Motixafortide

FDA-approved CXCR4 antagonistEstablished

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.

Calculate Dose

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.

FDA Approved

Dosage evidence summary for Motixafortide
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.

Research-reported dosing for Motixafortide, one row per studied regimen
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.

Motixafortide dosage in published studies and labels →

Sequence & molecular data

Sequence and molecular data for Motixafortide
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

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.

Regulatory and research status for Motixafortide
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

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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?

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

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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