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Orgovyx
relugolix
Adult Dosing .
Dosage forms: TAB: 120 mg
prostate CA, advanced
- [120 mg PO qd]
- Start: 360 mg PO x1 on day 1; Info: restart 360 mg PO x1 if tx interrupted >7 days; do not cut/crush/chew tab
renal dosing
- [see below]
- CrCl >15: no adjustment; CrCl <15: not defined
- HD/PD: not defined
hepatic dosing
- [see below]
- Child-Pugh Class A or B: no adjustment; 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
- caution: male patients of reproductive potential
- caution: electrolyte abnormalities
- caution: long QT syndrome, congenital
- caution: QT prolongation
- caution: QT prolongation family history
- caution: torsades de pointes history
- caution: ventricular arrhythmia
- caution: bradycardia
- caution: MI, recent
- caution: CHF
Drug Interactions .
Overview
relugolix
GnRH antagonist
- CYP3A4 substrate
- P-gp substrate
- GnRH receptor antagonist
- prolongs QT interval (conditional)
Contraindicated
- pimozide
- thioridazine
Avoid/Use Alternative
- abrocitinib
- adagrasib
- aficamten
- amiodarone
- apalutamide
- arsenic trioxide
- asciminib
- azithromycin
- bedaquiline
- belumosudil
- berotralstat
- bisoprolol
- brigatinib
- butalbital
- canagliflozin
- cannabidiol
- capmatinib
- captopril
- carbamazepine
- carvedilol
- cimetidine
- cisapride
- clarithromycin
- cobicistat
- crizotinib
- cyclosporine
- danicopan
- danshen
- daridorexant
- darunavir
- dicloxacillin
- diltiazem
- diosmin
- domperidone
- dronedarone
- efavirenz
- elacestrant
- elexacaftor/tezacaftor/ivacaftor
- eliglustat
- enasidenib
- encorafenib
- entrectinib
- ephedra
- erdafitinib
- eribulin
- erythromycin
- estetrol (contraceptive)
- estradiol (contraceptive)
- ethinyl estradiol (contraceptive)
- etravirine
- felodipine
- fexinidazole
- flibanserin
- fluvoxamine
- fosfomycin injection
- fosphenytoin
- fostamatinib
- gilteritinib
- ginkgo
- glecaprevir
- goserelin
- histrelin
- hydroxychloroquine
- ibrutinib
- imlunestrant
- indomethacin
- isavuconazonium
- istradefylline
- itraconazole
- ivacaftor
- ivosidenib
- ketoconazole
- lapatinib
- ledipasvir
- lefamulin
- lenacapavir
- leuprolide
- levacetylleucine
- levoketoconazole
- lomitapide
- lonafarnib
- lopinavir/ritonavir
- lorlatinib
- lumacaftor/ivacaftor
- maribavir
- mavorixafor
- mifepristone
- milk thistle
- mirabegron
- mitapivat
- mitotane
- mobocertinib
- naproxen
- nefazodone
- nelfinavir
- neratinib
- nifedipine
- osimertinib
- pacritinib
- paroxetine
- pentobarbital
- phenobarbital
- phenytoin
- pibrentasvir
- pirtobrutinib
- ponatinib
- posaconazole
- primidone
- propafenone
- quercetin
- quinidine (antiarrhythmic)
- quinidine (CYP2D6 inhibitor)
- quinine
- quizartinib
- ranolazine
- remibrutinib
- rifabutin
- rifampin
- rifapentine
- rilzabrutinib
- ritonavir
- rolapitant
- rucaparib
- sarecycline
- selpercatinib
- sevabertinib
- simvastatin
- sorafenib
- sotagliflozin
- sotalol
- sotorasib
- sparsentan
- St. John's wort
- stiripentol
- sunvozertinib
- suvorexant
- tacrolimus
- taletrectinib
- telmisartan
- tepotinib
- tezacaftor/ivacaftor
- ticagrelor
- tipranavir
- tolvaptan
- toremifene
- trazodone
- trimethoprim
- triptorelin
- trofinetide
- tucatinib
- turmeric
- uridine triacetate
- valbenazine
- vandetanib
- vanzacaftor/tezacaftor/deutivacaftor
- velpatasvir
- vemurafenib
- venetoclax
- verapamil
- voclosporin
- voxilaprevir
- xanomeline
- ziprasidone
- zonisamide
Monitor/Modify Tx
- anagrelide
- apomorphine
- artemether/lumefantrine
- asenapine
- cabozantinib
- ceritinib
- chloroquine
- citalopram
- clofazimine
- degarelix
- desflurane
- desipramine
- dexmedetomidine
- dexmedetomidine injection
- disopyramide
- dofetilide
- donepezil
- dordaviprone
- droperidol
- epirubicin
- flecainide
- fluorouracil
- glasdegib
- haloperidol
- hydroxyzine
- ibutilide
- inotuzumab ozogamicin
- isoflurane
- levofloxacin
- lofexidine
- macimorelin
- methadone
- moxifloxacin
- nilotinib
- oliceridine
- ondansetron
- paliperidone
- palonosetron
- pasireotide
- pentamidine
- pretomanid
- procainamide
- revumenib
- ribociclib
- romidepsin
- sevoflurane
- telavancin
- tetrabenazine
- tramadol
- triclabendazole
- trifluridine
- vimseltinib
- ziftomenib
Caution Advised
- bosentan
- cenobamate
- dabrafenib
- estrogens, conjugated (hormone replacement)
- estrogens, esterified (hormone replacement)
- ethinyl estradiol (hormone replacement)
- mavacamten
- meropenem
- modafinil
- nafcillin
- oxcarbazepine
- pexidartinib
- repotrectinib
- vaborbactam
Adverse Reactions .
Serious Reactions
- QT prolongation
- arrhythmia
- MI
- AV block
- cardiac failure
- hemorrhage
- acute kidney injury
- hypersensitivity reaction
- angioedema
Common Reactions
- hot flashes
- musculoskeletal pain
- fatigue
- diarrhea
- constipation
- weight gain
- insomnia
- gynecomastia
- hyperhidrosis
- depression
- libido decr.
- glucose incr.
- triglycerides incr.
- Hgb decr.
- ALT or AST incr.
Safety/Monitoring .
Monitoring Parameters
consider ECG, electrolytes including Ca, Mg periodically
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 x2wk after D/C in male patients
Lactation
Clinical Summary
N/A; drug unlikely to be used while breastfeeding based on indication
Pharmacology .
Metabolism: for relugolix: unknown; CYP450: 2C8, 3A (primary) substrate
Excretion: for relugolix: feces 81% (4.2% unchanged), urine 4.1% (2.2% unchanged); Half-life: 60.8h
Subclass: Hormonal Oncologics, GnRH Analogs
Mechanism of Action
for relugolix: antagonizes pituitary GnRH receptors, suppressing gonadotropin (LH and FSH) release and reducing testicular steroidogenesis (GnRH antagonist)
Formulary .
No Formulary Selected
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