Motixafortide
Motixafortide is an FDA-approved CXCR4 antagonist. Haematopoietic stem cells are retained in the bone marrow niche largely through the CXCR4 receptor binding its ligand CXCL12. Motixafortide is a synthetic cyclic peptide that blocks CXCR4 with high affinity and a long receptor occupancy, releasing stem cells into peripheral blood where they can be collected by apheresis.
For research use only.
Key Facts
- CAS
- 664334-36-5
- Molecular Weight (MW)
- 2159.5 g/mol
- Half-life
- Effective half-life about 2 hours
- FDA status
- Approved
- Evidence level
- FDA Approved
- Human dose established
- Yes
- Administration Route
- Subcutaneous
- Frequency
- One dose before the first apheresis; a second dose may be given before a third apheresis
- Last updated
- Nov 7, 2026
- Reviewed
- Nov 7, 2026
Research summary
CXCR4 antagonist peptide approved, in combination with filgrastim, to mobilise haematopoietic stem cells for collection and autologous transplantation in patients with multiple myeloma.
Research evidence
- Regulatory review (FDA label)1 reviewed source
- Controlled human trialsNone in reviewed sources
- Early or uncontrolled human studiesNone in reviewed sources
- Lab & animal studiesNone in reviewed sources
How it works
Each step shows whether the sources Peptide Library has reviewed include that kind of research. Counts are reviewed sources, not every study ever published. Reviews and programme summaries that describe human use are shown as "reported", not as trials, and registered trials without published results are listed but not counted. A higher step means research has progressed further; it does not mean a compound works better or is safer. Compounds whose evidence has not been reviewed yet show "Not reviewed" instead of a guess.
Peptide Library's Motixafortide profile summarises 5 cited studies listed in the Science section, the compound's regulatory status, and research-protocol parameters reported for it. It is a research reference, not medical advice.
Motixafortide dosage evidence
Motixafortide has an FDA-approved human dosage, as Aphexda, used together with filgrastim (G-CSF) to mobilise blood stem cells for collection and autologous transplantation in people with multiple myeloma. The label's recommended dose is 1.25 mg/kg of actual body weight by slow subcutaneous injection 10 to 14 hours before the first apheresis, with a second dose allowed before a third apheresis.
| Human dosing established | Yes |
|---|---|
| Studied dose range | 1.25 mg/kg before apheresis (FDA label) |
| Route | Subcutaneous |
| Frequency | One dose before the first apheresis; a second dose may be given before a third apheresis |
| Duration studied | One or two doses per mobilisation |
| Half-life | Effective half-life about 2 hours |
| Evidence level | FDA Approved |
| Last reviewed | 2026-11-07 |
Research-reported dosing
Doses as studied, one row per regimen. Different trials used different regimens; they are listed separately rather than averaged.
| Study / context | Population | Dose | Route | Frequency | Duration | Outcome studied | Source |
|---|---|---|---|---|---|---|---|
| FDA label — Aphexda with filgrastim, stem cell mobilisationFDA-approved label · FDA prescribing information | Adults with multiple myeloma undergoing stem cell collection for autologous transplantation | 1.25 mg/kg actual body weight, after filgrastim 10 mcg/kg once daily for 4 days and with premedication | Subcutaneous, slow injection over about 2 minutes | 10–14 hours before the first apheresis; a second dose 10–14 hours before a third apheresis if needed | One or two doses | In the GENESIS trial (NCT03246529), 67.5% reached the collection goal of at least 6 million CD34+ cells/kg in up to two aphereses, versus 9.5% with placebo plus filgrastim | APHEXDA (motixafortide) for injection (Gamida Cell) — FDA prescribing information, DailyMed |
Where sources disagree
- The label requires premedication before every dose (an H1 antihistamine, an H2 blocker and a leukotriene inhibitor, plus an analgesic) and administration where anaphylaxis can be treated: anaphylactic shock occurred in 0.7% of treated patients in clinical studies.
- The label warns that it may mobilise leukemic cells and should not be used in people with leukemia, and that it raises white cell counts. Safety and effectiveness in children have not been established.
- The label describes a lyophilised powder vial that is reconstituted before injection.
Sequence & molecular data
| Molecular formula | C97H144FN33O19S2 |
|---|---|
| Molecular weight | 2159.5 g/mol |
| CAS number | 664334-36-5 |
| PubChem CID | 91865076 |
| FDA UNII | DA9G065962 |
| ChEMBL | CHEMBL6067714 |
| DrugBank | DB14939 |
Identifiers link to the public PubChem, FDA Substance Registration (UNII), ChEMBL and DrugBank records for the same entity.
Science
Mechanism of Action
Haematopoietic stem cells are retained in the bone marrow niche largely through the CXCR4 receptor binding its ligand CXCL12. Motixafortide is a synthetic cyclic peptide that blocks CXCR4 with high affinity and a long receptor occupancy, releasing stem cells into peripheral blood where they can be collected by apheresis.
Studies
- Motixafortide and G-CSF to mobilize hematopoietic stem cells for autologous transplantation in multiple myeloma: a randomized phase 3 trial
- GENESIS: Phase III trial evaluating BL-8040 + G-CSF to mobilize hematopoietic cells for autologous transplant in myeloma
- Motixafortide and Pembrolizumab Combined to Nanoliposomal Irinotecan, Fluorouracil, and Folinic Acid in Metastatic Pancreatic Cancer: The COMBAT/KEYNOTE-202 Trial
- BL-8040, a CXCR4 antagonist, in combination with pembrolizumab and chemotherapy for pancreatic cancer: the COMBAT trial
- WBC Growth Factors: ASCO Guideline Update
Research statistics
29 PubMed publications · 37.9% human clinical research · 22 registered trials
Counts of published research through 2026-11-01, not evidence that it works. Publications by year, study types and trials · How publications are counted
Regulatory & research status
Motixafortide is an FDA-approved product for specific labelled indications. Approval does not extend to the research contexts described on this page, and approved products are prescription medicines.
| FDA status | Approved |
|---|---|
| Research status | Approved product (see FDA status) |
| Availability | Prescription-Only |
| WADA (sport) | Unknown / Not Listed |
| Library classification | FDA-Approved |
How FDA approval, compounding and research-only status differ
Benefits
—
Motixafortide side effects
No side effects listed yet for this entry.
Storage & stability
This compound is not supplied as a powder to be mixed, so the freeze-dried powder and reconstitution handling described for research peptides does not apply. Storage conditions are product-specific: follow the label or packaging of the product itself.
Motixafortide: frequently asked questions
What is Motixafortide?
CXCR4 antagonist peptide approved, in combination with filgrastim, to mobilise haematopoietic stem cells for collection and autologous transplantation in patients with multiple myeloma.
How does Motixafortide work?
Haematopoietic stem cells are retained in the bone marrow niche largely through the CXCR4 receptor binding its ligand CXCL12. Motixafortide is a synthetic cyclic peptide that blocks CXCR4 with high affinity and a long receptor occupancy, releasing stem cells into peripheral blood where they can be collected by apheresis.
Is Motixafortide FDA approved?
Yes. Motixafortide is approved by the FDA, and approved products are prescription medicines. Approval is always for specific indications studied in clinical trials, so an approved status does not mean the compound is approved for every use it is discussed for. Research-chemical material sold under the same name is not the approved product.
What peptides are similar to Motixafortide?
Compounds most often compared with Motixafortide include Angiotensin II, Cetrorelix, Corticorelin and Cosyntropin. They are grouped by shared mechanism or research area rather than by equivalence, and their regulatory status and evidence base differ.
References
- Motixafortide and G-CSF to mobilize hematopoietic stem cells for autologous transplantation in multiple myeloma: a randomized phase 3 trial — Nat Med, 2023External reference
- GENESIS: Phase III trial evaluating BL-8040 + G-CSF to mobilize hematopoietic cells for autologous transplant in myeloma — Future Oncol, 2019External reference
- Motixafortide and Pembrolizumab Combined to Nanoliposomal Irinotecan, Fluorouracil, and Folinic Acid in Metastatic Pancreatic Cancer: The COMBAT/KEYNOTE-202 Trial — Clin Cancer Res, 2021External reference
- BL-8040, a CXCR4 antagonist, in combination with pembrolizumab and chemotherapy for pancreatic cancer: the COMBAT trial — Nat Med, 2020External reference
- WBC Growth Factors: ASCO Guideline Update — J Clin Oncol, 2026External reference
Related research, comparisons & guides
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Compiled by Peptide Library Editorial · Reviewed Aug 30, 2026 · Updated Nov 7, 2026 · Version 2
This Motixafortide profile is compiled from published literature (5 cited studies linked above), public regulatory records and chemical registries. It describes what research reports; it is not medical advice, and nothing here is a dosing recommendation for humans. Peptide Library does not sell peptides. Editorial policy · How profiles are compiled · Report an error
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