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Nilceya
nilotinib
Black Box Warnings .
QT Prolongation and Sudden Deaths
prolonged QT and sudden deaths reported; do not use if hypokalemia, hypomagnesemia, or long QT syndrome; avoid drugs that prolong QT interval and strong CYP3A4 inhibitors; avoid food 2h before and 1h after taking dose; correct hypokalemia and hypomagnesemia prior to tx and monitor periodically; obtain ECG to monitor QTc at baseline, then 7 days after tx start, after dose adjustment, and periodically
Adult Dosing .
Dosage forms: CAP: 50 mg, 150 mg, 200 mg
Special Note
- [equivalency or interchangeability info]
- Info: not interchangeable w/ nilotinib tablets; do not substitute on a mg to mg basis
- [uses, dosing may vary]
- Info: refer to institution protocols and pkg insert prior to prescribing for uses and dosing incl. toxicity-related dose adjustments
Ph-positive CML
- [chronic phase, newly diagnosed dz]
- Dose: 300 mg PO q12h; Info: give on empty stomach, 1h before or 2h after food; may consider D/C tx if on nilotinib >3y w/ sustained molecular response; cont. monitoring BCR-ABL, CBC w/ diff after D/C q4wk x1y, then q6wk x1y, then q12wk thereafter; restart tx if molecular response lost; see pkg insert for detailed D/C and restart criteria
- [chronic phase, resistant or intolerant dz]
- Dose: 400 mg PO q12h; Info: give on empty stomach, 1h before or 2h after food; may consider D/C tx if on nilotinib >3y w/ sustained molecular response; cont. monitoring BCR-ABL, CBC w/ diff after D/C q4wk x1y, then q6wk x1y, then q12wk thereafter; restart tx if molecular response lost; see pkg insert for detailed D/C and restart criteria
- [accelerated phase, resistant or intolerant dz]
- Dose: 400 mg PO q12h; Info: give on empty stomach, 1h before or 2h after food
renal dosing
- [not defined]
- renal impairment: not defined
- HD/PD: not defined
hepatic dosing
- [newly diagnosed Ph-positive CML]
- Child-Pugh Class A, B, or C: start 200 mg q12h
- [resistant or intolerant Ph-positive CML]
- Child-Pugh Class A or B: start 300 mg q12h; Child-Pugh Class C: start 200 mg q12h
Peds Dosing .
Peds dosing is currently unavailable or not applicable for this drug.
Contraindications / Cautions .
- hypersensitivity to drug or ingredient
- hypokalemia
- hypomagnesemia
- QT prolongation
- long QT syndrome, congenital
- avoid: breastfeeding during tx and x14 days after D/C
- caution: patients of childbearing potential
- caution: UGT1A1*28 homozygous allele carriers
- caution: QT prolongation family history
- caution: torsades de pointes history
- caution: ventricular arrhythmia
- caution: bradycardia
- caution: MI, recent
- caution: CHF
- caution: cardiovascular dz
- caution: cardiovascular dz history
- caution: cardiovascular dz risk
- caution: hepatic impairment
- caution: pancreatitis history
- caution: thyroid disorder
- caution: gastrectomy, total
- caution: galactose intolerance (cap form)
- caution: lactase deficiency, severe (cap form)
- caution: glucose-galactose malabsorption (cap form)
Drug Interactions .
Overview
nilotinib
kinase inhibitor
- CYP3A4 substrate
- CYP3A4 inhibitor, moderate
- antiplatelet/anticoagulant effects
- gastric pH sensitive
- GI mucosal injury/bleeding risk
- hyperkalemia
- hyperuricemic effects
- hypocalcemia
- hypokalemia
- hyponatremia
- hypophosphatemia
- immunomodulatory effects
- myelosuppressive oncologic agent
- prolongs QT interval (known)
Contraindicated
- cisapride
- colchicine
- domperidone
- lomitapide
- posaconazole
- thioridazine
- ziprasidone
Avoid/Use Alternative
- alfentanil
- alprazolam
- amiloride
- amiodarone
- anagrelide
- apalutamide
- arsenic trioxide
- artemether/lumefantrine
- cenobamate
- ceritinib
- chikungunya vaccine, live
- chloramphenicol
- desflurane
- desipramine
- dexlansoprazole
- dexmedetomidine
- dexmedetomidine injection
- dexrazoxane
- dihydrocodeine
- dihydroergotamine
- disopyramide
- dofetilide
- donepezil
- dordaviprone
- doxorubicin
- droperidol
- efavirenz
- elacestrant
- encorafenib
- ensartinib
- entrectinib
- enzalutamide
- ephedra
- epirubicin
- erdafitinib
- ergotamine
- eribulin
- erythromycin
- fexinidazole
- fingolimod
- flecainide
- fluconazole
- fluorouracil
- fluoxetine
- fosaprepitant
- foscarnet
- fosphenytoin
- ganciclovir
- gemtuzumab ozogamicin
- gepotidacin
- gilteritinib
- givinostat
- glasdegib
- goserelin
- grapefruit
- haloperidol
- histrelin
- hydrocodone
- hydroxychloroquine
- hydroxyzine
- ibutilide
- idelalisib
- iloperidone
- influenza nasal vaccine, live
- inotuzumab ozogamicin
- midazolam
- pazopanib
- pemigatinib
- penicillamine
- pentamidine
- pexidartinib
- phenytoin
- pitolisant
- potassium phosphate
- primaquine
- procainamide
- propafenone
- radium Ra 223 dichloride
- revumenib
- ribociclib
- ritonavir
- romidepsin
- ropeginterferon alfa-2b
- rotavirus vaccine, live
- rucaparib
- selumetinib
- sertraline
- typhoid vaccine, live
- valganciclovir
- valsartan
- vandetanib
- vardenafil
- varicella vaccine, live
- vemurafenib
- venetoclax
- vonoprazan
- voriconazole
- yellow fever vaccine, live
Monitor/Modify Tx
- abemaciclib
- abiraterone acetate
- acalabrutinib
- acetazolamide
- ado-trastuzumab emtansine
- afatinib
- albendazole
- albuterol
- albuterol inhaled
- alemtuzumab
- alendronate
- alfuzosin
- aliskiren
- allopurinol
- aloe
- alteplase
- aluminum hydroxide
- amifostine
- amisulpride
- amitriptyline
- amphotericin
- anacaulase topical
- anthrax vaccine
- anti-thymocyte globulin
- antithrombin
- apixaban
- arformoterol inhaled
- argatroban
- aripiprazole oral
- asciminib
- asparaginase
- aspirin
- atidarsagene autotemcel
- atorvastatin
- auranofin
- avacopan
- avanafil
- avatrombopag
- axitinib
- azathioprine
- benazepril
- benznidazole
- berotralstat
- betamethasone
- betibeglogene autotemcel
- bevacizumab
- binimetinib
- bivalirudin
- brentuximab vedotin
- brexpiprazole
- bromelain
- bromfenac ophthalmic
- budesonide
- bumetanide
- buprenorphine
- butorphanol
- cabazitaxel
- calaspargase
- calcitonin-salmon
- calcium carbonate
- candesartan cilexetil
- cangrelor
- capivasertib
- caplacizumab
- captopril
- carfilzomib
- cariprazine
- celecoxib
- cetuximab
- chikungunya vaccine
- chlorothiazide
- chlorthalidone
- cidofovir
- cilostazol
- cimetidine
- cinacalcet
- ciprofloxacin
- cisplatin
- clomipramine
- clonazepam
- clopidogrel
- clozapine
- collagenase clostridium histolyticum
- copanlisib
- corticotropin
- cortisone
- COVID-19 vaccine
- cyclophosphamide
- cyclosporine
- dabigatran
- dalteparin
- danazol
- danshen
- dapsone
- daridorexant
- darunavir
- dasatinib
- decitabine
- deferasirox
- defibrotide
- denosumab
- desmopressin
- desvenlafaxine
- deuruxolitinib
- deutetrabenazine
- dexamethasone
- dichlorphenamide
- diclofenac
- diclofenac ophthalmic
- diclofenac topical
- diflunisal
- digoxin
- diltiazem
- dimethyl fumarate
- dinutuximab
- diosmin
- diphtheria/tetanus vaccine
- diphtheria/tetanus/pertussis vaccine
- dipyridamole
- diroximel fumarate
- docetaxel
- drospirenone (contraceptive)
- drospirenone (hormone replacement)
- duloxetine
- duvelisib
- ebola vaccine, live
- edoxaban
- efbemalenograstim alfa
- eflapegrastim (G-CSF)
- elexacaftor/tezacaftor/ivacaftor
- elivaldogene autotemcel
- emapalumab
- enalapril
- enalaprilat
- enoxaparin
- epinephrine
- eplerenone
- epoprostenol
- erlotinib
- eslicarbazepine acetate
- estazolam
- estradiol (contraceptive)
- ethacrynic acid
- ethanol
- ethinyl estradiol (contraceptive)
- etodolac
- evening primrose oil
- everolimus
- exagamglogene autotemcel
- famotidine
- febuxostat
- fedratinib
- felodipine
- fenoprofen
- fenugreek
- filgrastim (G-CSF)
- finerenone
- flucytosine
- fludrocortisone
- fluphenazine
- flurbiprofen
- fluvoxamine
- fondaparinux
- formoterol inhaled
- fosamprenavir
- fosinopril
- fostamatinib
- fostemsavir
- fruquintinib
- furosemide
- futibatinib
- galantamine
- garlic
- gefitinib
- gentamicin
- gepirone
- ginkgo
- granisetron
- guanfacine
- Haemophilus b vaccine
- heparin
- hepatitis A vaccine
- hepatitis B vaccine
- human papillomavirus vaccine
- hydroxyurea
- ibandronate
- ibrutinib
- ibuprofen
- ibuprofen lysine
- icosapent ethyl
- ifosfamide
- iloprost inhaled
- imatinib
- indapamide
- indomethacin
- influenza H5N1 vaccine
- influenza vaccine
- insulin
- interferon beta 1a
- interferon beta 1b
- interferon gamma 1b
- irbesartan
- irinotecan
- isavuconazonium
- isoproterenol
- Japanese encephalitis vaccine
- ketoprofen
- ketorolac
- ketorolac ophthalmic
- landiolol
- lanthanum
- lapatinib
- leflunomide
- lenacapavir
- lenalidomide
- lenvatinib
- letermovir
- levalbuterol inhaled
- levomilnacipran
- licorice
- lidocaine
- lifileucel
- linezolid
- losartan
- lovotibeglogene autotemcel
- lumateperone
- lurasidone
- lymphocyte immune globulin, anti-thymocyte globulin
- magnesium carbonate
- magnesium citrate
- magnesium hydroxide
- magnesium oxide
- magnesium salicylate
- mannitol
- mavorixafor
- meclofenamate
- mefenamic acid
- mefloquine
- meloxicam
- meningococcal vaccine
- mercaptopurine
- mesalamine
- mesalamine rectal
- methazolamide
- methotrexate
- metronidazole
- midostaurin
- milnacipran
- mirtazapine
- moexipril
- monomethyl fumarate
- motixafortide
- mycophenolate mofetil
- mycophenolic acid
- nabumetone
- naproxen
- nattokinase
- necitumumab
- nepafenac ophthalmic
- netupitant
- niacin (vitamin B3)
- nifedipine
- nimodipine
- nintedanib
- nizatidine
- nortriptyline
- nusinersen
- ofloxacin
- olodaterol inhaled
- olsalazine
- omega-3-acid
- osilodrostat
- oxaprozin
- oxcarbazepine
- oxytocin
- palbociclib
- palopegteriparatide
- pamidronate
- panitumumab
- paroxetine
- pegaspargase
- pegfilgrastim (G-CSF)
- peginterferon alfa 2a
- peginterferon beta 1a
- pegloticase
- penicillin G
- pentosan polysulfate sodium
- pentoxifylline
- piperacillin
- piroxicam
- pirtobrutinib
- polyethylene glycol/electrolytes
- ponatinib
- potassium bicarbonate
- prednisolone
- probenecid
- proguanil
- promethazine
- pyridostigmine
- pyrimethamine
- quinapril
- ramipril
- ramucirumab
- ranibizumab
- ranolazine
- rasburicase
- red yeast rice
- respiratory syncytial virus vaccine
- resveratrol
- reteplase
- revakinagene taroretcel
- ribavirin
- rimegepant
- riociguat
- risedronate
- rituximab
- rivastigmine
- romosozumab
- ruxolitinib
- ruxolitinib topical
- sacituzumab govitecan
- salmeterol inhaled
- salsalate
- sargramostim (GM-CSF)
- sarilumab
- satralizumab
- saw palmetto
- sebetralstat
- selinexor
- sepiapterin
- sirolimus
- sirolimus albumin-bound
- smallpox/mpox vaccine, live
- sodium benzoate
- sodium bicarbonate
- sodium citrate
- sodium phenylacetate
- sodium phenylbutyrate
- sodium polystyrene sulfonate
- sodium thiosulfate
- sodium zirconium cyclosilicate
- sotatercept
- sparsentan
- spironolactone
- stiripentol
- succimer
- succinylcholine
- sulfasalazine
- sulfate bowel prep
- sulindac
- sunitinib
- suvorexant
- suzetrigine
- tadalafil
- tafasitamab
- tamsulosin
- telmisartan
- temsirolimus
- tenecteplase
- teplizumab
- terbutaline
- teriflunomide
- tezacaftor/ivacaftor
- thalidomide
- ticagrelor
- tick-borne encephalitis vaccine
- tirofiban
- tisotumab vedotin
- tivozanib
- tobramycin
- tocilizumab
- tofacitinib
- tolmetin
- tolterodine
- topiramate
- torsemide
- tovorafenib
- trabectedin
- trametinib
- trandolapril
- trastuzumab
- treprostinil
- triamcinolone
- triamterene
- triazolam
- trimethoprim
- typhoid vaccine
- ubrogepant
- upadacitinib
- vadadustat
- valbenazine
- valproic acid
- vamorolone
- vancomycin
- vanzacaftor/tezacaftor/deutivacaftor
- vasopressin
- venlafaxine
- verapamil
- vilanterol inhaled
- vilazodone
- vinblastine
- vincristine
- vinorelbine
- vinpocetine
- voclosporin
- vorapaxar
- vortioxetine
- warfarin
- willow bark
- zanubrutinib
- zidovudine
- ziv-aflibercept
- zoledronic acid
- zonisamide
Caution Advised
- armodafinil
- belzutifan
- bexarotene
- budesonide rectal
- clobazam
- darifenacin
- darolutamide
- dicloxacillin
- echinacea
- elafibranor
- elagolix
- eletriptan
- enasidenib
- felbamate
- ginseng, Asian
- glycerol phenylbutyrate
- grazoprevir
- griseofulvin
- istradefylline
- larotrectinib
- maraviroc
- meropenem
- naldemedine
- nevirapine
- odevixibat
- olutasidenib
- ospemifene
- perampanel
- pioglitazone
- roflumilast
- roflumilast topical
- rufinamide
- saxagliptin
- seladelpar
- sildenafil
- silodosin
- sirolimus topical
- sunvozertinib
- tecovirimat
- telotristat ethyl
- tretinoin
- vaborbactam
- vorasidenib
Adverse Reactions .
Serious Reactions
- QT prolongation
- torsades de pointes
- sudden death
- arterial thromboembolic event
- cardiac ischemia
- ischemic stroke
- thrombotic microangiopathy
- peripheral vascular disease
- thrombocytopenia
- neutropenia
- anemia
- hemorrhage, severe
- intracranial hemorrhage
- hypophosphatemia
- hypokalemia
- hyperkalemia
- hypocalcemia
- hyponatremia
- hepatotoxicity
- pancreatitis
- pneumonia
- pleural effusion
- pericardial effusion
- tumor lysis syndrome
- hypothyroidism
- hyperthyroidism
- HBV reactivation
- growth abnormalities (peds patients)
- osteonecrosis
Common Reactions
- rash
- headache
- nausea
- fatigue
- pruritus
- diarrhea
- URI
- arthralgia
- constipation
- cough
- vomiting
- fever
- pain
- asthenia
- muscle spasms
- dyspnea
- peripheral edema
- alopecia
- insomnia
- night sweats
- HTN
- appetite decr.
- dyspepsia
- influenza
- xeroderma
- dizziness
- gastroenteritis
- thrombocytopenia
- neutropenia
Safety/Monitoring .
Monitoring Parameters
pregnancy test at baseline; chemistry profile incl. electrolytes, Mg, Ca, PO4 at baseline, then periodically; LFTs at baseline, then qmo, and after dose adjustment; glucose, lipid panel at baseline, periodically x1y, then at least q12mo; ECG at baseline, then 7 days after tx start, after dose adjustment, and periodically; CBC w/ diff q2wk x2mo, then qmo; lipase qmo; weight; cardiac eval; growth (peds)
Look/Sound-Alike Drug Names
nilotinib confused with: neratinib; niraparib
Pregnancy/Lactation .
Pregnancy
Clinical Summary
weigh risk/benefit during pregnancy; no human data available; risk of embryo-fetal death, decr. fetal wt, and delayed skeletal ossification based on animal data at 0.5-2x systemic exposure and drug's mechanism of action
Individuals of Reproductive Potential
obtain pregnancy test before tx start; avoid pregnancy by using effective contraception during tx and x14 days after D/C in patients of childbearing potential
Lactation
Clinical Summary
avoid breastfeeding during tx and x14 days after D/C; no human data available to assess risk of infant harm or effects on milk production
Pharmacology .
Metabolism: liver; CYP450: 3A4 (primary), 2C8 substrate
Excretion: feces 93% (69% unchanged); Half-life: 14-17h
Subclass: Kinase Inhibitors, BCR-ABL Inhibitors
Mechanism of Action
inhibits BCR-ABL tyrosine kinase, inducing apoptosis in BCR-ABL-positive cell lines
Formulary .
No Formulary Selected
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