Motixafortide
Also known as: BL-8040, BKT140, APHEXDA, TF 14016
๐TL;DR
- โขFDA-approved for stem cell mobilization in multiple myeloma
- โขHigh-affinity CXCR4 antagonism (Ki 0.32 nM) with extended duration of action (>48 hours)
- โข92.5% success rate for adequate stem cell collection in two apheresis sessions
- โขPreferentially mobilizes primitive hematopoietic stem cells
- โขSingle subcutaneous injection per apheresis session
Protocol Quick-Reference
Hematopoietic stem cell mobilization for autologous transplantation in multiple myeloma
Dosing
Amount
1.25 mg/kg actual body weight
Frequency
Once per apheresis session
Duration
1-3 doses over mobilization period
Administration
Route
SCSchedule
Once per apheresis session
Timing
Administer 10-14 hours prior to each planned apheresis session; given in conjunction with G-CSF priming (4-5 days prior)
Cycle
Duration
3-7 days (mobilization period)
Repeatable
Single cycle
โ๏ธ Suggested Bloodwork (3 tests)
CBC with differential and CD34+ cell count
When: Baseline
Why: Baseline blood counts and stem cell levels
CD34+ cell count
When: Day of apheresis
Why: Assess adequacy of stem cell mobilization
CBC with differential
When: Post-apheresis
Why: Monitor blood counts after collection
๐ก Key Considerations
- โFDA-approved prescription medication: must be administered in healthcare settings equipped for anaphylaxis management
- โRequired premedication: H1 blocker, H2 blocker, leukotriene inhibitor, and acetaminophen before each dose
- โReconstituted solution must be used within 4 hours
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Scientific Details
- Molecular Formula
- C97H144FN33O19S2
- Molecular Weight
- 2159.55 Da
- CAS Number
- 664334-36-5
- Sequence
- 14-amino acid cyclic peptide (contains non-natural amino acids)
What is Motixafortide?#
Motixafortide (APHEXDA, BL-8040) is an FDA-approved synthetic cyclic peptide that selectively antagonizes the CXCR4 chemokine receptor. It was developed by BioLineRx under license from Biokine Therapeutics and received FDA approval on September 8, 2023, for use in combination with filgrastim (G-CSF) to mobilize hematopoietic stem cells (HSCs) to the peripheral blood for collection and subsequent autologous transplantation in patients with multiple myeloma.
Mechanism of Action#
CXCR4 and its ligand CXCL12 (SDF-1) form a critical axis that anchors hematopoietic stem cells within the bone marrow niche. Motixafortide disrupts this interaction by:
- High-affinity CXCR4 binding: Binds CXCR4 with a Ki of 0.32 nM, approximately 2,000-fold higher affinity than plerixafor (Ki 652 nM)
- Blocking CXCL12 binding: Prevents CXCL12 from binding to CXCR4 on HSCs
- Releasing HSCs from bone marrow: HSCs are mobilized into the peripheral blood
- Extended receptor occupancy: Provides clinical activity exceeding 48 hours from a single dose
- Preferential primitive HSC mobilization: Mobilizes immunophenotypically and transcriptionally primitive HSCs, potentially improving transplant quality
Clinical Significance#
Multiple myeloma patients who undergo autologous stem cell transplantation (ASCT) require collection of adequate numbers of CD34+ hematopoietic stem cells via apheresis. G-CSF alone is the standard mobilization agent but often requires multiple apheresis sessions. Adding motixafortide dramatically increases the proportion of patients who achieve adequate collection within one or two sessions.
Additional Indications Under Investigation#
| Indication | Status | Notes |
|---|---|---|
| Sickle cell disease gene therapy | Phase 1 | HSC mobilization for gene therapy |
| Pancreatic cancer | Phase 2 | Orphan Drug Designation (US and EU) |
| Acute myeloid leukemia | Phase 2 | Orphan Drug Designation (US) |
Important Considerations#
Motixafortide is a prescription medication administered in healthcare settings under medical supervision. It carries warnings for anaphylactic shock and hypersensitivity reactions, requiring premedication before administration.
Key Research Findings#
Motixafortide and G-CSF to mobilize hematopoietic stem cells for autologous transplantation in multiple myeloma: a randomized phase 3 trial, published in Nature Medicine (Crees ZD et al., 2023; PMID: 37069359):
- The study demonstrated achieved target collection of 88.8% in one session versus 9.5% placebo
Related Reading#
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Community Protocols Available
See real-world usage patterns alongside the clinical evidence above. Community-sourced, not clinically verified.
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Medical Disclaimer
This website is for educational and informational purposes only. The information provided is not intended to diagnose, treat, cure, or prevent any disease. Always consult with a qualified healthcare professional before using any peptide or supplement.
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