Plerixafor

What is plerixafor used for?

Plerixafor is a prescription medicine that is used to raise the number of stem cells.

Description

Mozobil (plerixafor) injection is a sterile, preservative-free, clear, colorless to pale-yellow, isotonic solution for subcutaneous injection. Each mL of the sterile solution contains 20 mg of plerixafor. Each single-dose vial is filled to deliver 1.2 mL of the sterile solution that contains 24 mg of plerixafor and 5.9 mg of sodium chloride in Water for Injection adjusted to a pH of 6.0 to 7.5 with hydrochloric acid and with sodium hydroxide, if required.

Plerixafor is a hematopoietic stem cell mobilizer with a chemical name 1,4-Bis((1,4,8,11-tetraazacyclotetradecan-1-yl)methyl)benzene.  It has the molecular formula C28H54N8. The molecular weight of plerixafor is 502.79 g/mol.

Figure 1: Structural Formula

Plerixafor is a white to off-white crystalline solid. It is hygroscopic. Plerixafor has a typical melting point of 131.5°C. The partition coefficient of plerixafor between 1-octanol and pH 7 aqueous buffer is <0.1.

Mechanism of Action

Plerixafor is an inhibitor of the CXCR4 chemokine receptor and blocks binding of its cognate ligand, stromal cell-derived factor-1α (SDF-1α). SDF-1α and CXCR4 are recognized to play a role in the trafficking and homing of human hematopoietic stem cells (HSCs) to the marrow compartment. Once in the marrow, stem cell CXCR4 can act to help anchor these cells to the marrow matrix, either directly via SDF-1α or through the induction of other adhesion molecules. Treatment with plerixafor resulted in leukocytosis and elevations in circulating hematopoietic progenitor cells in mice, dogs and humans. CD34+ cells mobilized by plerixafor were capable of engraftment with long-term repopulating capacity up to one year in canine transplantation models.

Before taking plerixafor, tell your doctor:

• If you are allergic to plerixafor; any part of this medicine; or any other drugs, foods, or substances. Tell your doctor about the allergy and what signs you had.
• If you have leukemia.
• If you are breast-feeding. Do not breast-feed while you take plerixafor and for 1 week after your last dose.

This is not a list of all drugs or health problems that interact with plerixafor.

Tell your doctor and pharmacist about all of your drugs (prescription or OTC, natural products, vitamins) and health problems. You must check to make sure that it is safe for you to take plerixafor with all of your drugs and health problems. Do not start, stop, or change the dose of any drug without checking with your doctor.

What are some things I need to know or do while I take plerixafor?

• Tell all of your health care providers that you take plerixafor. This includes your doctors, nurses, pharmacists, and dentists.
• To lower the chance of feeling dizzy or passing out, rise slowly if you have been sitting or lying down. Be careful going up and down stairs.
• Allergic reactions have happened with plerixafor. Rarely, some reactions can be very bad or life-threatening. Talk with the doctor.
• Have blood work checked as you have been told by the doctor. Talk with the doctor.
• This medicine may cause harm to an unborn baby. A pregnancy test will be done before you start plerixafor to show that you are NOT pregnant.
• Women must use birth control while taking plerixafor and for some time after the last dose. Ask your doctor how long to use birth control. If you get pregnant, call your doctor right away.

How is plerixafor best taken?

Use plerixafor as ordered by your doctor. Read all information given to you. Follow all instructions closely.

• It is given as a shot into the fatty part of the skin.

What do I do if I miss a dose?

• Call your doctor to find out what to do.

What are the side effects of plerixafor that I need to call my doctor about immediately?

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.
• Very bad dizziness or passing out.
• Any unexplained bruising or bleeding.
• Enlarged spleens have happened with plerixafor. This may lead to rupture of the spleen. Call your doctor right away if you have left upper stomach pain or shoulder pain.

What are some other side effects of plerixafor?

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

• Dizziness.
• Feeling tired or weak.
• Headache.
• Upset stomach or throwing up.
• Stomach pain or diarrhea.
• Gas.
• Joint pain.
• Irritation where the shot is given.
• Trouble sleeping.

These are not all of the side effects that may occur. If you have questions about side effects, call your doctor. Call your doctor for medical advice about side effects.

You may report side effects to the FDA at 1-800-332-1088. You may also report side effects at https://www.fda.gov/medwatch.

If overdose is suspected:

If you think there has been an overdose, call your poison control center or get medical care right away. Be ready to tell or show what was taken, how much, and when it happened.

How do I store and/or throw out plerixafor?

• If you need to store plerixafor at home, talk with your doctor, nurse, or pharmacist about how to store it.

Label

PRINCIPAL DISPLAY PANEL – 1.2 ML VIAL CARTON

• NDC 0024-5862-01
• Mozobil®
  (plerixafor injection)
• 24 mg/1.2 mL
  (20 mg/mL)
• For subcutaneous
  injection only
• One single-dose vial.
  Discard unused portion.
• Rx only
• SANOFI GENZYME

SRC: NLM .