Also known as Afinitor, Certican, Everolimus, RAD 001, RAD001, Votubia, Zortress

A derivative of the natural macrocyclic lactone sirolimus with immunosuppressant and anti-angiogenic properties. In cells, everolimus binds to the immunophilin FK Binding Protein-12 (FKBP-12) to generate an immunosuppressive complex that binds to and inhibits the activation of the mammalian Target of Rapamycin (mTOR), a key regulatory kinase. Inhibition of mTOR activation results in the inhibition of T lymphocyte activation and proliferation associated with antigen and cytokine (IL-2, IL-4, and IL-15) stimulation and the inhibition of antibody production. (NCI05)

Originator: NCI Thesaurus | Source: The website of the National Cancer Institute (http://www.cancer.gov)

Can I take Everolimus while breastfeeding?

In one patient, everolimus was not detected in the colostrum of a mother taking everolimus; however, no information is available on the use of everolimus during breastfeeding. An alternate drug may be preferred, especially while nursing a newborn or preterm infant.

Drug levels

Maternal Levels. A woman was receiving everolimus 2 mg/kg daily and cyclosporine 1.5 mg/kg daily during pregnancy and postpartum following a heart transplant. Although she did not breastfeed, a colostrum sample was obtained one day postpartum which contained undetectable everolimus levels (<0.5 mcg/L). The timing of the sample with respect to the previous everolimus dose was not stated. Measurement of serial plasma levels of everolimus obtained transplacentally found the estimated elimination half-life of everolimus to be about 86 hours in the newborn.[1] Infant Levels. Relevant published information was not found as of the revision date.

Effects in breastfed infants

Maternal Levels. A woman was receiving everolimus 2 mg/kg daily and cyclosporine 1.5 mg/kg daily during pregnancy and postpartum following a heart transplant. Although she did not breastfeed, a colostrum sample was obtained one day postpartum which contained undetectable everolimus levels (<0.5 mcg/L). The timing of the sample with respect to the previous everolimus dose was not stated. Measurement of serial plasma levels of everolimus obtained transplacentally found the estimated elimination half-life of everolimus to be about 86 hours in the newborn.[1] Infant Levels. Relevant published information was not found as of the revision date.

Possible effects on lactation

Relevant published information was not found as of the revision date.

Alternate drugs to consider

Azathioprine, Cyclosporine , Tacrolimus

References

1. Fiocchi R, D’Elia E, Vittori C et al. First report of a successful pregnancy in an everolimus-treated heart-transplanted patient: Neonatal disappearance of immunosuppressive drugs. Am J Transplant. 2016;16:1319-22. PMID: 26555407

Last Revision Date

20160426

Disclaimer:Information presented in this database is not meant as a substitute for professional judgment. You should consult your healthcare provider for breastfeeding advice related to your particular situation. The U.S. government does not warrant or assume any liability or responsibility for the accuracy or completeness of the information on this Site.

Source: LactMed – National Library of Medicine (NLM)

3D Model of the Everolimus molecule

MolView – data visualization platform