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Nubeqa
darolutamide
Adult Dosing .
Dosage forms: TAB: 300 mg
Special Note
- [uses, dosing may vary]
- Info: refer to institution protocols and pkg insert prior to prescribing for uses and dosing incl. toxicity-related dose adjustments
prostate CA
- [non-metastatic castration-resistant dz]
- Dose: 600 mg PO bid; Info: use w/ GnRH analog in pts w/o bilateral orchiectomy; give w/ food; do not cut/crush/chew tab
- [metastatic castration-sensitive dz]
- Dose: 600 mg PO bid; Info: use as monotherapy or w/ docetaxel; use w/ GnRH analog in pts w/o bilateral orchiectomy; give w/ food; do not cut/crush/chew tab
renal dosing
- [adjust dose amount]
- eGFR 15-29: 300 mg bid; eGFR <15: not defined
- HD/PD: not defined
hepatic dosing
- [adjust dose amount]
- Child-Pugh Class B: 300 mg bid; Child-Pugh Class C: not defined
Peds Dosing .
Peds dosing is currently unavailable or not applicable for this drug.
Contraindications / Cautions .
- hypersensitivity to drug or ingredient
- pregnancy
- caution: male pts of reproductive potential
- caution: CrCl <30
- caution: hepatic impairment, Child-Pugh Class B-C
- caution: cardiovascular dz risk
Drug Interactions .
Overview
darolutamide
antiandrogen
- CYP3A4 substrate
- P-gp substrate
- BCRP inhibitor
- OATP1B1 inhibitor, strong
- OATP1B3 inhibitor, strong
- CYP3A4 inducer, weak
- lowers seizure threshold
Contraindicated
- elagolix
- grazoprevir
- ranolazine
Avoid/Use Alternative
- aldesleukin
- alpelisib
- amifampridine
- apalutamide
- atazanavir
- atogepant
- atrasentan
- bosentan
- brincidofovir
- butalbital
- carbamazepine
- cenobamate
- cladribine oral
- codeine
- dabrafenib
- danshen
- desogestrel (contraceptive)
- dicloxacillin
- dienogest (contraceptive)
- dolutegravir
- drospirenone (contraceptive)
- efavirenz
- encorafenib
- enzalutamide
- estradiol (contraceptive)
- ethinyl estradiol (contraceptive)
- ethynodiol (contraceptive)
- etonogestrel (contraceptive)
- etravirine
- fentanyl
- fexinidazole
- fosamprenavir
- fosphenytoin
- iohexol
- ivosidenib
- levonorgestrel (contraceptive)
- levonorgestrel (post-coital contraceptive)
- lopinavir/ritonavir
- lorlatinib
- lovastatin
- lumacaftor/ivacaftor
- lumateperone
- mavacamten
- medroxyprogesterone (contraceptive)
- meperidine
- mitapivat
- mitotane
- modafinil
- nafcillin
- norelgestromin (contraceptive)
- norethindrone (contraceptive)
- norgestimate (contraceptive)
- norgestrel (contraceptive)
- oliceridine
- oxycodone
- pacritinib
- pazopanib
- pentobarbital
- pexidartinib
- phenobarbital
- phenytoin
- pitavastatin
- primidone
- red yeast rice
- repotrectinib
- resmetirom
- revefenacin inhaled
- rifabutin
- rifampin
- rifapentine
- segesterone (contraceptive)
- sotorasib
- St. John's wort
- tenofovir disoproxil
- tipranavir
- topotecan
- tramadol
- turmeric
- ulipristal (post-coital contraceptive)
- voxilaprevir
- zavegepant
- zuranolone
Monitor/Modify Tx
- amlodipine
- atorvastatin
- buprenorphine
- bupropion
- cyclophosphamide
- cyclosporine
- diltiazem
- disopyramide
- eluxadoline
- erdafitinib
- erythromycin
- everolimus
- fluvastatin
- glyburide
- ifosfamide
- imatinib
- iopamidol
- irinotecan
- isradipine
- ketoconazole
- lapatinib
- maraviroc
- methotrexate
- mitoxantrone
- momelotinib
- nateglinide
- nicardipine
- nimodipine
- nisoldipine
- perampanel
- pravastatin
- quinidine (antiarrhythmic)
- repaglinide
- riociguat
- rosuvastatin
- simvastatin
- sirolimus
- tacrolimus
- talazoparib
- tenofovir alafenamide
- tiagabine
- ubrogepant
- valsartan
- venetoclax
- vimseltinib
- voriconazole
- warfarin
Caution Advised
- abemaciclib
- abrocitinib
- acalabrutinib
- acetazolamide
- adagrasib
- alfentanil
- alprazolam
- amiodarone
- aprepitant
- artemether/lumefantrine
- asciminib
- avacopan
- avapritinib
- axitinib
- azithromycin
- belumosudil
- berotralstat
- bictegravir
- bisoprolol
- bosutinib
- brigatinib
- brivaracetam
- budesonide
- buspirone
- busulfan
- cabozantinib
- canagliflozin
- cannabidiol
- capivasertib
- capmatinib
- captopril
- carvedilol
- ceritinib
- chlorambucil
- chloramphenicol
- cimetidine
- clarithromycin
- clobazam
- clomipramine
- clonazepam
- clorazepate
- cobicistat
- cobimetinib
- conivaptan
- crizotinib
- danicopan
- daridorexant
- darunavir
- dasatinib
- defactinib
- deflazacort
- diazepam
- diosmin
- doravirine
- dronedarone
- drospirenone (hormone replacement)
- elacestrant
- elbasvir
- elexacaftor/tezacaftor/ivacaftor
- eliglustat
- elvitegravir
- enasidenib
- entrectinib
- erlotinib
- eslicarbazepine acetate
- ethosuximide
- fedratinib
- felbamate
- felodipine
- fenfluramine
- finerenone
- flibanserin
- fluvoxamine
- fosaprepitant
- fostamatinib
- fruquintinib
- futibatinib
- gabapentin
- ganaxolone
- gepirone
- gilteritinib
- ginkgo
- glasdegib
- glecaprevir
- guanfacine
- haloperidol
- hydrocortisone
- hydroxychloroquine
- ibrutinib
- idelalisib
- indomethacin
- infigratinib
- isavuconazonium
- istradefylline
- itraconazole
- ivacaftor
- lacosamide
- lamotrigine
- larotrectinib
- lasmiditan
- lazertinib
- ledipasvir
- lefamulin
- lenacapavir
- leniolisib
- letermovir
- levacetylleucine
- levetiracetam
- levoketoconazole
- levonorgestrel intrauterine device (contraceptive)
- lindane topical
- lomitapide
- lonafarnib
- lorazepam
- lurasidone
- macitentan
- magnesium citrate
- maribavir
- mavorixafor
- meropenem
- methadone
- methsuximide
- midazolam
- midostaurin
- mifepristone
- milk thistle
- mirabegron
- mobocertinib
- naldemedine
- naloxegol
- naproxen
- nefazodone
- nelfinavir
- neratinib
- netupitant
- nevirapine
- nifedipine
- nilotinib
- nirmatrelvir
- nirogacestat
- olaparib
- olutasidenib
- osimertinib
- oxcarbazepine
- palbociclib
- paroxetine
- pemigatinib
- pibrentasvir
- pimavanserin
- pirtobrutinib
- polyethylene glycol
- polyethylene glycol/electrolytes
- ponatinib
- posaconazole
- praziquantel
- pregabalin
- pretomanid
- promethazine
- propafenone
- quercetin
- quetiapine
- quinidine (CYP2D6 inhibitor)
- quinine
- quizartinib
- ribociclib
- rilpivirine
- ripretinib
- ritonavir
- roflumilast
- rolapitant
- rucaparib
- rufinamide
- samidorphan
- sarecycline
- seladelpar
- selpercatinib
- selumetinib
- sildenafil
- sirolimus albumin-bound
- sodium picosulfate
- sonidegib
- sorafenib
- sotagliflozin
- sparsentan
- stiripentol
- sulfasalazine
- sulfate bowel prep
- suvorexant
- suzetrigine
- tadalafil
- tamoxifen
- tasimelteon
- tazemetostat
- telmisartan
- temsirolimus
- tepotinib
- tezacaftor/ivacaftor
- ticagrelor
- tofacitinib
- tolvaptan
- topiramate
- toremifene
- trazodone
- treosulfan
- trimethoprim
- tucatinib
- uridine triacetate
- vaborbactam
- valbenazine
- valproic acid
- vandetanib
- vanzacaftor/tezacaftor/deutivacaftor
- velpatasvir
- vemurafenib
- verapamil
- vigabatrin
- voclosporin
- vonoprazan
- voxelotor
- xanomeline
- zanubrutinib
- zonisamide
Adverse Reactions .
Serious Reactions
- ischemic heart dz
- cardiac failure
- cardiac arrest
- arrhythmia
- pulmonary embolism
- seizures
- sepsis
- pneumonia
- UTI
- urinary retention
- hematuria
- hemorrhage
Common Reactions
- fatigue
- extremity pain
- rash
- ischemic heart dz
- heart failure
- HTN
- hemorrhage (combo tx)
- fractures (combo tx)
- ALT or AST incr.
- neutrophils decr.
- bilirubin incr.
Safety/Monitoring .
Monitoring Parameters
cardiac fxn
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 x1wk after D/C in male pts
Lactation
Clinical Summary
N/A; drug unlikely to be used while breastfeeding based on indication
Pharmacology .
Metabolism: unknown; CYP450: 3A4 substrate; UGT: 1A1, 1A9 substrate; Info: active metabolite
Excretion: urine 63% (7% unchanged), feces 32% (30% unchanged); Half-life: 20h
Subclass: Hormonal Oncologics, Antiandrogens
Mechanism of Action
binds and inhibits androgen receptors
Formulary .
No Formulary Selected
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