Tìm theo
Plerixafor
Các tên gọi khác (3) :
  • AMD3100
  • LM3100
  • Mozobil
anti hiv agents, hematopoietic agents
Thuốc Gốc
Small Molecule
CAS: 110078-46-1
ATC: L03AX16
CTHH: C28H54N8
PTK: 502.782
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.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C28H54N8
Phân tử khối
502.782
Monoisotopic mass
502.447143768
InChI
InChI=1S/C28H54N8/c1-9-29-15-17-31-13-3-21-35(23-19-33-11-1)25-27-5-7-28(8-6-27)26-36-22-4-14-32-18-16-30-10-2-12-34-20-24-36/h5-8,29-34H,1-4,9-26H2
InChI Key
InChIKey=YIQPUIGJQJDJOS-UHFFFAOYSA-N
IUPAC Name
1-{[4-(1,4,8,11-tetraazacyclotetradecan-1-ylmethyl)phenyl]methyl}-1,4,8,11-tetraazacyclotetradecane
Traditional IUPAC Name
plerixafor
SMILES
C(N1CCCNCCNCCCNCC1)C1=CC=C(CN2CCCNCCNCCCNCC2)C=C1
Độ tan chảy
131.5 °C
Độ hòa tan
Soluble
logP
-0.43
logS
-4
pKa (Strongest Basic)
10.54
PSA
78.66 Å2
Refractivity
155.01 m3·mol-1
Polarizability
60.51 Å3
Rotatable Bond Count
4
H Bond Acceptor Count
8
H Bond Donor Count
6
Physiological Charge
4
Number of Rings
3
Bioavailability
0
pKa
6.0 - 7.5
Dược Lực Học : Plerixafor is a bicyclam derivative that antagonizes CXCR4 by binding to three acidic residues in the ligand-binding pocket: Asp171, Asp262, and Glu288. Blood levels of CD34+ cells peaked at 9 hours after administration of 0.24 mg/kg plerixafor in healthy subjects. In patients that have non-Hodgkin’s lymphoma or multiple myeloma, blood levels of CD34+ peaked at 6 hours. In combination with a G-CSF, circulating CD34+ cells in the peripheral blood peaked at 9-14 hours.
Cơ Chế Tác Dụng : 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. Plerixafor inhibits the CXCR4 chemokine receptors on CD34+ cells and reversibly blocks binding of the ligand, stromal cell-derived factor-1-alpha (SDF-1α). By blocking the interaction between SDF-1α 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.
Dược Động Học :
▧ 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.
▧ Volume of Distribution :
0.3 L/kg
▧ Protein binding :
58%
▧ Metabolism :
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.
▧ Half Life :
Terminal elimination half-life, NHL patients: 4.4 hours; Terminal elimination half-life, MM patients: 5.6 hours; Terminal elimination half-life, Hodgkin's lymphoma patients: 3.5 hours; Distribution half-life: 0.3 hours
▧ Clearance :
Total plasma clearance: 4.38 L/h; Renal clearance: 3.15 L/h
Độc Tính : LD50, mouse, SC: 16.3 mg/kg; LD50, rat, SC: >50 mg/kg; LD50, mouse and rat, IV injection: 5.2 mg/kg
Chỉ Định : 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).
Liều Lượng & Cách Dùng : Injection - Subcutaneous - 20 mg/mL
Dữ Kiện Thương Mại
Nhà Sản Xuất
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB06809
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=65015
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=99443297
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D08971
ChemSpider
http://www.chemspider.com/Chemical-Structure.58531.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/58468-0140-1
PharmGKB
http://www.pharmgkb.org/drug/PA165958410
Wikipedia
http://en.wikipedia.org/wiki/Plerixafor
RxList
http://www.rxlist.com/mozobil-drug.htm
Drugs.com
http://www.drugs.com/ppa/plerixafor.html
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