Plerixafor

Plerixafor

Clinical data
Trade names	Mozobil
AHFS/Drugs.com	Consumer Drug Information
MedlinePlus	a609018
Pregnancy category	US: D (Evidence of risk)
Routes of administration	Subcutaneous injection
ATC code	L03AX16 (WHO)
Legal status
Legal status	US: ℞-only In general: ℞ (Prescription only)
Pharmacokinetic data
Protein binding	Up to 58%
Metabolism	None
Biological half-life	3–5 hours
Excretion	Renal
Identifiers
IUPAC name 1,1’-(1,4-phenylenebismethylene)bis(1,4,8,11- tetraazacyclotetradecane)
Synonyms	JM 3100, AMD3100
CAS Number	155148-31-5 N
PubChem CID	65015
IUPHAR/BPS	844
DrugBank	DB06809 Y
ChemSpider	58531 Y
UNII	S915P5499N
KEGG	D08971 Y
ChEMBL	CHEMBL18442 Y
Chemical and physical data
Formula	C28H54N8
Molar mass	502.782 g/mol
3D model (Jmol)	Interactive image
SMILES N1CCNCCCN(CCNCCC1)Cc2ccc(cc2)CN3CCCNCCNCCCNCC3
InChI InChI=1S/C28H54N8/c1-9-29-15-17-31-13-3-21-35(23-19-33-11-1)25-27-5-7-28(8-6-27)26-36-22-4-14-32-18-16-30-10-2-12-34-20-24-36/h5-8,29-34H,1-4,9-26H2 Y Key:YIQPUIGJQJDJOS-UHFFFAOYSA-N Y
NY (what is this?)

Plerixafor (INN and USAN, trade name Mozobil) is an immunostimulant used to mobilize hematopoietic stem cells in cancer patients into the bloodstream. The stem cells are then extracted from the blood and transplanted back to the patient. The drug was developed by AnorMED which was subsequently bought by Genzyme.

Peripheral blood stem cell mobilization, which is important as a source of hematopoietic stem cells for transplantation, is generally performed using granulocyte colony-stimulating factor (G-CSF), but is ineffective in around 15 to 20% of patients. Combination of G-CSF with plerixafor increases the percentage of persons that respond to the therapy and produce enough stem cells for transplantation. The drug is approved for patients with lymphoma and multiple myeloma.

Studies in pregnant animals have shown teratogenic effects. Plerixafor is therefore contraindicated in pregnant women except in critical cases. Fertile women are required to use contraception. It is not known whether the drug is secreted into the breast milk. Breast feeding should be discontinued during therapy.

Nausea, diarrhea and local reactions were observed in over 10% of patients. Other problems with digestion and general symptoms like dizziness, headache, and muscular pain are also relatively common; they were found in more than 1% of patients. Allergies occur in less than 1% of cases. Most adverse effects in clinical trials were mild and transient.

The European Medicines Agency has listed a number of safety concerns to be evaluated on a post-marketing basis, most notably the theoretical possibilities of spleen rupture and tumor cell mobilisation. The first concern has been raised because splenomegaly was observed in animal studies, and G-CSF can cause spleen rupture in rare cases. Mobilisation of tumor cells has occurred in patients with leukaemia treated with plerixafor.