development of PAMDs as potential therapeutics for patients with T-ALL.
Journal
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CXCR4 (Chemokine (C-X-C motif) receptor 4)
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plerixafor
12d
Mechanism of LPS-activated gingival fibroblasts promote the migration of gastric cancer cells via CXCL12/CXCR4-Snail2-EMT axis. (PubMed, In Vitro Cell Dev Biol Anim)
AMD3100 and si-CXCR4 can significantly inhibit the expression of Snail2...In summary, the CXCL12/CXCR4-Salil2-EMT signaling pathway is involved in the migration of gastric cancer cells promoted by periodontitis. This will uncover new insights into the mechanisms that might play a role in the development of gastric cancer and strategies for targeted therapy.
Journal
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CXCR4 (Chemokine (C-X-C motif) receptor 4) • CDH1 (Cadherin 1) • CXCL12 (C-X-C Motif Chemokine Ligand 12) • VIM (Vimentin) • CDH2 (Cadherin 2) • SNAI2 (Snail Family Transcriptional Repressor 2)
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plerixafor
14d
Theranostic applications of CXCR4-targeted imaging ligands in lymphoma: integrating diagnosis and precision therapy. (PubMed, Am J Nucl Med Mol Imaging)
Therapeutic strategies include peptide antagonists (BL-8040, Balixafortide), radioligand therapies ([177Lu]Pentixather, [177Lu]Lu-BL02), small-molecule inhibitors (Plerixafor, WK1), and monoclonal antibodies (PF-06747143, Ulocuplomab, LY2624587). Key challenges include off-target uptake due to physiological CXCR4 expression and compensatory signaling via CXCR7. Future directions involve dual-receptor targeting, nanoparticle-based delivery, and integration into precision oncology for both hematologic and solid tumors.
Review • Journal
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CXCR4 (Chemokine (C-X-C motif) receptor 4) • ACKR3 (Atypical Chemokine Receptor 3)
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balixafortide (POL 6326) • Aphexda (motixafortide) • plerixafor
1m
P2 data • Journal
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CD34 (CD34 molecule)
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Rituxan (rituximab) • bendamustine • plerixafor
1m
CXCR4: A Promising Novel Strategy for Lung Cancer Treatment. (PubMed, Biomolecules)
Therapeutic strategies targeting CXCR4 include small-molecule antagonists (e.g., AMD3100/plerixafor; balixafortide), anti-CXCR4 antibodies, and CXCL12 decoys, as well as imaging probes for patient selection and response monitoring (e.g., 68Ga-pentixafor PET). Preclinical and early clinical studies suggest that CXCR4 blockade can impair tumor growth, limit metastatic spread, and enhance chemotherapy and immunotherapy efficacy, although hematopoietic side effects and infection risk necessitate careful therapeutic design. This review synthesizes the molecular features, regulatory networks, and translational potential of CXCR4 in lung cancer and discusses future directions for precision therapy and biomarker-guided intervention.
Review • Journal • IO biomarker
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CXCR4 (Chemokine (C-X-C motif) receptor 4) • CXCL12 (C-X-C Motif Chemokine Ligand 12)
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balixafortide (POL 6326) • plerixafor
1m
WBC Growth Factors: ASCO Guideline Update. (PubMed, J Clin Oncol)
Prophylactic use of CSFs to reduce the risk of febrile neutropenia is warranted when the risk of febrile neutropenia from chemotherapy is approximately 20% or higher and no other equally effective and safe regimen that does not require CSFs is available. For patients receiving chemotherapy with a <20% risk of febrile neutropenia, primary prophylaxis with a CSF may be warranted if patients are at a high risk of febrile neutropenia based on age, medical history, or disease characteristics. For stem-cell mobilization, CSFs may be used either alone, after chemotherapy, or in combination with plerixafor or motixafortide. The guideline also provides information about the dosing and selection of CSFs.Additional information is available at www.asco.org/supportive-care-guidelines.
Journal
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CXCR4 (Chemokine (C-X-C motif) receptor 4)
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Aphexda (motixafortide) • plerixafor
1m
Superiority of high-dose cytarabine-based mobilisation over cyclophosphamide or plerixafor in primary CNS lymphoma. (PubMed, Ann Hematol)
The first-day CD34⁺ cell count provides a robust, real-time tool for guiding apheresis. HD-Ara-C-based mobilisation should be considered the preferred regimen for fit patients, with steady-state mobilisation as an alternative for selected cases.
Clinical • Retrospective data • Journal • Head-to-Head
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CD34 (CD34 molecule)
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cytarabine • cyclophosphamide • plerixafor
1m
EPI-X4 is a peptide antagonist of CXCR4 with therapeutic prospects for cancer and inflammatory disorders. (PubMed, Peptides)
Currently, plerixafor (AMD3100) is the only approved CXCR4 antagonist used to mobilize hematopoietic stem cells into the peripheral blood for transplantation therapy...One interesting compound is the endogenous peptide inhibitor for CXCR4 (EPI-X4), recently discovered in the hemofiltrate of dialysis patients. It was traced back to human serum albumin, from where it was generated by the proteolytic activity of cathepsins E and D. Based on its implications for cancer therapy, this review describes its recent evaluations, which include sequence optimization, in vivo efficacy, toxicity, and bioavailability studies.
Review • Journal
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CXCR4 (Chemokine (C-X-C motif) receptor 4) • CXCL12 (C-X-C Motif Chemokine Ligand 12) • CTSS (Cathepsin S)
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plerixafor
2ms
Trial completion date • Trial primary completion date
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Hemady (dexamethasone tablets) • Aphexda (motixafortide)