Index of drugs

In combination with G-CSF, to increase the mobilization of hematopoietic stem cells in the peripheral blood to retrieve and then autologous transplantation in patients with lymphoma or multiple myeloma, in which mobilization of these cells is insufficient.

1 ml of solution contains 20 mg of plerixafor.

A bicyclam derivative, a reversible CXCR4 chemokine receptor antagonist. It blocks the binding of parental ligand, stromal factor-1α (SDF-1α, another name CXCL12). The following mechanism was adopted to increase leukocytosis and the number of circulating parent progenitor cells: after the administration of plerixafor, the binding of the native ligand to the CXCR4 chemokine receptor is broken, leading to the release of circulating mature and multipotent cells into the blood. After plerixafor administration, functional CD34 + cells are mobilized that are capable of taking up haemopoietic function and hematopoietic repopulation. The maximum concentration after subcutaneous injection occurs after approx. 30-60 min. Plerixafor binds plasma proteins to 58%. It is excreted mainly in the urine, in about 70% in unchanged form. T_0,5 is 3-5 hours.

Hypersensitivity to the components of the preparation.

Possibility of mobilization of cancer cells in patients diagnosed with lymphoma and multiple myeloma. There has not been enough research on tumor cell reinfusion. After application of the preparation in combination with G-CSF for the mobilization of hematopoietic stem cells in patients diagnosed with lymphoma or multiple myeloma during leukapheresis, cancer cells released from the bone marrow may be harvested. There have been no exhaustive studies assessing the clinical significance of the theoretical risk of cancer cell recruitment. In clinical trials, no mobilization of tumor cells was observed after administration of plerixafor to patients diagnosed with non-Hodgkin's lymphoma or multiple myeloma.Mobilization of tumor cells in patients diagnosed with leukemia. Plerixafor and G-CSF were administered to patients diagnosed with acute myeloid leukemia and plasma leukemia as part of the extended access program. In some cases, there was an increase in the number of leukemia cells in the blood. During mobilization of hematopoietic cells, plerixafor may cause mobilization and leukemic cell entry into the apheresis product - plerixafor is not recommended for mobilization of hematopoietic stem cells or bone marrow harvesting in patients diagnosed with leukemia. The use of the product in combination with G-CSF increases the pool of circulating leukocytes and hematopoietic stem cells. When used in patients with peripheral blood neutrophilia exceeding 50,000 / μl, all clinical premises should be considered. During treatment, the number of leukocytes and platelets should be monitored. The possibility of splenomegaly due to the use of plerixafor in combination with G-CSF can not be ruled out. G-CSF can rarely lead to splenic rupture. Spleen examination should be performed if the use of plerixafor in combination with G-CSF results in pain in the left epigastric region and / or around the shoulder or shoulder. Use with caution in elderly patients. The safety and efficacy of the preparation in children and adolescents has not been established.

Plerixafor can cause birth defects in children of women who took plerixafor during pregnancy. In animal studies, teratogenic effects have been demonstrated. The preparation should not be used during pregnancy if the woman's clinical condition does not require treatment with plerixaphor. Women of childbearing potential must use effective contraception during treatment. Breast-feeding should be discontinued while using the product.

Very common: diarrhea, nausea, reactions at the injection site. Common: insomnia, headache and dizziness, vomiting, stomach ache, abdominal discomfort, indigestion, bloating, constipation, flatulence, hypoaesthesia in the mouth, dry mouth, excessive secretion of sweat, erythema, arthralgia, osteo-muscular pain, chronic fatigue, malaise.Uncommon: allergic reactions (including urticaria, periocular swelling, shortness of breath, hypoxia). In addition, a myocardial infarction was observed (however, the preparation does not appear to be an independent risk factor for myocardial infarction in patients receiving G-CSF), hyperleukocytosis, vasovagal reactions (orthostatic hypotension, syncope), thrombocytopenia and paraesthesia.

Treatment with the product should be started and supervised by a doctor with experience in the field of oncology and / or hematology. Cell mobilization and apheresis procedures should be performed in cooperation with an oncological or hematological center with appropriate experience and the possibility of correct monitoring of hematopoietic progenitor cells.
Subcutaneously. The daily dose is 0.24 mg / kg, by injection for 6 hours to 11 hours before the start of apheresis, after a 4-day treatment with the introduction of G-CSF granulocytes. In clinical trials, plerixafor was usually administered for 2 to 4 (and up to 7) consecutive days. The dose should be calculated based on the patient's body weight measured within 1 week before the first dose of plerixafor. In clinical trials, the dose of plerixafor was calculated for patients weighing up to 175% of their body weight. No studies on dosing or treatment with plerixafor of patients weighing more than 175% of body weight have been performed. As higher body weight is accompanied by higher systemic exposure, daily doses of more than 40 mg should not be used. Recommended drugs in combination therapy: 10 μg / kg was administered in clinical trials. G-CSF once daily in the morning for 4 consecutive days prior to the first dose of plerixafor and every morning before apheresis).
In patients with a creatinine clearance of 20-50 ml / min, the dose of plerixafor should be reduced by one third to 0.16 mg / kg / day. There are incomplete clinical data on this dose modification. There are no dose recommendations for patients with creatinine clearance <20 ml / min and hemodialyzed patients. For patients with a creatinine clearance of <50 ml / min, do not exceed 27 mg of plerixafor / day. There is no need to modify the dosage in elderly patients with normal renal function.