Identification | |
---|---|
Name | Plerixafor |
Accession Number | DB06809 |
Type | small molecule |
Description | Plerixafor is a hematopoietic stem cell mobilizer. It is used to stimulate the release of stem cells from the bone marrow into the blood in patients with non-Hodgkin lymphoma and multiple myeloma for the purpose of stimulating the immune system. These stem cells are then collected and used in autologous stem cell transplantation to replace blood-forming cells that were destroyed by chemotherapy. Plerixafor has orphan drug status in the United States and European Union; it was approved by the U.S. Food and Drug Administration on December 15, 2008. |
Structure |
|
Categories (*) | |
Molecular Weight | 502.782 |
Groups | approved |
Monoisotopic Weight | 502.447143768 |
Pharmacology | |
Indication | Used in combination with granulocyte-colony stimulating factor (G-CSF, filgrastim) 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). |
Mechanism of action | Plerixafor inhibits the CXCR4 chemokine receptors on CD34+ cells and reversibly blocks binding of the ligand, stromal cell-derived factor-1-alpha (SDF-1?). By blocking the interaction between SDF-1? and CXCR4 with plerixafor, mobilization of progenitor cells is triggered. Filgrastim, a granulocyte-colony stimulating factor, is added to enhance CD34+ cell mobilization, thus increasing the yield of stem cells- an important determinant of graft adequacy. |
Absorption | Pharmacokinetic profile follows a two-compartment model with first-order absorption. A median peak plasma concentration of 0.24 mg/kg of plerixafor occurred 30-60 minutes after subcutaneous dose. |
Protein binding | 58% |
Biotransformation | Metabolism does not involved CYP isoenzymes |
Route of elimination | 0.24 mg/kg, healthy subjects: ~70% of the parent drug is excreted in urine in the first 24 hours. |
Toxicity | LD50, mouse, SC: 16.3 mg/kg; LD50, rat, SC: >50 mg/kg; LD50, mouse and rat, IV injection: 5.2 mg/kg |
Affected organisms |
|
Interactions | |
Drug Interactions | Not Available |
Food Interactions | Not Available |
C-X-C chemokine receptor type 4 | |
---|---|
Name | C-X-C chemokine receptor type 4 |
Gene Name | CXCR4 |
Pharmacological action | yes |
Actions | antagonist |
References |
|
DTHybrid score | 1.2375 |
Id | Partner name | Gene Name | Score |
---|---|---|---|
308 | 30S ribosomal protein S12 | rpsL | 0.2124 |
6704 | 30S ribosomal protein S12 | rpsL | 0.2124 |