Last update Nov. 25, 2024

Everolimus

Limited compatibility

Unsafe. Moderate/severe adverse effects. Compatible under certain circumstances. Follow-up recommended. Use safer alternative or discontinue breastfeeding from 5 to 7 T ½ . Read Commentary.

Everolimus is a macrolide, a derivative of sirolimus, with immunosuppressive properties. It is used in the prevention of graft rejection in heart, kidney or liver transplant patients and in the treatment of certain cancers. It frequently causes potentially serious adverse effects: infections, anemia, anemia, thrombopenia, leukolymphopenia, anorexia, irritability, weight loss, increased liver enzymes... (Everolimius 2013).  Oral administration once or twice daily.

Its pharmacokinetic data (large volume of distribution and high molecular weight) make it unlikely to pass into breast milk in clinically significant quantities. There are published data on its excretion in colostrum, which is undetectable or negligible (Kociszewska 2017, Fiocchi 2016).

Its low oral bioavailability makes it difficult to pass into infant plasma from ingested breast milk, except in premature infants and immediate neonatal period where there may be higher intestinal permeability.

Expert authors consider breastfeeding compatible with the mother taking this drug, especially in the first days after delivery (Kociszewska 2017).

Pending further published data on this drug in relation to breastfeeding, safer known alternatives may be preferable, especially during the neonatal period and in case of prematurity.

Alternatives

  • Azathioprine (Safe product and/or breastfeeding is the best option.)
  • Ciclosporin (Safe product and/or breastfeeding is the best option.)
  • Tacrolimus (Safe product and/or breastfeeding is the best option.)

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

Your contribution is essential for this service to continue to exist. We need the generosity of people like you who believe in the benefits of breastfeeding.

Thank you for helping to protect and promote breastfeeding.

José María Paricio, founder of e-lactancia.

Other names

Everolimus in other languages or writings:

  • إيفيروليموس (Arabic)
  • Эверолимус (Cyrillic)
  • 依维莫司 (Chinese)
  • エベロリムス (Japanese)
  • (3S,6R,7E,9R,10R,12R,14S,15E,17E,19E,21S,23S,26R,27R,34aS)-9,10,12,13,14,21,22,23,24,25,26,27,32,33,34,34a-Hexadecahydro-9,27-dihydroxy-3-{(1R)-2-[(1S,3R,4R)-4-(2-hydroxyethoxy)-3-methoxycyclohexyl]-1-methylethyl}-10,21-dimethoxy-6,8,12,14,20,26-hexamethyl-23,27-epoxy-3H-pyrido[2,1-c][1,4]oxaazacyclohentriacontine-1,5,11,28,29(4H,6H,31H)-pentone (Chemical name)
  • C53H83NO14 (Molecular formula)
  • L01EG02; L04AH02 (ATC Code/s)

Tradenames

Main tradenames from several countries containing Everolimus in its composition:

Pharmacokinetics

Variable Value Unit
Oral Bioavail. 30 %
Molecular weight 958 daltons
Protein Binding 74 %
VD 1.6 l/Kg
Tmax 1 - 2 hours
30 hours
Theoretical Dose Calostro: 0.0000001 mg/Kg/d
Relative Dose 0.001 %

References

  1. Kociszewska-Najman B, Szpotańska-Sikorska M, Mazanowska N, Pączek L, Samborowska E, Dadlez M, Wielgoś M, Pietrzak B. Transfer of Everolimus into Colostrum of a Kidney Transplant Mother. Ann Transplant. 2017 Dec 19;22:755-758. Abstract Full text (link to original source)
  2. Fiocchi R, D'Elia E, Vittori C, Sebastiani R, Strobelt N, Eleftheriou G, Introna M, Freddi C, Crippa A. First Report of a Successful Pregnancy in an Everolimus-Treated Heart-Transplanted Patient: Neonatal Disappearance of Immunosuppressive Drugs. Am J Transplant. 2016 Apr;16(4):1319-22. Abstract Full text (link to original source)
  3. Constantinescu S, Pai A, Coscia LA, Davison JM, Moritz MJ, Armenti VT. Breast-feeding after transplantation. Best Pract Res Clin Obstet Gynaecol. 2014 Nov;28(8):1163-73. Abstract
  4. Everolimus Drug Summary 2013 Full text (in our servers)
  5. Everolimus Ficha técnica 2013 Full text (in our servers)

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