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Xtandi
enzalutamide
Adult Dosing .
Dosage forms: CAP: 40 mg; TAB: 40 mg, 80 mg
Special Note
- [uses, dosing may vary]
- Info: refer to institution protocols and pkg insert prior to prescribing for uses and dosing including toxicity-related dose adjustments
prostate CA
- [castration-resistant disease]
- Dose: 160 mg PO qd; Info: use with GnRH analog in patients without bilateral orchiectomy; do not open/dissolve cap; do not cut/crush/chew tab
- [metastatic castration-sensitive disease]
- Dose: 160 mg PO qd; Info: use with GnRH analog in patients without bilateral orchiectomy; do not open/dissolve cap; do not cut/crush/chew tab
- [non-metastatic castration-sensitive, high-risk disease]
- Dose: 160 mg PO qd; Info: for patients with biochemical recurrence; may suspend tx if PSA <0.2 ng/mL after 36wk tx; reinitiate when PSA 2 ng/mL or greater for patients with radical prostatectomy history or PSA 5 ng/mL or greater for patients with primary XRT history; do not open/dissolve cap; do not cut/crush/chew tab
renal dosing
- [see below]
- CrCl >30: no adjustment; CrCl <30: not defined
- HD/PD: not defined
hepatic dosing
- [no adjustment]
Peds Dosing .
Peds dosing is currently unavailable or not applicable for this drug.
Contraindications / Cautions .
- hypersensitivity to drug or ingredient
- caution: male patients of reproductive potential
- caution: seizure risk
- caution: cardiovascular disease risk
- caution: fracture risk
Drug Interactions .
Overview
enzalutamide
antiandrogen
- CYP2C8 substrate
- CYP3A4 substrate
- P-gp inhibitor, weak
- CYP2C9 inducer, moderate
- CYP2C19 inducer, moderate
- CYP3A4 inducer, strong
- lowers seizure threshold
Contraindicated
- artemether/lumefantrine
- atazanavir
- colchicine
- doravirine
- elbasvir
- fostemsavir
- grazoprevir
- isavuconazonium
- lenacapavir
- lonafarnib
- lorlatinib
- lurasidone
- mavacamten
- nirmatrelvir
- pacritinib
- praziquantel
- ranolazine
- tipranavir
- zoliflodacin
Avoid/Use Alternative
- abemaciclib
- abiraterone acetate
- acalabrutinib
- acoramidis
- adagrasib
- aldesleukin
- alfentanil
- alpelisib
- amifampridine
- apalutamide
- apixaban
- apremilast
- aprepitant
- aripiprazole bimonthly injection
- aripiprazole lauroxil
- aripiprazole monthly injection
- atogepant
- atrasentan
- avacopan
- avanafil
- avapritinib
- axitinib
- bedaquiline
- bictegravir
- bortezomib
- bosutinib
- brigatinib
- buprenorphine
- buspirone
- butalbital
- cabozantinib
- capivasertib
- capmatinib
- carbamazepine
- cariprazine
- ceritinib
- clarithromycin
- clozapine
- cobicistat
- cobimetinib
- codeine
- copanlisib
- crizotinib
- dabigatran
- daridorexant
- darolutamide
- dasatinib
- defactinib
- deflazacort
- desogestrel (contraceptive)
- deuruxolitinib
- dexamethasone
- diazoxide
- dienogest (contraceptive)
- dihydrocodeine
- diltiazem
- dolutegravir
- dordaviprone
- doxorubicin
- dronedarone
- drospirenone (contraceptive)
- duvelisib
- elacestrant
- elexacaftor/tezacaftor/ivacaftor
- eliglustat
- elinzanetant
- elvitegravir
- encorafenib
- ensartinib
- entrectinib
- erdafitinib
- erlotinib
- estradiol (contraceptive)
- ethinyl estradiol (contraceptive)
- ethynodiol (contraceptive)
- etonogestrel (contraceptive)
- everolimus
- fedratinib
- felodipine
- fenfluramine
- fentanyl
- fexinidazole
- finerenone
- flibanserin
- fosamprenavir
- fosaprepitant
- fosphenytoin
- fostamatinib
- fruquintinib
- futibatinib
- ganaxolone
- gemfibrozil
- gepirone
- gepotidacin
- gilteritinib
- glasdegib
- glecaprevir
- hydrocodone
- ibrexafungerp
- ibrutinib
- idelalisib
- imatinib
- imlunestrant
- iohexol
- irinotecan
- isradipine
- istradefylline
- itraconazole
- ivabradine
- ivacaftor
- ivosidenib
- ixabepilone
- ixazomib
- ketoconazole
- lapatinib
- larotrectinib
- lazertinib
- lefamulin
- lemborexant
- leniolisib
- letermovir
- levoketoconazole
- levonorgestrel (contraceptive)
- levonorgestrel (post-coital contraceptive)
- linagliptin
- lopinavir/ritonavir
- lumacaftor/ivacaftor
- lumateperone
- lurbinectedin
- macitentan
- maraviroc
- maribavir
- mavorixafor
- medroxyprogesterone (contraceptive)
- meperidine
- methadone
- midazolam
- midostaurin
- mifepristone
- mitapivat
- mitotane
- mobocertinib
- naldemedine
- naloxegol
- nefazodone
- nelfinavir
- nerandomilast
- neratinib
- netupitant
- nevirapine
- nicardipine
- nifedipine
- nilotinib
- nimodipine
- nintedanib
- nirogacestat
- nisoldipine
- norelgestromin (contraceptive)
- norethindrone (contraceptive)
- norgestimate (contraceptive)
- norgestrel (contraceptive)
- olaparib
- oliceridine
- olutasidenib
- omaveloxolone
- osimertinib
- oxycodone
- palbociclib
- paliperidone
- palovarotene
- pazopanib
- pemigatinib
- pentobarbital
- pexidartinib
- phenobarbital
- phenytoin
- pimavanserin
- pirtobrutinib
- ponatinib
- pralsetinib
- pretomanid
- primidone
- quinine
- quizartinib
- regorafenib
- remibrutinib
- repotrectinib
- revumenib
- ribociclib
- rifabutin
- rifampin
- rilpivirine
- rilzabrutinib
- rimegepant
- ripretinib
- ritlecitinib
- ritonavir
- rivaroxaban
- roflumilast
- rolapitant
- romidepsin
- samidorphan
- sebetralstat
- segesterone (contraceptive)
- selpercatinib
- selumetinib
- sevabertinib
- simvastatin
- siponimod
- sirolimus
- sirolimus albumin-bound
- sonidegib
- sorafenib
- sotorasib
- sparsentan
- St. John's wort
- stiripentol
- sufentanil
- sunitinib
- sunvozertinib
- suzetrigine
- tadalafil
- taletrectinib
- tamoxifen
- tasimelteon
- tazemetostat
- temsirolimus
- tezacaftor/ivacaftor
- thiotepa
- ticagrelor
- tivozanib
- tofacitinib
- tolvaptan
- topotecan
- toremifene
- trabectedin
- tramadol
- tretinoin
- triazolam
- tucatinib
- ubrogepant
- ulipristal (post-coital contraceptive)
- upadacitinib
- valbenazine
- vandetanib
- vanzacaftor/tezacaftor/deutivacaftor
- velpatasvir
- vemurafenib
- venetoclax
- verapamil
- vinblastine
- vincristine
- vinorelbine
- voclosporin
- vonoprazan
- vorapaxar
- voriconazole
- voxilaprevir
- zaleplon
- zanubrutinib
- ziftomenib
- zolpidem
- zongertinib
- zuranolone
Monitor/Modify Tx
- afatinib
- aficamten
- aminophylline
- amitriptyline
- amlodipine
- aripiprazole oral
- atorvastatin
- avatrombopag
- belumosudil
- betamethasone
- brexpiprazole
- bupropion
- butorphanol
- calcitriol
- cannabidiol
- carvedilol
- celecoxib
- cholecalciferol (vitamin D3)
- clobazam
- cortisone
- crinecerfont
- cyclophosphamide
- cyclosporine
- diclofenac
- digoxin
- disopyramide
- doxercalciferol
- edoxaban
- enfortumab vedotin
- eravacycline
- ethosuximide
- exemestane
- fludrocortisone
- gefitinib
- glimepiride
- guanfacine
- haloperidol
- hydrocortisone
- ifosfamide
- imipramine
- iopamidol
- macimorelin
- methylprednisolone
- mirtazapine
- morphine
- nateglinide
- nortriptyline
- osilodrostat
- oxcarbazepine
- paltusotine
- perampanel
- pitolisant
- prednisolone
- prednisone
- propranolol
- quetiapine
- quinidine (antiarrhythmic)
- repaglinide
- risperidone
- seladelpar
- sildenafil
- tacrolimus
- talazoparib
- tenofovir alafenamide
- tenofovir disoproxil
- theophylline
- tiagabine
- torsemide
- trazodone
- triamcinolone
- vilazodone
- vortioxetine
- warfarin
- zonisamide
Caution Advised
- abrocitinib
- acetazolamide
- albendazole
- aliskiren
- alprazolam
- amiodarone
- armodafinil
- asciminib
- bosentan
- brentuximab vedotin
- brivaracetam
- bromocriptine
- budesonide
- busulfan
- cannabis
- carisoprodol
- cenobamate
- chlorambucil
- citalopram
- clindamycin
- clomipramine
- clonazepam
- clopidogrel
- clorazepate
- dabrafenib
- dapsone
- darunavir
- deferasirox
- dexlansoprazole
- diazepam
- domperidone
- donepezil
- dronabinol
- drospirenone (hormone replacement)
- efavirenz
- elagolix
- eplerenone
- erythromycin
- escitalopram
- eslicarbazepine acetate
- esomeprazole
- estradiol (hormone replacement)
- estrogens, conjugated (hormone replacement)
- estrogens, esterified (hormone replacement)
- eszopiclone
- ethinyl estradiol (hormone replacement)
- etoposide
- etrasimod
- etravirine
- felbamate
- fesoterodine
- finasteride
- fingolimod
- fluvastatin
- gabapentin
- glyburide
- hydroxychloroquine
- isotretinoin
- lacosamide
- lamotrigine
- lansoprazole
- leflunomide
- levetiracetam
- levonorgestrel (hormone replacement)
- levonorgestrel intrauterine device (contraceptive)
- lorazepam
- lovastatin
- magnesium citrate
- medroxyprogesterone (hormone replacement)
- mefloquine
- methsuximide
- methylergonovine
- metoclopramide
- modafinil
- montelukast
- nafcillin
- norethindrone (hormone replacement)
- olanzapine
- omeprazole
- ondansetron
- ospemifene
- paclitaxel
- paroxetine
- pibrentasvir
- polatuzumab vedotin
- polyethylene glycol
- polyethylene glycol/electrolytes
- pregabalin
- progesterone (hormone replacement)
- progesterone vaginal (hormone replacement)
- promethazine
- propafenone
- quinidine (CYP2D6 inhibitor)
- ramelteon
- red yeast rice
- rifapentine
- riociguat
- rufinamide
- ruxolitinib
- selegiline
- sertraline
- sodium picosulfate
- solifenacin
- sulfate bowel prep
- suvorexant
- telisotuzumab vedotin
- terbinafine
- teriflunomide
- tinidazole
- tisotumab vedotin
- topiramate
- treosulfan
- valproic acid
- vigabatrin
Adverse Reactions .
Serious Reactions
- seizures
- posterior reversible encephalopathy syndrome
- infection, severe
- ischemic heart disease
- fractures
- hypersensitivity reaction
- Stevens-Johnson syndrome
- erythema multiforme
- toxic epidermal necrolysis
- drug reaction with eosinophilia and systemic symptoms
- acute generalized exanthematous pustulosis
- dysphagia, severe
Common Reactions
- asthenia
- fatigue
- hot flashes
- back pain
- diarrhea
- musculoskeletal pain
- HTN
- arthralgia
- constipation
- appetite decr.
- dizziness
- vertigo
- headache
- respiratory infection
- fractures
- peripheral edema
- insomnia
- gynecomastia
- mental impairment
- nausea
- weight decr.
- hematuria
- breast tenderness
- dyspnea
- muscular weakness
- hemorrhage
- hyperglycemia
- Hgb decr.
- neutrophils decr.
Safety/Monitoring .
Monitoring Parameters
no routine tests recommended
Pregnancy/Lactation .
Pregnancy
Clinical Summary
N/A; drug unlikely to be used during pregnancy based on indication
Individuals of Reproductive Potential
avoid pregnancy by using effective contraception during tx and x3mo after D/C in male patients
Lactation
Clinical Summary
N/A; drug unlikely to be used while breastfeeding based on indication
Pharmacology .
Metabolism: for enzalutamide: liver; CYP450: 2C8 (primary), 3A4 substrate; Info: active metabolite
Excretion: for enzalutamide: urine 71% (minimally unchanged), feces 14% (0.4% unchanged); Half-life: 5.8 days (parent drug), 7.8-8.6 days (active metabolite)
Subclass: Hormonal Oncologics, Antiandrogens
Mechanism of Action
for enzalutamide: binds and inhibits androgen receptors
Formulary .
No Formulary Selected
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