Is Everolimus safe while breastfeeding?

Summary of use during breastfeeding

The amounts of everolimus in milk is very small and would provide a dose less than dosages reportedly used safely in neonates of 0.1 to 0.5 mg daily. If a mother requires everolimus, it is not a reason to discontinue breastfeeding

Effects on the breastfed infant

A review of the Transplant Pregnancy Registry International database from 1999 to 2024 found that one mother with a transplant had breastfed her infant for at least 4 weeks while taking everolimus, although no infant outcome was reported.[4]

A woman with a liver transplant was taking prednisolone, cyclosporine, and everolimus 0.25 mg once daily during pregnancy and postpartum while breastfeeding. Initially, approximately 70% of the infant’s feeding consisted of breast milk. This proportion decreased to approximately 50% by 2 weeks postpartum. Breastfeeding was gradually tapered and continued until 10 months postpartum. The infant showed normal growth throughout infancy and no developmental abnormalities at 1 year of age.[3]

Effects on milk supply

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

Levels in milk

Maternal Levels. A woman was receiving everolimus 2 mg 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]

A woman with a kidney transplant received azathioprine 125 mg, methylprednisolone 12 mg, and everolimus 0.5 mg daily during pregnancy and postpartum. On the second day postpartum, 6 colostrum samples were collected. The pre-dose level was 33 ng/L. The highest level was 66 ng/L at 4 hours after the dose. Samples taken at 2, 6, 8 and 12 hours after the dose contained concentrations that ranged from 45 to 51 ng/L. The authors estimated the maximal dose of everolimus in colostrum (RID) was 0.38% of the mother’s dose.[2]

A woman with a liver transplant was taking prednisolone, cyclosporine, and everolimus 0.25 mg once daily during pregnancy and postpartum while breastfeeding. Breast milk samples were collected immediately before everolimus administration and at 3, 6, 9, and 12 hours after dosing on postpartum day 5. The highest milk concentration of 0.117 mcg/L was found at 9 hours after the dose. Based on the AUC0-24 analysis, the authors estimated the RID to be 0.30%.[3]

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

Alternatives LactMed lists

• Azathioprine
• Cyclosporine
• Tacrolimus