DB06809 - Plerixafor
| 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 |
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| Interactions | |
| Drug Interactions | Not Available |
| Food Interactions | Not Available |
Targets
| 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 |
Predictions
| Id | Partner name | Gene Name | Score |
|---|---|---|---|
| 308 | 30S ribosomal protein S12 | rpsL | 0.2124 |
| 6704 | 30S ribosomal protein S12 | rpsL | 0.2124 |