Last update Aug. 30, 2021

1,1′-(1,4-Phenylenebismethylene)bis(1,4,8,11-tetraazacyclotetradecane)

Likely Compatibility

Fairly safe. Mild or unlikely adverse effects. Compatible under certain circumstances. Follow-up recommended. Read Commentary.

Plerixafor is a selective CXCR4 chemokine receptor antagonist. It causes leukocytosis and elevated levels of hematopoietic progenitor cells.
Indicated, in combination with a granulocyte colony stimulating factor, to enhance the mobilization of hematopoietic stem cells into peripheral blood for their collection and subsequent autologous transplantation in patients with non-Hodgkin’s lymphoma or multiple myeloma.
Authorized use in patients from one year of age.
Daily subcutaneous administration for 2 to 4 and up to 7 days.

At the date of the last update, there was no available published data on its excretion in breast milk.

Its pharmacokinetic data (large volume of distribution and moderately high molecular weight) make it unlikely to pass into breast milk in a clinically significant amount.

Its null oral bioavailability (Pettersson 2008, Rosenkilde 2007 and 2004) prevents the passage to plasma of the infant from ingested breast milk, except perhaps in the premature and during the immediate neonatal period during which there may be greater intestinal permeability.

Its possible frequent side effects (mainly gastrointestinal) are not serious and should be monitored for in the infant.

Alternatives

We do not have alternatives for 1,1′-(1,4-Phenylenebismethylene)bis(1,4,8,11-tetraazacyclotetradecane) .

Suggestions made at e-lactancia are done by APILAM team of health professionals, and are based on updated scientific publications. It is not intended to replace the relationship you have with your doctor but to compound it. The pharmaceutical industry contraindicates breastfeeding, mistakenly and without scientific reasons, in most of the drug data sheets.

Jose Maria Paricio, Founder & President of APILAM/e-Lactancia

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José María Paricio, founder of e-lactancia.

Other names

1,1′-(1,4-Phenylenebismethylene)bis(1,4,8,11-tetraazacyclotetradecane) is Plerixafor in Chemical name.

Is written in other languages:

1,1′-(1,4-Phenylenebismethylene)bis(1,4,8,11-tetraazacyclotetradecane) is also known as

Group

1,1′-(1,4-Phenylenebismethylene)bis(1,4,8,11-tetraazacyclotetradecane) belongs to this group or family:

Tradenames

Main tradenames from several countries containing 1,1′-(1,4-Phenylenebismethylene)bis(1,4,8,11-tetraazacyclotetradecane) in its composition:

Pharmacokinetics

Variable Value Unit
Oral Bioavail. ≈ 0 %
Molecular weight 503 daltons
Protein Binding 58 %
VD 0.3 l/Kg
Tmax 0.5 - 1 hours
3 - 5 hours

References

  1. Sanofi A. Plerixafor Drug Summary. 2019 Full text (in our servers)
  2. EMA. Plerixafor. Ficha técnica. 2014 Full text (in our servers)
  3. Pettersson S, Pérez-Nueno VI, Ros-Blanco L, Puig de La Bellacasa R, Rabal MO, Batllori X, Clotet B, Clotet-Codina I, Armand-Ugón M, Esté J, Borrell JI, Teixidó J. Discovery of novel non-cyclam polynitrogenated CXCR4 coreceptor inhibitors. ChemMedChem. 2008 Oct;3(10):1549-57. Abstract
  4. Rosenkilde MM, Gerlach LO, Hatse S, Skerlj RT, Schols D, Bridger GJ, Schwartz TW. Molecular mechanism of action of monocyclam versus bicyclam non-peptide antagonists in the CXCR4 chemokine receptor. J Biol Chem. 2007 Sep 14;282(37):27354-27365. Abstract Full text (link to original source)
  5. Rosenkilde MM, Gerlach LO, Jakobsen JS, Skerlj RT, Bridger GJ, Schwartz TW. Molecular mechanism of AMD3100 antagonism in the CXCR4 receptor: transfer of binding site to the CXCR3 receptor. J Biol Chem. 2004 Jan 23;279(4):3033-41. Epub 2003 Oct 28. Abstract Full text (link to original source)

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