Nilotinib

The Basics

What is Nilotinib?

Used to treat chronic myelogenous leukemia-CML.

Brand names for Nilotinib

Tasigna

How Nilotinib is classified

Antineoplastic Agents, Enzyme Inhibitors, Protein Kinase Inhibitors, Signal Transduction Inhibitors, Tyrosine Kinase Inhibitors

Nilotinib During Pregnancy

Nilotinib pregnancy category

Category DNote that the FDA has deprecated the use of pregnancy categories, so for some medications, this information isn’t available. We still think it’s useful to list historical info, however, given what a common proxy this has been in the past.

What we know about taking Nilotinib while pregnant

Based on its mechanism of action and findings in animals, Tasigna may cause fetal harmwhen administered to a pregnant woman. There are no adequate and well controlledstudies with Tasigna in pregnant women. Women should be advised to avoid becomingpregnant while on Tasigna. If this drug is used during pregnancy, or if the patientbecomes pregnant while taking this drug, the patient should be apprised of the potentialhazard to the fetus.Nilotinib was studied for effects on embryo-fetal development in pregnant rats andrabbits given oral doses of 10, 30, 100 mg/kg/day, and 30, 100, 300 mg/kg/day,respectively, during organogenesis. In rats, nilotinib at doses of 100 mg/kg/day(approximately 5.7 times the AUC in patients at the dose of 400 mg twice daily) wasassociated with maternal toxicity (decreased gestation weight, gravid uterine weight, netweight gain, and food consumption). Nilotinib at doses ≥30 mg/kg/day (approximately 2times the AUC in patients at the dose of 400 mg twice daily) resulted in embryo-fetaltoxicity as shown by increased resorption and post-implantation loss, and at 100mg/kg/day a decrease in viable fetuses. In rabbits, maternal toxicity at 300 mg/kg/day(approximately one-half the human exposure based on AUC) was associated withmortality, abortion, decreased gestation weights and decreased food consumption.Embryonic toxicity (increased resorption) and minor skeletal anomalies were observed ata dose of 300 mg/kg/day. Nilotinib is not considered teratogenic.When pregnant rats were dosed with nilotinib during organogenesis and throughlactation, the adverse effects included a longer gestational period, lower pup bodyweights until weaning and decreased fertility indices in the pups when they reachedmaturity, all at a maternal dose of 360 mg/m2 (approximately 0.7 times the clinical doseof 400 mg twice daily based on body surface area). At doses up to 120 mg/m2(approximately 0.25 times the clinical dose of 400 mg twice daily based on body surfacearea) no adverse effects were seen in the maternal animals or the pups.

Taking Nilotinib While Breastfeeding

What are recommendations for lactation if you're taking Nilotinib?

Although the amount of nilotinib in milk appears to be small and one breastfed infants apparently experienced no adverse effects during maternal use of nilotinib, no long-term data are available. Because nilotinib is 98% bound to plasma proteins, the amounts in milk are likely to be low. However, there is little published experience with nilotinib during breastfeeding, and an alternate drug may be preferred, especially while nursing a newborn or preterm infant. The manufacturer recommends that breastfeeding be discontinued during nilotinib therapy and for 14 days after the last dose.

Maternal / infant drug levels

Although the amount of nilotinib in milk appears to be small and one breastfed infants apparently experienced no adverse effects during maternal use of nilotinib, no long-term data are available. Because nilotinib is 98% bound to plasma proteins, the amounts in milk are likely to be low. However, there is little published experience with nilotinib during breastfeeding, and an alternate drug may be preferred, especially while nursing a newborn or preterm infant. The manufacturer recommends that breastfeeding be discontinued during nilotinib therapy and for 14 days after the last dose.

Possible effects of Nilotinib on milk supply

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

Possible alternatives to Nilotinib

Imatinib.