Plerixafor
Myeloid colony-stimulating factors
Myeloid colony-stimulating factors
A CXCR4 blocker that, added to G-CSF, frees blood stem cells from the marrow for collection before an autologous transplant.
Quick facts
- Group
- Myeloid colony-stimulating factors
- Target
- Chemokine receptor CXCR4 on haematopoietic stem cells
- Used for
- Stem cell mobilisation · Stem cell mobilisation
- Key effects
- Diarrhoea · Injection-site reactions · Headache
- Monitor
- White cell and platelet counts · Kidney function
- ATC
- L03AX16
No doses: the clinician sets them by the current guideline.
Mechanism of action
The figure shows plerixafor bound to the human CXCR4 receptor (cryo-EM); the nanobody used to stabilise it is not part of the receptor.
Stem cells stay in the marrow because CXCR4 on their surface binds the chemokine SDF-1α (CXCL12) made by marrow stromal cells. Plerixafor, a bicyclam molecule first developed against HIV, blocks CXCR4 so the cells lose their anchor and move into the blood, where they are collected by apheresis. It is a mobiliser, not a growth factor.
- SDF-1α (CXCL12) holds stem cells in the marrow through CXCR4
- Plerixafor blocks CXCR4
- Stem cells (CD34+) leave the marrow for the blood
- They are collected by apheresis for transplant
Indications
- Stem cell mobilisation with G-CSF before autologous transplant in non-Hodgkin lymphoma Non-Hodgkin lymphoma →
- Stem cell mobilisation with G-CSF before autologous transplant in multiple myeloma Multiple myeloma →
Adverse effects
Common
- Diarrhoea, nausea, vomiting, abdominal pain, gas
- Injection-site reactions
- Headache, dizziness, tiredness
- Joint pain, trouble sleeping
Contraindications
- Previous hypersensitivity to plerixafor
- Not used to mobilise stem cells in leukaemia (it may also mobilise leukaemic cells)
Key interactions
- Filgrastim or another G-CSF
- Combined on purpose: G-CSF is given first and continued while plerixafor is added
What is monitored
- White cell and platelet counts
- Kidney function (the dose is reduced in renal impairment)
- Abdominal or shoulder pain suggesting splenic enlargement
- Hypersensitivity during and after the injection
Administration and safety
- Subcutaneous injection by a health professional, timed some hours before each apheresis session
- Given only after several days of G-CSF
- Observe for hypersensitivity after each dose
Pregnancy and breastfeeding
It can harm the fetus: effective contraception is used during treatment, and breastfeeding is avoided during treatment and for one week after the last dose.
Nursing care
- Check the white count, platelets and creatinine before dosing
- Coordinate timing with the apheresis unit
- Teach to report left upper abdominal or shoulder pain at once
- Check pregnancy status and contraception
Pharmacokinetics
- Absorption
- Subcutaneous injection
- Elimination
- Mainly by the kidneys; about 70% excreted unchanged in urine within 24 hours
- Half-life
- About 3–5 hours
Test yourself
Think of the answer, then tap the question to see it.
Which receptor does plerixafor block?
CXCR4, the receptor for SDF-1α (CXCL12).
Which drug is it combined with?
A G-CSF such as filgrastim.
In which disease is it not used for mobilisation, and why?
Leukaemia, because it may mobilise leukaemic cells too.
Connections
← Back to the class: Myeloid colony-stimulating factors
Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.
Sources: DailyMed - PLERIXAFOR injection, solution (DailyMed (U.S. National Library of Medicine), 2026); Plerixafor Injection: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2025).
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Representative model, for educational purposes only.