Peringatan Keamanan

There is limited data about the effects of plerixafor at doses higher than the recommended (0.24 mg/kg subcutaneously). However, the frequency of gastrointestinal disorders, vasovagal reactions, orthostatic hypotension, and/or syncope may be higher.L45678 The carcinogenicity of plerixafor has not been evaluated, and the effect of plerixafor on human fertility is unknown. According to the results from an in vitro bacterial mutation assay, an in vitro chromosomal aberration test, and an in vivo bone marrow micronucleus test in rats after subcutaneous doses up to 25 mg/kg, plerixafor is not genotoxic.L45678 In mice and rats, the LD50 of plerixafor by intravenous injection is 5 mg/kg. The LD50 of plerixafor by subcutaneous injection is 16 mg/kg in mice and >50 mg/kg in rats/.L45688

Plerixafor

DB06809

small molecule approved investigational

Deskripsi

Plerixafor is a small-molecule inhibitor of C-X-C chemokine receptor type 4 (CXCR4) that acts as a hematopoietic stem cell mobilizer.A7117,L45678 It is used to stimulate the release of stem cells from the bone marrow into the blood in patients with non-Hodgkin's lymphoma (NHL) and multiple myeloma to stimulate their immune system. These stem cells are then collected and used in autologous stem cell transplantation to replace blood-forming cells destroyed by chemotherapy.A7118,L45678

As an inhibitor of CXCR4, plerixafor blocks the binding of its ligand, stromal cell-derived factor-1-alpha (SDF-1?). Since CXCR4 and SDF-1? are involved in the trafficking and homing of CD34+ cells to the marrow compartment, blocking this interaction leads to an increase in CD34+ cell circulating levels.A7117 Compared to placebo with G-CSF, the plerixafor and G-CSF mobilization regimen has a higher probability of achieving the optimal CD34+ cell target for tandem transplantation in fewer apheresis procedures.A7115

Plerixafor has orphan drug status in the United States and European Union and was approved by the US Food and Drug Administration on December 15, 2008.A7117,L45678

Struktur Molekul 2D

Berat 502.782
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) Plerixafor has a distribution half-life of 0.3 hours and a terminal population half-life of 5.3 hours in patients with normal renal function. In studies with healthy subjects and patients, the terminal half-life in plasma ranges between 3 and 5 hours.[L45678] In patients with non-Hodgkin lymphoma, the terminal half-life of plerixafor is 4.4 hours, and in patients with multiple myeloma, the terminal half-life is 5.6 hours.[A7116]
Volume Distribusi Plerixafor has an apparent volume of distribution of 0.3 L/kg.[L45678]
Klirens (Clearance) Plerixafor has a total plasma clearance of 4.38 L/h, and a renal clearance of 3.15 L/h.[A7116,A258423]

Absorpsi

Plerixafor follows a two-compartment pharmacokinetic profile with first-order absorption and exhibits linear kinetics between 0.04 mg/kg and 0.24 mg/kg. The pharmacokinetic profile of plerixafor in healthy subjects was similar to the one observed in patients with non-Hodgkin’s lymphoma (NHL) and multiple myeloma (MM) who received plerixafor in combination with granulocyte-colony stimulating factor (G-CSF). In addition, the clearance of plerixafor has a significant relationship with creatinine clearance (CLCR). The population pharmacokinetic analysis showed that, with increasing body weight, a mg/kg-based dosage leads to a higher plerixafor exposure (AUC0-24h). However, NHL patients (<70 kg) given a fixed dose of 20 mg of plerixafor had an AUC0-10h 1.43-fold higher than the one detected in patients given 0.24 mg/kg of plerixafor. Therefore, a body weight of 83 kg was selected as an appropriate cut-off point to transition patients from fixed to weight-based dosing.L45678 Peak concentrations are reached in approximately 30-60 minutes (tmax) following subcutaneous injection.L45678,L45683 In patients given 0.24 mg/kg of plerixafor subcutaneously after receiving 4-days of G-CSF pre-treatment, the Cmax and AUC0-24 were 887 ng/ml and 4337 ng·hr/ml, respectively.L45683

Metabolisme

Plerixafor is not metabolized by the liver and is not a metabolism-dependent inhibitor of major cytochrome P450 enzymes, including 1A2, 2C9, 2C19, 2D6 and 3A4. In addition, it does not induce cytochrome P450 1A2, 2B6, or 3A4 enzymes.L45678 Plerixafor is metabolically stable, and in vivo studies in rats and dogs showed that the non-parent radiolabelled components in plasma and urine were Cu2+ complexes with plerixafor. This is consistent with the presence of two cyclam rings in plerixafor, which may act as potential chelating sites.L45713

Rute Eliminasi

Plerixafor is mainly eliminated through urine. In healthy volunteers with normal renal function given 0.24 mg/kg of plerixafor, approximately 70% of the parent drug is excreted in urine in the first 24 hours. An in vitro study with MDCKII and MDCKII-MDR1 cell models found that plerixafor is not a substrate or inhibitor of P-glycoprotein.L45678

Interaksi Obat

727 Data
Cyclosporine Cyclosporine may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Icosapent Icosapent may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Cefotiam Cefotiam may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Mesalazine Mesalazine may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Cefmenoxime Cefmenoxime may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Cefmetazole Cefmetazole may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Pamidronic acid Pamidronic acid may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Tenofovir disoproxil Tenofovir disoproxil may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Indomethacin Indomethacin may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Cidofovir Cidofovir may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Cefpiramide Cefpiramide may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Ceftazidime Ceftazidime may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Loracarbef Loracarbef may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Cefalotin Cefalotin may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Nabumetone Nabumetone may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Ketorolac Ketorolac may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Tenoxicam Tenoxicam may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Celecoxib Celecoxib may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Cefotaxime Cefotaxime may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Tolmetin Tolmetin may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Foscarnet Foscarnet may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Rofecoxib Rofecoxib may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Piroxicam Piroxicam may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Methotrexate Methotrexate may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Cephalexin Cephalexin may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Fenoprofen Fenoprofen may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Valaciclovir Valaciclovir may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Valdecoxib Valdecoxib may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Diclofenac Diclofenac may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Sulindac Sulindac may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Bacitracin Bacitracin may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Amphotericin B Amphotericin B may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Cephaloglycin Cephaloglycin may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Flurbiprofen Flurbiprofen may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Adefovir dipivoxil Adefovir dipivoxil may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Pentamidine Pentamidine may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Etodolac Etodolac may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Mefenamic acid Mefenamic acid may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Acyclovir Acyclovir may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Naproxen Naproxen may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Sulfasalazine Sulfasalazine may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Phenylbutazone Phenylbutazone may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Meloxicam Meloxicam may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Carprofen Carprofen may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Cefaclor Cefaclor may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Diflunisal Diflunisal may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Tacrolimus Tacrolimus may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Ceforanide Ceforanide may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Salicylic acid Salicylic acid may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Meclofenamic acid Meclofenamic acid may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Acetylsalicylic acid Acetylsalicylic acid may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Carboplatin Carboplatin may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Oxaprozin Oxaprozin may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Ketoprofen Ketoprofen may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Balsalazide Balsalazide may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Ibuprofen Ibuprofen may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Cefditoren Cefditoren may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Atazanavir Atazanavir may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Colistimethate Colistimethate may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Cefuroxime Cefuroxime may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Cefapirin Cefapirin may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Cefadroxil Cefadroxil may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Cefprozil Cefprozil may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Ceftriaxone Ceftriaxone may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Olsalazine Olsalazine may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Lumiracoxib Lumiracoxib may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Cefamandole Cefamandole may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Cefazolin Cefazolin may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Cefonicid Cefonicid may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Cefoperazone Cefoperazone may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Cefotetan Cefotetan may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Cefoxitin Cefoxitin may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Ceftizoxime Ceftizoxime may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Cefradine Cefradine may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Magnesium salicylate Magnesium salicylate may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Salsalate Salsalate may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Choline magnesium trisalicylate Choline magnesium trisalicylate may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Cefepime Cefepime may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Cefacetrile Cefacetrile may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Ceftibuten Ceftibuten may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Cefpodoxime Cefpodoxime may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Antrafenine Antrafenine may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Aminophenazone Aminophenazone may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Antipyrine Antipyrine may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Tiaprofenic acid Tiaprofenic acid may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Lopinavir Lopinavir may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Etoricoxib Etoricoxib may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Hydrolyzed Cephalothin Hydrolyzed Cephalothin may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Cephalothin Group Cephalothin Group may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Oxyphenbutazone Oxyphenbutazone may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Latamoxef Latamoxef may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Nimesulide Nimesulide may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Benoxaprofen Benoxaprofen may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Metamizole Metamizole may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Zomepirac Zomepirac may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Ceftobiprole Ceftobiprole may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Cimicoxib Cimicoxib may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Ceftaroline fosamil Ceftaroline fosamil may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Lornoxicam Lornoxicam may decrease the excretion rate of Plerixafor which could result in a higher serum level.
Aceclofenac Aceclofenac may decrease the excretion rate of Plerixafor which could result in a higher serum level.

Target Protein

C-X-C chemokine receptor type 4 CXCR4

Referensi & Sumber

Synthesis reference: Xu, D., et al. (1997). Process for preparing 1,1'-1,4-phenylenebis-(methylene)-bis-1,4,8,11-tetraazacyclotetradecane (U.S. Patent No. 5,612,478 A). U.S. Patent and Trademark Office. https://patentimages.storage.googleapis.com/23/2a/c4/cdec2e80dbe460/US5612478.pdf
Artikel (PubMed)
  • PMID: 18847313
    Uy GL, Rettig MP, Cashen AF: Plerixafor, a CXCR4 antagonist for the mobilization of hematopoietic stem cells. Expert Opin Biol Ther. 2008 Nov;8(11):1797-804. doi: 10.1517/14712598.8.11.1797 .
  • PMID: 18922110
    Fricker SP: A novel CXCR4 antagonist for hematopoietic stem cell mobilization. Expert Opin Investig Drugs. 2008 Nov;17(11):1749-60. doi: 10.1517/13543784.17.11.1749 .
  • PMID: 19363221
    DiPersio JF, Stadtmauer EA, Nademanee A, Micallef IN, Stiff PJ, Kaufman JL, Maziarz RT, Hosing C, Fruehauf S, Horwitz M, Cooper D, Bridger G, Calandra G: Plerixafor and G-CSF versus placebo and G-CSF to mobilize hematopoietic stem cells for autologous stem cell transplantation in patients with multiple myeloma. Blood. 2009 Jun 4;113(23):5720-6. doi: 10.1182/blood-2008-08-174946. Epub 2009 Apr 10.
  • PMID: 19135941
    Stewart DA, Smith C, MacFarland R, Calandra G: Pharmacokinetics and pharmacodynamics of plerixafor in patients with non-Hodgkin lymphoma and multiple myeloma. Biol Blood Marrow Transplant. 2009 Jan;15(1):39-46. doi: 10.1016/j.bbmt.2008.10.018.
  • PMID: 20530974
    Brave M, Farrell A, Ching Lin S, Ocheltree T, Pope Miksinski S, Lee SL, Saber H, Fourie J, Tornoe C, Booth B, Yuan W, He K, Justice R, Pazdur R: FDA review summary: Mozobil in combination with granulocyte colony-stimulating factor to mobilize hematopoietic stem cells to the peripheral blood for collection and subsequent autologous transplantation. Oncology. 2010;78(3-4):282-8. doi: 10.1159/000315736. Epub 2010 Jun 8.
  • PMID: 20009003
    Choi HY, Yong CS, Yoo BK: Plerixafor for stem cell mobilization in patients with non-Hodgkin's lymphoma and multiple myeloma. Ann Pharmacother. 2010 Jan;44(1):117-26. doi: 10.1345/aph.1M380. Epub 2009 Dec 15.
  • PMID: 21861545
    Keating GM: Plerixafor: a review of its use in stem-cell mobilization in patients with lymphoma or multiple myeloma. Drugs. 2011 Aug 20;71(12):1623-47. doi: 10.2165/11206040-000000000-00000.
  • PMID: 19748593
    MacFarland R, Hard ML, Scarborough R, Badel K, Calandra G: A pharmacokinetic study of plerixafor in subjects with varying degrees of renal impairment. Biol Blood Marrow Transplant. 2010 Jan;16(1):95-101. doi: 10.1016/j.bbmt.2009.09.003. Epub 2009 Sep 10.

Contoh Produk & Brand

Produk: 19 • International brands: 1
Produk
  • Mozobil
    Solution • 24 mg/1.2mL • Subcutaneous • US • Approved
  • Mozobil
    Injection, solution • 24 mg/1.2mL • Subcutaneous • US • Approved
  • Mozobil
    Solution • 20 mg / mL • Subcutaneous • Canada • Approved
  • Mozobil
    Injection, solution • 20 mg/ml • Subcutaneous • EU • Approved
  • Plerixafor
    Injection, solution • 24 mg/1.2mL • Subcutaneous • US • Generic • Approved
  • Plerixafor
    Solution • 24 mg/1.2mL • Subcutaneous • US • Generic • Approved
  • Plerixafor
    Solution • 24 mg/1.2mL • Subcutaneous • US • Generic • Approved
  • Plerixafor
    Injection, solution • 24 mg/1.2mL • Subcutaneous • US • Generic • Approved
Menampilkan 8 dari 19 produk.
International Brands
  • Mozobil — Genzyme Corporation

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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