Can I take Nilotinib while breastfeeding?

Although one breastfed infants apparently experienced no adverse effects during maternal use of nilotinib, no long-term data are available. Because there is little published experience with nilotinib during breastfeeding, an alternate drug may be preferred, especially while nursing a newborn or preterm infant.

Drug levels

Maternal Levels. A woman receiving oral imatinib 400 mg daily for chronic myeloid leukemia breastfed her infant. During week 4 postpartum, serum and milk levels of imatinib and its active metabolite (CGP 74588) were measured before and at several times during the 9 hours after the dose. The highest concentrations of imatinib and its metabolite were at 2 and 4 hours after the dose. Peak concentrations of imatinib ranged between 1.1 and 1.4 mg/L and were 0.8 mg/L for the metabolite. The concentrations of both were 25 to 50% lower 9 hours after the dose. Milk and serum levels were also measured during the second month of breastfeeding with similar results (details not reported).[2] Using these data, the estimated maximum dosage of the drug and metabolite that a fully breastfed infant would receive is 0.3 mg/kg daily or 4.5% of the maternal weight-adjusted dosage.

A woman who was 7 days postpartum and had been taking imatinib 400 mg daily since the middle of her pregnancy had a single milk sample analyzed for the drug an its metabolite. Imatinib concentration 15 hours after a dose was 596 mcg/L and CGP 74588 was 1513 mcg/L. The authors estimated that a fully breastfed infant would receive between 1.2 and 2 mg of the drug and metabolite daily with this maternal dose.[3]

A woman who took imatinib 400 mg daily during pregnancy and postpartum delivered a normal infant, but did not breastfeed. Breastmilk imatinib concentrations were measured on the 7th, 14th, 15th and 16th days postpartum at times ranging from 10 to 16 hours after the previous dose. Breastmilk concentrations ranged between 1.4 and 2.6 mg/L.[4]

A woman with chronic myeloid leukemia was begun on imatinib 400 mg daily immediately after delivery. She did not breastfeed, but 5 breastmilk samples were obtained over the 7 days after the first dose, on days 1, 2, 3 and 7 postpartum, apparently 3 hours after the daily doses (exact times not stated). Imatinib milk levels were about half of maternal plasma levels and ranged from 151 to 1153 mcg/L. Milk levels of the metabolite, N-desmethylimatinib were about 3 times those in maternal plasma and ranged from 409 to 1052 mcg/L.[5]

A woman received imatinib 400 mg daily beginning in week 30 of pregnancy. Colostrum and milk samples obtained during the first 5 days postpartum contained an average of 0.233 mg/L of imatinib and 0.529 mg/L of n-desmethylimatinib, the active metabolite. The authors estimated that an exclusively breastfed infant would ingest a mean of 0.12 mg/kg daily of the active drug (imatinib plus metabolite).[6] This would be approximately 1.8% of the weight-adjusted maternal dosage.

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

Effects in breastfed infants

Maternal Levels. A woman receiving oral imatinib 400 mg daily for chronic myeloid leukemia breastfed her infant. During week 4 postpartum, serum and milk levels of imatinib and its active metabolite (CGP 74588) were measured before and at several times during the 9 hours after the dose. The highest concentrations of imatinib and its metabolite were at 2 and 4 hours after the dose. Peak concentrations of imatinib ranged between 1.1 and 1.4 mg/L and were 0.8 mg/L for the metabolite. The concentrations of both were 25 to 50% lower 9 hours after the dose. Milk and serum levels were also measured during the second month of breastfeeding with similar results (details not reported).[2] Using these data, the estimated maximum dosage of the drug and metabolite that a fully breastfed infant would receive is 0.3 mg/kg daily or 4.5% of the maternal weight-adjusted dosage.

A woman who was 7 days postpartum and had been taking imatinib 400 mg daily since the middle of her pregnancy had a single milk sample analyzed for the drug an its metabolite. Imatinib concentration 15 hours after a dose was 596 mcg/L and CGP 74588 was 1513 mcg/L. The authors estimated that a fully breastfed infant would receive between 1.2 and 2 mg of the drug and metabolite daily with this maternal dose.[3]

A woman who took imatinib 400 mg daily during pregnancy and postpartum delivered a normal infant, but did not breastfeed. Breastmilk imatinib concentrations were measured on the 7th, 14th, 15th and 16th days postpartum at times ranging from 10 to 16 hours after the previous dose. Breastmilk concentrations ranged between 1.4 and 2.6 mg/L.[4]

A woman with chronic myeloid leukemia was begun on imatinib 400 mg daily immediately after delivery. She did not breastfeed, but 5 breastmilk samples were obtained over the 7 days after the first dose, on days 1, 2, 3 and 7 postpartum, apparently 3 hours after the daily doses (exact times not stated). Imatinib milk levels were about half of maternal plasma levels and ranged from 151 to 1153 mcg/L. Milk levels of the metabolite, N-desmethylimatinib were about 3 times those in maternal plasma and ranged from 409 to 1052 mcg/L.[5]

A woman received imatinib 400 mg daily beginning in week 30 of pregnancy. Colostrum and milk samples obtained during the first 5 days postpartum contained an average of 0.233 mg/L of imatinib and 0.529 mg/L of n-desmethylimatinib, the active metabolite. The authors estimated that an exclusively breastfed infant would ingest a mean of 0.12 mg/kg daily of the active drug (imatinib plus metabolite).[6] This would be approximately 1.8% of the weight-adjusted maternal dosage.

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.

References

1. Alizadeh H, Jaafar H, Kajtar B . Outcome of 3 pregnancies in a patient with chronic myeloid leukemia who received 3 types of tyrosine kinase inhibitors each in different pregnancy: Follow-up of the case with a review of published reports. Ann Saudi Med. 2015;35:468-71. PMID: 26657232

Last Revision Date

20160401

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 Nilotinib molecule

MolView – data visualization platform