Plerixafor

Plerixafor (rINN and USAN, also known as MOZOBIL, JM 3100 and AMD3100) is a macrocyclic compound and potential fusion inhibitor. It is an antagonist (or perhaps more accurately a partial agonist) of the alpha-chemokine receptor CXCR4.

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Research

HIV

It was initially developed for potential use in the treatment of HIV, for its role in the blocking of CXCR4, a chemokine receptor which acts as a co-receptor for certain strains of HIV (along with the virus's main cellular receptor, CD4). However, clinical trials in patients with HIV-AIDS have to date shown relatively little useful anti-viral activity.

Further information: Entry inhibitors

Mobilization of hematopoietic stem cells

However, the CXCR4 alpha-chemokine receptor and its ligand SDF-1 are also important in hematopoietic stem cell homing to the bone marrow and in hematopoietic stem cell quiescence. Plerixafor has been found to be a strong inducer of "mobilization" of hematopoietic stem cells from the bone marrow to the bloodstream as peripheral blood stem cells.^[1]

Peripheral blood stem cell mobilization, which has become extremely important as a source of hematopoietic stem cells for transplantation over the past 10 to 15 years, is generally performed using the cytokine drug G-CSF, but is ineffective in around 15 to 20% of patients. AMD3100 offers clinical promise as a drug for peripheral blood stem cell mobilization, and has recently completed Phase 3 clinical trials.^[2] It is not yet in routine clinical use.

Small molecule cancer therapy

AMD3100 was seen to decrease metastasis in mice in several studies.^[3]

References

1. ^ Cashen A, Nervi B, DiPersio J (2007). "AMD3100: CXCR4 antagonist and rapid stem cell-mobilizing agent". Future Oncol 3 (1): 19-27. PMID 17280498.
2. ^ (2007) "Plerixafor: AMD 3100, AMD3100, JM 3100, SDZ SID 791". Drugs R D 8 (2): 113-9. PMID 17324009.
3. ^ (2004) "CXCR4 regulates growth of both primary and metastatic breast cancer.". Cancer Research 64 (23): 8604-8612. PMID 15574767.