Drug Interactions of Dasatinib and Nilotinib

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Drug Interactions:11,12 Dasatinib is a substrate for CYP3A4. Therefore, drugs

that inhibit this isozyme (e.g., ketoconazole, itraconazole, erythromycin, cla­

rithromycin, ritonavir, atazanavir, indinavir, nefazodone, nelfinavir,

saquinavir, and telithromycin) may increase dasatinib concentrations.

Concomitant use of such drugs with dasatinib should be avoided. If systemic

administration of a potent CYP3A4 inhibitor cannot be avoided, close monitoring

for toxicity and dosage reduction should be considered. Drugs that induce CYP3A4

(e.g., dexamethasone, phenytoin, carbamazepine, and phenobarbital) may decrease

dasatinib concentrations. Alternative agents with less enzyme-induction

potential should be used, or a dosage increase of dasatinib should be

considered. St. 's wort (Hypericum perforatum ) may decrease dasatinib

plasma concentrations unpredictably; thus, patients taking dasatinib should not

take St. 's wort. Click on this website to read the entire warning.

http://www.uspharmacist.com/content/d/+/c/10368/

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Adverse Reactions9-11: In clinical trials, the most commonly reported adverse

reactions (>10%) associated with nilotinib therapy were rash, pruritus, nausea,

fatigue, headache, constipation, diarrhea, and vomiting. Less common, but more

severe, adverse effects included thrombocytopenia, neutropenia, pneumonia,

febrile neutropenia, leukopenia, intracranial hemorrhage, elevated lipase, and

pyrexia. Nilotinib has been reported to cause concentration-dependent QT

prolongation, prompting a black box warning for possible life-threatening

irregular heartbeat and sudden death. Patients should consult with their

physician about avoiding other medications that can cause heart problems when

taking nilotinib. Women are advised to avoid breastfeeding or becoming pregnant

while taking nilotinib (Pregnancy Category D). Nilotinib is supplied as 200-mg

hard gelatin capsules in blister packs. The recommended initial dosage is 400 mg

orally twice daily, at 12-hour intervals. No food should be consumed at least

two hours before and one hour after administration of nilotinib.

http://prod.uspharmacist.com/content/d/featured_articles/c/10996/

Warning labels on drugs and what they mean.

http://prod.uspharmacist.com/content/c/12279/

This might answer a few lingering questions.

Blessings,

Lottie