Approved December 15, 2008

PLERIXAFOR
(FDA Category 1S)

MOZOBIL (Genzyme)

DOSING INFORMATION: The recommended dose of plerixafor is 0.24 mg/kg (actual body weight) via subQ injection approximately 11 hours prior to initiation of apheresis for up to 4 consecutive days. Administer granulocyte-colony stimulating factor (G-CSF) 10 micrograms/kg via subQ bolus or continuous infusion once daily in the morning for 4 days prior to the first evening dose of plerixafor, and on each day prior to apheresis. Adjust dose in patients with renal impairment.

PHARMACOKINETICS: The Vd was 0.3 L/kg. Protein binding was up to 58%. Tmax is approximately 30 to 60 minutes after a subQ injection. Plerixafor was not metabolized using human liver microsomes or human primary hepatocytes. Additionally, plerixafor did not exhibit inhibitory activity towards the major drug metabolizing cytochrome P450 enzymes nor did it induce CYP1A2, CYP2B6, or CYP3A4 enzymes. About 70% of plerixafor was excreted in the urine. The half-life was 3 to 5 hrs.

CAUTIONS: Plerixafor may mobilize leukemic cells and should not be used in patients with leukemia. Blood counts may be altered. Tumor cells may be released from marrow. Splenic rupture may occur. The most common adverse events were diarrhea, nausea, fatigue, injection site reactions, headache, arthralgia, dizziness, and vomiting.

FDA APPROVED INDICATIONS: Plerixafor is indicated in combination with granulocyte-colony stimulating factor (G-CSF) to mobilize hematopoietic stem cells to the peripheral blood for collection and subsequent autologous transplantation in patients with non-Hodgkin's lymphoma (NHL) and multiple myeloma (MM).