Motixafortide is a synthetic cyclic peptide and CXCR4 antagonist with pharmaceutical applications in hematopoietic stem-cell mobilization. It is a 14-amino-acid cyclic peptide containing a disulfide bridge and a 4-fluorobenzoyl group. FDA describes motixafortide acetate as the active pharmaceutical ingredient in APHEXDA.
Motixafortide selectively targets the C-X-C chemokine receptor type 4 (CXCR4) pathway. By interfering with CXCR4-mediated retention of hematopoietic stem cells within the bone marrow, motixafortide promotes mobilization of these cells into peripheral blood for collection.
The free-base molecular formula of motixafortide is C₉₇H₁₄₄FN₃₃O₁₉S₂, with a molecular weight of approximately 2159.5 g/mol. PubChem identifies BL-8040, BKT140 and 4F-benzoyl-TN14003 among its synonyms.
Motixafortide is a peptide-based pharmaceutical compound developed as a potent CXCR4 antagonist. The drug substance is manufactured as an acetate salt. FDA states that the drug substance is a white to off-white hygroscopic powder and is freely soluble in water.
Motixafortide is marketed in the United States as APHEXDA and received FDA marketing approval in September 2023 for use in combination with filgrastim to mobilize hematopoietic stem cells to peripheral blood for collection and subsequent autologous transplantation in patients with multiple myeloma.
Motixafortide is used as a hematopoietic stem-cell mobilizer.
The FDA-approved indication is in combination with filgrastim (G-CSF) to mobilize hematopoietic stem cells into peripheral blood for collection and subsequent autologous transplantation in patients with multiple myeloma.
Motixafortide has also been investigated for applications involving CXCR4-dependent tumor biology and hematological malignancies, but these investigational applications should not be presented as approved indications on a commercial API page.
Motixafortide is a CXCR4 antagonist.
CXCR4 is a chemokine receptor involved in retention of hematopoietic stem cells within the bone marrow through interaction with its ligand CXCL12.
By antagonizing CXCR4, motixafortide disrupts CXCR4/CXCL12 signaling and promotes movement of hematopoietic stem cells from the bone marrow into peripheral blood, where they can be collected for transplantation.
| Parameter | Specification |
|---|---|
| Appearance | White crystalline powder or crystals |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 98.0% – 102.0% |
| Loss on Drying | NMT 1.0% |
| Residue on Ignition | NMT 0.5% |
| Heavy Metals | NMT 20 ppm |
| Individual Impurity | NMT 0.5% |
| Total Impurities | NMT 1.0% |
| Water Content | NMT 1.0% |